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Synthesis, In Vivo and In Silico Evaluation of Analgesic, Anti-Inflammatory and Antidiarrheal Activities of Benzimidazole Derivatives
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-05 DOI: 10.1002/slct.202401267
Saikat Kumar Poddar, Poushali Saha, Sabiha Enam Spriha, S. M. Abdur Rahman

A number of benzimidazole derivatives (3a–3d) were synthesized in high yields (66–94%) by condensing carboxylic acid and aromatic diamine, namely o-phenylenediamine, in the presence of concentrated HCl and evaluated for their analgesic, anti-inflammatory, and antidiarrheal actions in both in vivo and in silico methods. Among the synthesized compounds, compounds 3d and 3b showed the most potent analgesic (62.3% and 58.98% writhing inhibition respectively), and compound 3c and 3d showed anti-inflammatory activity in 1st hour to 4th hour (76.36, 76.60, 71.43, 73.29, and 80.61, 88.30, 80.52, and 66.07% inhibition of paw edema, respectively) compared to standard diclofenac sodium (92.54% writhing inhibition and 56.97, 78.72, 90.91, and 99.64% inhibition of paw edema). Compound 3a showed the most significant antidiarrheal activity (66.67% inhibition of defecation) compared to standard loperamide (75.0%) at 50 mg/kg dose. In molecular docking analysis, compound 3d showed the highest binding affinity toward COX-1 and COX-2 (−8.7 and −8.9 kcal/mol respectively) compared to standard diclofenac sodium (−8.2 and −8.4 kcal/mol), which is consistent with the in vivo result. Molecular docking thus revealed that analgesic and anti-inflammatory activity is likely to be related to inhibition of COX enzymes, with the structure of the substituents having an effect on both binding affinity and selectivity. On the other hand, compounds 3c and 3d showed the highest binding (−9.1 and −10.2 kcal/mol) compared to loperamide (−8.4 kcal/mol) against kappa opioid receptor (KOR). Since compound 3a did not show much affinity toward KOR, suggesting a potential different target and/or mechanism. So, the synthesized benzimidazole derivatives could act as potential leads for developing new analgesic and antidiarrheal molecules.

{"title":"Synthesis, In Vivo and In Silico Evaluation of Analgesic, Anti-Inflammatory and Antidiarrheal Activities of Benzimidazole Derivatives","authors":"Saikat Kumar Poddar,&nbsp;Poushali Saha,&nbsp;Sabiha Enam Spriha,&nbsp;S. M. Abdur Rahman","doi":"10.1002/slct.202401267","DOIUrl":"https://doi.org/10.1002/slct.202401267","url":null,"abstract":"<p>A number of benzimidazole derivatives (<b>3a–3d</b>) were synthesized in high yields (66–94%) by condensing carboxylic acid and aromatic diamine, namely <i>o</i>-phenylenediamine, in the presence of concentrated HCl and evaluated for their analgesic, anti-inflammatory, and antidiarrheal actions in both in vivo and in silico methods. Among the synthesized compounds, compounds <b>3d</b> and <b>3b</b> showed the most potent analgesic (62.3% and 58.98% writhing inhibition respectively), and compound <b>3c</b> and <b>3d</b> showed anti-inflammatory activity in 1st hour to 4th hour (76.36, 76.60, 71.43, 73.29, and 80.61, 88.30, 80.52, and 66.07% inhibition of paw edema, respectively) compared to standard diclofenac sodium (92.54% writhing inhibition and 56.97, 78.72, 90.91, and 99.64% inhibition of paw edema). Compound <b>3a</b> showed the most significant antidiarrheal activity (66.67% inhibition of defecation) compared to standard loperamide (75.0%) at 50 mg/kg dose. In molecular docking analysis, compound <b>3d</b> showed the highest binding affinity toward COX-1 and COX-2 (−8.7 and −8.9 kcal/mol respectively) compared to standard diclofenac sodium (−8.2 and −8.4 kcal/mol), which is consistent with the in vivo result. Molecular docking thus revealed that analgesic and anti-inflammatory activity is likely to be related to inhibition of COX enzymes, with the structure of the substituents having an effect on both binding affinity and selectivity. On the other hand, compounds <b>3c</b> and <b>3d</b> showed the highest binding (−9.1 and −10.2 kcal/mol) compared to loperamide (−8.4 kcal/mol) against kappa opioid receptor (KOR). Since compound <b>3a</b> did not show much affinity toward KOR, suggesting a potential different target and/or mechanism. So, the synthesized benzimidazole derivatives could act as potential leads for developing new analgesic and antidiarrheal molecules.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554245","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, Hydrolytic Behavior, and Anticancer Activity of a PAMAM–Janus Dendrimer Conjugates with Prednisone and Ibuprofen
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-05 DOI: 10.1002/slct.202404544
Israel Barajas-Mendoza, Irving Osiel Castillo-Rodríguez, Isabel Hernández-Rioja, Elena Martínez-Klimova, Teresa Ramírez-Ápan, Marcos Martínez-García

Herein, we report the synthesis of an ibuprofen dendron with an alkyne focal group and prednisone dendron with an azide focal group, both with polyamidoamine (PAMAM) chains. The Janus dendrimer was obtained via a Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC) reaction. Dendrons and dendrimers are stable at acidic pH values but undergo hydrolysis at alkaline pH 7.4. The Janus dendrimer conjugate with ibuprofen–prednisone had a better time of action (t½) than did the other dendrons. The anticancer activity studies revealed the best activity against human chronic myelogenous leukemia (K-562) cells.

{"title":"Synthesis, Hydrolytic Behavior, and Anticancer Activity of a PAMAM–Janus Dendrimer Conjugates with Prednisone and Ibuprofen","authors":"Israel Barajas-Mendoza,&nbsp;Irving Osiel Castillo-Rodríguez,&nbsp;Isabel Hernández-Rioja,&nbsp;Elena Martínez-Klimova,&nbsp;Teresa Ramírez-Ápan,&nbsp;Marcos Martínez-García","doi":"10.1002/slct.202404544","DOIUrl":"https://doi.org/10.1002/slct.202404544","url":null,"abstract":"<p>Herein, we report the synthesis of an ibuprofen dendron with an alkyne focal group and prednisone dendron with an azide focal group, both with polyamidoamine (PAMAM) chains. The Janus dendrimer was obtained via a Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC) reaction. Dendrons and dendrimers are stable at acidic pH values but undergo hydrolysis at alkaline pH 7.4. The Janus dendrimer conjugate with ibuprofen–prednisone had a better time of action (<i>t</i>½) than did the other dendrons. The anticancer activity studies revealed the best activity against human chronic myelogenous leukemia (K-562) cells.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554247","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Mesoporous Graphitic Carbon Nitride Photocatalyzed 6‑Substituted Phenanthridines Synthesis from 2‑Isocyanobiaryls
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-04 DOI: 10.1002/slct.202500082
Jie Gao, Tiankai Zhang, Quan Zhu, Chuan Bai, Dr. Pan Gao, Dr. Guodong Zhang, Prof. Dr. Feng Chen

Mesoporous graphitic carbon nitride (mpg-CN) has been successfully employed as a highly efficient photocatalyst for the annulation of 2-isocyanobiaryls with ethers to synthesize 6-substituted phenanthridines. This method facilitates the preparation of a diverse range of 6-substituted phenanthridines, demonstrating a broad substrate scope under mild and environmentally benign reaction conditions. The versatility of this approach allows for the incorporation of various functional groups, making it a valuable tool for the synthesis of complex phenanthridine derivatives. Notably, this transition metal-free heterogeneous photocatalytic system offers significant advantages over traditional methods, which often rely on expensive precious metal catalysts. The system achieves reduced costs and enhanced sustainability by eliminating the need for such metals. Additionally, the recyclability of the mpg-CN catalyst is a key feature, as it can be reused for five consecutive cycles without significant loss of catalytic activity. This durability not only improves the economic feasibility of the process but also aligns with the principles of green chemistry by minimizing waste. The combination of mild conditions, cost-effectiveness, and recyclability positions this method as a practical and scalable alternative for the synthesis of 6-substitued phenanthridines.

{"title":"Mesoporous Graphitic Carbon Nitride Photocatalyzed 6‑Substituted Phenanthridines Synthesis from 2‑Isocyanobiaryls","authors":"Jie Gao,&nbsp;Tiankai Zhang,&nbsp;Quan Zhu,&nbsp;Chuan Bai,&nbsp;Dr. Pan Gao,&nbsp;Dr. Guodong Zhang,&nbsp;Prof. Dr. Feng Chen","doi":"10.1002/slct.202500082","DOIUrl":"https://doi.org/10.1002/slct.202500082","url":null,"abstract":"<p>Mesoporous graphitic carbon nitride (mpg-CN) has been successfully employed as a highly efficient photocatalyst for the annulation of 2-isocyanobiaryls with ethers to synthesize 6-substituted phenanthridines. This method facilitates the preparation of a diverse range of 6-substituted phenanthridines, demonstrating a broad substrate scope under mild and environmentally benign reaction conditions. The versatility of this approach allows for the incorporation of various functional groups, making it a valuable tool for the synthesis of complex phenanthridine derivatives. Notably, this transition metal-free heterogeneous photocatalytic system offers significant advantages over traditional methods, which often rely on expensive precious metal catalysts. The system achieves reduced costs and enhanced sustainability by eliminating the need for such metals. Additionally, the recyclability of the mpg-CN catalyst is a key feature, as it can be reused for five consecutive cycles without significant loss of catalytic activity. This durability not only improves the economic feasibility of the process but also aligns with the principles of green chemistry by minimizing waste. The combination of mild conditions, cost-effectiveness, and recyclability positions this method as a practical and scalable alternative for the synthesis of 6-substitued phenanthridines.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554604","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Surface-Functionalized PAMAM Dendrimers as Synthetic Chaperones for Prevention of Bovine γ-Crystallin Aggregation
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-04 DOI: 10.1002/slct.202405327
Ashleigh N. Bristol, Lisa K. Kemp, Vijayaraghavan Rangachari, Eric R. George, Sarah E. Morgan

We present a fundamental study that supports the feasibility of delaying the onset of presbyopia and age-related cataracts via the utilization of surface-functionalized poly(amidoamine) (PAMAM) dendrimers. These PAMAM derivatives are known to have the added benefit of permeating the human cornea with possible absorption/distribution into the crystalline lens, indicating the potential for use in a topically applied eye solution. Mature onset cataract formation occurs because of γ-crystallin and β-crystallin aggregation in the human lens over time. As the molecular chaperone α-crystallin becomes saturated with unfolded γ-crystallins, the ability to prevent aggregation becomes limited. PAMAM dendrimers containing either sodium carboxylate- or succinamic acid-surface functionality are employed as synthetic chaperones to evaluate the effect of structure and local concentration on γ-crystallin aggregation. The chaperone/γ-crystallin blends are examined via DLS, zeta potential measurements, and fluorescence spectroscopy. DLS studies show a reduction in hydrodynamic size for γ-crystallin in the presence of PAMAM dendrimers and their small molecule counterparts compared to the control. Structural identity and local concentration of functionality are found to impact solution behavior. Zeta potential measurements and fluorescence studies indicate that synthetic chaperones can have multiple modes of non-covalent interactions and are the most effective in preventing or reducing γ-crystallin aggregation.

{"title":"Surface-Functionalized PAMAM Dendrimers as Synthetic Chaperones for Prevention of Bovine γ-Crystallin Aggregation","authors":"Ashleigh N. Bristol,&nbsp;Lisa K. Kemp,&nbsp;Vijayaraghavan Rangachari,&nbsp;Eric R. George,&nbsp;Sarah E. Morgan","doi":"10.1002/slct.202405327","DOIUrl":"https://doi.org/10.1002/slct.202405327","url":null,"abstract":"<p>We present a fundamental study that supports the feasibility of delaying the onset of presbyopia and age-related cataracts via the utilization of surface-functionalized poly(amidoamine) (PAMAM) dendrimers. These PAMAM derivatives are known to have the added benefit of permeating the human cornea with possible absorption/distribution into the crystalline lens, indicating the potential for use in a topically applied eye solution. Mature onset cataract formation occurs because of γ-crystallin and β-crystallin aggregation in the human lens over time. As the molecular chaperone α-crystallin becomes saturated with unfolded γ-crystallins, the ability to prevent aggregation becomes limited. PAMAM dendrimers containing either sodium carboxylate- or succinamic acid-surface functionality are employed as synthetic chaperones to evaluate the effect of structure and local concentration on γ-crystallin aggregation. The chaperone/γ-crystallin blends are examined via DLS, zeta potential measurements, and fluorescence spectroscopy. DLS studies show a reduction in hydrodynamic size for γ-crystallin in the presence of PAMAM dendrimers and their small molecule counterparts compared to the control. Structural identity and local concentration of functionality are found to impact solution behavior. Zeta potential measurements and fluorescence studies indicate that synthetic chaperones can have multiple modes of non-covalent interactions and are the most effective in preventing or reducing γ-crystallin aggregation.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554603","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Recent Advancements in Metal-Free Catalysis for Cyclopropane Ring Cleavage
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-04 DOI: 10.1002/slct.202500035
Amit Pramanik, Asit Kumar Das, Sanjay Bhar, Avishek Ghatak

Over the last decade, there have been notable advances in the field of ring opening reaction of numerous cyclopropane derivatives under metal-free conditions including donor–acceptor cyclopropanes, acceptor-activated cyclopropanes, alkylidenecyclopropanes, cyclopropyl alcohols, and vinylidenecyclopropanes. This review article aims to offer a comprehensive overview on cleavage reactions of cyclopropanes using Bronsted and Lewis acids, organic and inorganic bases, TCT-DMF, ionic liquids etc. Photoinduced and catalyst-free ring cleavage of cyclopropanes are also accentuated in this review.

{"title":"Recent Advancements in Metal-Free Catalysis for Cyclopropane Ring Cleavage","authors":"Amit Pramanik,&nbsp;Asit Kumar Das,&nbsp;Sanjay Bhar,&nbsp;Avishek Ghatak","doi":"10.1002/slct.202500035","DOIUrl":"https://doi.org/10.1002/slct.202500035","url":null,"abstract":"<p>Over the last decade, there have been notable advances in the field of ring opening reaction of numerous cyclopropane derivatives under metal-free conditions including donor–acceptor cyclopropanes, acceptor-activated cyclopropanes, alkylidenecyclopropanes, cyclopropyl alcohols, and vinylidenecyclopropanes. This review article aims to offer a comprehensive overview on cleavage reactions of cyclopropanes using Bronsted and Lewis acids, organic and inorganic bases, TCT-DMF, ionic liquids etc. Photoinduced and catalyst-free ring cleavage of cyclopropanes are also accentuated in this review.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554681","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Unveiling Anticancer Phytoconstituents: A Comprehensive Review of GC–MS Applications in Natural Products
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-04 DOI: 10.1002/slct.202405724
Akrit Verma, Manish Vyas, Sanjeev Kumar Sahu

Cancer remains a significant global health challenge characterized by the uncontrolled proliferation of malignant cells. While conventional treatments such as chemotherapy and radiotherapy are effective, they often cause severe side effects, driving interest in alternative therapies derived from medicinal plants. These plants are rich in bioactive compounds, including terpenoids, phenolics, and flavonoids, which exhibit promising anticancer properties. This review focuses on gas chromatography–mass spectrometry (GC–MS) for identifying and characterizing these phytochemicals, highlighting its value in natural product research due to its precise separation and identification capabilities. An analysis of over 30 studies identified key compounds with significant cytotoxic effects. Limonene (IC50: 47–57.34 µg/mL for A549, HepG2, CaCo, and PANC-1 cells), squalene (IC50: 26.22 µg/mL for JURKAT), sesamin (IC50: 52–57.2 µg/mL for MCF-7 and HCT116 cells), and β-caryophyllene (IC50: 19.4–58.2 µg/mL for ME-180 and MCF-7 cells) have exhibited potent anticancer activities. Despite its advantages, GC-MS realizes limitations, including difficulty in differentiating structural isomers and detecting low-abundance compounds. Integrating GC–MS with complementary analytical techniques can overcome these challenges and enhance phytochemical profiling. Addressing bioavailability challenges and conducting clinical trials is essential for translating these promising findings into effective cancer therapies. These findings underscore the therapeutic potential of phytochemicals as safer alternatives to conventional treatments.

{"title":"Unveiling Anticancer Phytoconstituents: A Comprehensive Review of GC–MS Applications in Natural Products","authors":"Akrit Verma,&nbsp;Manish Vyas,&nbsp;Sanjeev Kumar Sahu","doi":"10.1002/slct.202405724","DOIUrl":"https://doi.org/10.1002/slct.202405724","url":null,"abstract":"<p>Cancer remains a significant global health challenge characterized by the uncontrolled proliferation of malignant cells. While conventional treatments such as chemotherapy and radiotherapy are effective, they often cause severe side effects, driving interest in alternative therapies derived from medicinal plants. These plants are rich in bioactive compounds, including terpenoids, phenolics, and flavonoids, which exhibit promising anticancer properties. This review focuses on gas chromatography–mass spectrometry (GC–MS) for identifying and characterizing these phytochemicals, highlighting its value in natural product research due to its precise separation and identification capabilities. An analysis of over 30 studies identified key compounds with significant cytotoxic effects. Limonene (IC<sub>50</sub>: 47–57.34 µg/mL for A549, HepG2, CaCo, and PANC-1 cells), squalene (IC<sub>50</sub>: 26.22 µg/mL for JURKAT), sesamin (IC<sub>50</sub>: 52–57.2 µg/mL for MCF-7 and HCT116 cells), and <i>β</i>-caryophyllene (IC<sub>50</sub>: 19.4–58.2 µg/mL for ME-180 and MCF-7 cells) have exhibited potent anticancer activities. Despite its advantages, GC-MS realizes limitations, including difficulty in differentiating structural isomers and detecting low-abundance compounds. Integrating GC–MS with complementary analytical techniques can overcome these challenges and enhance phytochemical profiling. Addressing bioavailability challenges and conducting clinical trials is essential for translating these promising findings into effective cancer therapies. These findings underscore the therapeutic potential of phytochemicals as safer alternatives to conventional treatments.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143533325","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nitrogen, Oxygen, and Sulphur Heterocycles as Potent Anti-Inflammatory Agents: Insight Into the Synthetic Routes
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-04 DOI: 10.1002/slct.202403824
M. J. Nagesh Khadri, Uday Shashikumar, Pei-Chien Tsai, Prof. Kiran B. Manjappa, Prof. Vinoth Kumar Ponnusamy, Prof. Shaukath Ara Khanum

Nitrogen, oxygen, and sulfur-containing heterocyclic compounds are broadly established as key scaffolds with potential chemical and biological properties. Benzimidazole, indole, benzoxazole, benzothiazole, pyrazole, and thiophene analogs are significant heterocyclic motifs that bear almost all pharmacological activities. Anti-inflammatory activity is one of the most commonly associated biological activities with these heterocycles and thus has attracted the interest of researchers to synthesize and study them in-depth. The present review highlights mainly the various synthetic methodologies utilized to prepare these diverse heterocycles and their associated pharmacological properties limited to anti-inflammatory activities. Further, this review will provide a comprehensive idea of the methodologies used to prepare biologically active nitrogen, oxygen, and sulfur-bearing heterocycles and possibly invoke new thoughts in the search for rational designs for developing more promising anti-inflammatory agents.

{"title":"Nitrogen, Oxygen, and Sulphur Heterocycles as Potent Anti-Inflammatory Agents: Insight Into the Synthetic Routes","authors":"M. J. Nagesh Khadri,&nbsp;Uday Shashikumar,&nbsp;Pei-Chien Tsai,&nbsp;Prof. Kiran B. Manjappa,&nbsp;Prof. Vinoth Kumar Ponnusamy,&nbsp;Prof. Shaukath Ara Khanum","doi":"10.1002/slct.202403824","DOIUrl":"https://doi.org/10.1002/slct.202403824","url":null,"abstract":"<p>Nitrogen, oxygen, and sulfur-containing heterocyclic compounds are broadly established as key scaffolds with potential chemical and biological properties. Benzimidazole, indole, benzoxazole, benzothiazole, pyrazole, and thiophene analogs are significant heterocyclic motifs that bear almost all pharmacological activities. Anti-inflammatory activity is one of the most commonly associated biological activities with these heterocycles and thus has attracted the interest of researchers to synthesize and study them in-depth. The present review highlights mainly the various synthetic methodologies utilized to prepare these diverse heterocycles and their associated pharmacological properties limited to anti-inflammatory activities. Further, this review will provide a comprehensive idea of the methodologies used to prepare biologically active nitrogen, oxygen, and sulfur-bearing heterocycles and possibly invoke new thoughts in the search for rational designs for developing more promising anti-inflammatory agents.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Cyclopropane Containing Triterpenoids, Cycloartenone, and Cycloartenol: Isolation, Chemical Transformations, and Anticancer Studies
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-03 DOI: 10.1002/slct.202403698
Sayantan Paul, Kartik Mandal, Manas K. Santra, Asish K. Bhattacharya

Cycloartenone and cycloartenol, two plant-derived triterpenoids possessing cyclopropane ring were isolated from the latex of Artocarpus heterophyllus (jackfruit). Cycloartenol was chemically modified to synthesize dihydrocycloartenol via acetylation and deacetylation methodology followed by hydrogenation. Hydroxyl group present in the cycloartenol was also employed for the nitro benzoate formation. All the isolated and synthesized compounds were assayed against MCF7 breast cancer cell line for their anticancer properties.

环木菠萝烯酮和环木菠萝烯醇这两种植物源三萜类化合物具有环丙烷环,它们是从异叶菠萝蒿(千层塔)的乳汁中分离出来的。环木菠萝烯醇通过乙酰化和脱乙酰化方法进行化学修饰,然后加氢合成二氢环木菠萝烯醇。环木菠萝烯醇中的羟基也被用于形成硝基苯甲酸酯。所有分离和合成的化合物都针对 MCF7 乳腺癌细胞系进行了抗癌特性检测。
{"title":"Cyclopropane Containing Triterpenoids, Cycloartenone, and Cycloartenol: Isolation, Chemical Transformations, and Anticancer Studies","authors":"Sayantan Paul,&nbsp;Kartik Mandal,&nbsp;Manas K. Santra,&nbsp;Asish K. Bhattacharya","doi":"10.1002/slct.202403698","DOIUrl":"https://doi.org/10.1002/slct.202403698","url":null,"abstract":"<p>Cycloartenone and cycloartenol, two plant-derived triterpenoids possessing cyclopropane ring were isolated from the latex of <i>Artocarpus heterophyllus</i> (jackfruit). Cycloartenol was chemically modified to synthesize dihydrocycloartenol via acetylation and deacetylation methodology followed by hydrogenation. Hydroxyl group present in the cycloartenol was also employed for the nitro benzoate formation. All the isolated and synthesized compounds were assayed against MCF7 breast cancer cell line for their anticancer properties.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 9","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143530271","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Expanded Vermiculite-Based Calcium Chloride Hexahydrate Phase Change Materials: Preparation, Characterization, and Phase Change Kinetics
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-03 DOI: 10.1002/slct.202405355
Shaogang Zhang, Xiaolong Ma, Xin Min, Xiaoguang Zhang, Jinhong Li

Solid-liquid phase change materials (PCMs) made from calcium chloride hexahydrate (CaCl2·6H2O) offer benefits such as significant latent heat during phase change, high heat storage efficiency, low preparation costs, a nearly constant temperature exothermic process, and environmentally friendly attributes. However, they also face challenges like poor thermal conductivity, susceptibility to leakage, supercooling, and phase separation. The melt impregnation method prepared shape-stable composite PCMs using expanded vermiculite (EV) and CaCl2·6H2O as raw materials. The layered pore structure of EV can be used as an encapsulation matrix to prevent the leakage of the CaCl2·6H2O liquid phase. Adding 1 wt% strontium chloride hexahydrate (SrCl2·6H2O) nucleating agent and 3 wt% copper nanoparticle thermal conductivity enhancer can reduce the supercooling by 8 °C and increase the thermal conductivity by 0.2092 W/(m·K). The kinetic equation effectively describes the non-isothermal melt crystallization process. An increase in the cooling rate creates a thermal hysteresis effect on melt crystallization; the faster the cooling rate, the lower the temperature at which crystallization begins and the shorter the duration required for crystallization to complete. Both SrCl2·6H2O and copper nanoparticles can reduce the crystallization activation energy, which is the essential reason for lowering the supercooling of CaCl2·6H2O.

由六水氯化钙(CaCl2-6H2O)制成的固液相变材料(PCMs)具有相变过程中潜热大、储热效率高、制备成本低、放热过程几乎恒温以及环保等优点。然而,它们也面临着导热性差、易泄漏、过冷和相分离等挑战。熔体浸渍法以膨胀蛭石(EV)和 CaCl2-6H2O 为原料,制备了形状稳定的复合 PCM。EV 的层状孔隙结构可用作封装基质,防止 CaCl2-6H2O 液相泄漏。加入 1 wt% 的六水氯化锶(SrCl2-6H2O)成核剂和 3 wt% 的纳米铜导热增强剂,可使过冷度降低 8 ℃,导热率提高 0.2092 W/(m-K)。动力学方程有效地描述了非等温熔体结晶过程。冷却速率的增加会对熔体结晶产生热滞后效应;冷却速率越快,开始结晶的温度越低,结晶完成所需的时间越短。SrCl2-6H2O 和纳米铜粒子都能降低结晶活化能,这是降低 CaCl2-6H2O 过冷度的根本原因。
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引用次数: 0
Advancement of Environment Friendly Emerging Lead-Free Perovskite Solar Cell Materials and Its Devices 推进环境友好型新兴无铅过氧化物太阳能电池材料及其设备的发展
IF 1.9 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-03-03 DOI: 10.1002/slct.202405119
Ambapuram Meenakshamma, Adike Neeraja, Mitty Raghavender

In the advancement of photovoltaic (PV) technology, perovskite solar cells (PSCs) have proven potential in their evolution and have become vanguard research with an extraordinary power conversion efficiency (PCE) performance up to 26%, which stances a remarkable challenge to thin film and multi crystalline silicon (Si) photovoltaic technology. However, the toxicity of lead (Pb), stability issues etc., hampered the commercialization of perovskite solar cells. Scientists have made efforts for the development of different categories of lead-free perovskites, including tin halide perovskites, germanium-based perovskites, and heterovalent elements (Transition metal halide perovskite, double perovskites etc.). However, the performance of the corresponding devices is not up to the mark, and there are stability issues. The limitations mainly initiate from either the unstable lattice structure of these materials or their low dimensionality (e.g., structural and electronic dimensionality)-related to poor carrier transport and self-trapping effect, accelerating nonradiative recombination. This article reviews the environmentally friendly PSCs developed by the use of novel, low/nontoxic perovskite materials, with specific attention focused on assets of identical perovskites and pertinent production of high efficiency PV devices, notable achievement reports of all lead-free perovskites to date with PV performance, and stability of corresponding devices, photovoltaic applications and their commercialization.

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ChemistrySelect
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