Pub Date : 2024-03-13DOI: 10.11648/j.ajhc.20241001.11
Omkar S. Kamble, Rana Chatterjee, Shubhada Gad, Samarath Kansara, Sonal Ayakar, Amit Kumar Pandey, R. Dandela
N, N'-alkylidene bisamides show promise in biological and pharmaceutical uses. Advanced chemistry now explores cleaner and more environmentally friendly methods. One such method involves using concentrated solar radiation (CSR) to facilitate the green synthesis of N, N'-alkylidene bisamides. This approach simplifies the process by combining aldehydes and amides in a one-pot reaction. Its solvent-free nature sets it apart, aligning with environmentally friendly practices. Any regular catalyst aids the response, making it efficient. The simplicity continues with an easy filtration step to isolate the products. Notably, there's no need for column chromatography, making the purification process straightforward. In general, a mixture of aldehyde, aryl/alkylamide was taken in a round bottom flask. The reaction mass in RBF was then kept under the concentrated solar radiation (CSR) setup with continuous stirring on a magnetic stirrer. After few hours of stirring the precipitate was observed. After completion of the reaction, the precipitated product was washed with water and recrystallized from hot ethanol to afford pure product symmetrical N, N'-alkylidene bisamide. Dimethyl sulfoxide (DMSO) was used as a solvent to prepare a stock of derivatives. Luria Bertani broth (LB) used for the present study viz; Staphylococ-cus aureus MCC 2408, Escherichia coli MCC 2412, Pseudomonas aeruginosa MCC 2080 and Klebsiella pneumoniae MCC 2451 used to evaluate the antibacterial property of the derivatives. Indeed, this method offers an eco-friendly solution and showcases the potential of using renewable energy sources in chemical synthesis. It is a significant step towards sustainable practices in chemistry, particularly in producing complex organic compounds for biological and pharmaceutical purposes.
{"title":"Solar-Assisted Green Synthesis, Molecular Docking, Antibacterial, and Cytotoxicity Studies of Symmetrical N, N’-Alkylidene Bisamides Bearing Lower E-Factors","authors":"Omkar S. Kamble, Rana Chatterjee, Shubhada Gad, Samarath Kansara, Sonal Ayakar, Amit Kumar Pandey, R. Dandela","doi":"10.11648/j.ajhc.20241001.11","DOIUrl":"https://doi.org/10.11648/j.ajhc.20241001.11","url":null,"abstract":"N, N'-alkylidene bisamides show promise in biological and pharmaceutical uses. Advanced chemistry now explores cleaner and more environmentally friendly methods. One such method involves using concentrated solar radiation (CSR) to facilitate the green synthesis of N, N'-alkylidene bisamides. This approach simplifies the process by combining aldehydes and amides in a one-pot reaction. Its solvent-free nature sets it apart, aligning with environmentally friendly practices. Any regular catalyst aids the response, making it efficient. The simplicity continues with an easy filtration step to isolate the products. Notably, there's no need for column chromatography, making the purification process straightforward. In general, a mixture of aldehyde, aryl/alkylamide was taken in a round bottom flask. The reaction mass in RBF was then kept under the concentrated solar radiation (CSR) setup with continuous stirring on a magnetic stirrer. After few hours of stirring the precipitate was observed. After completion of the reaction, the precipitated product was washed with water and recrystallized from hot ethanol to afford pure product symmetrical N, N'-alkylidene bisamide. Dimethyl sulfoxide (DMSO) was used as a solvent to prepare a stock of derivatives. Luria Bertani broth (LB) used for the present study viz; Staphylococ-cus aureus MCC 2408, Escherichia coli MCC 2412, Pseudomonas aeruginosa MCC 2080 and Klebsiella pneumoniae MCC 2451 used to evaluate the antibacterial property of the derivatives. Indeed, this method offers an eco-friendly solution and showcases the potential of using renewable energy sources in chemical synthesis. It is a significant step towards sustainable practices in chemistry, particularly in producing complex organic compounds for biological and pharmaceutical purposes. \u0000","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"267 2‐3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140247324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-04-20DOI: 10.11648/j.ajhc.20230901.12
Robert Michael Moriarty, C. Mitan, Baohua Gu, T. Block
: N -Alkyl-C 1 -dialkyl chains iminocyclitols with D or L-ribitol stereochemistry are synthesized with high diastereoselectivity after Grignard reagents addition to N -quaternary pyrrolines salts, and tested for antiviral activity in bovine viral diarrhea virus (BVDV), surrogate for hepatitis C virus (HCV). Dihedral angles are calculated from carbon chemical shift (δ Cn [ppm]) with 3-sphere method without building units. 3-Sphere, a hypersphere in 4D, under Hopf fibration and Lie algebra mathematics theories enable calculation of the dihedral angles from the NMR data (vicinal coupling constant 3 J HnHn+1 [Hz], chemical shift δ Cn [ppm]). Instead of 3D manifold equations on seven sets unit or six sets units are proposed equations between 4D – 2D, in function of the curvature. The relationship between the antiviral activity and the iminocyclitol structure reveals that monoalkyl chain, N -n-C 1 -dodecyl β-L-ribitol trifloroacetate salt 30 (IC 50 1.5 uM) has higher antiviral activity in tangential space, relative to three alkyl chain, N -Methyl-C 1 -butil, nonyl-L-ribitol. HCl 26 (IC 50 < 2 uM) with torus and Dupin cyclide coordinate, both with coordinates in 2D. Three alkyl chain isopropylidene protected pyrrolidine 25 has in 4D with all equations for calculation of the dihedral angles, and in protected pyrroline 19b double bond moves the coordinates in 2D.
{"title":"Hypersphere and Antiviral Activity of Three Alkyl Chain Iminocyclitols with D and L Ribitol Stereochemistry","authors":"Robert Michael Moriarty, C. Mitan, Baohua Gu, T. Block","doi":"10.11648/j.ajhc.20230901.12","DOIUrl":"https://doi.org/10.11648/j.ajhc.20230901.12","url":null,"abstract":": N -Alkyl-C 1 -dialkyl chains iminocyclitols with D or L-ribitol stereochemistry are synthesized with high diastereoselectivity after Grignard reagents addition to N -quaternary pyrrolines salts, and tested for antiviral activity in bovine viral diarrhea virus (BVDV), surrogate for hepatitis C virus (HCV). Dihedral angles are calculated from carbon chemical shift (δ Cn [ppm]) with 3-sphere method without building units. 3-Sphere, a hypersphere in 4D, under Hopf fibration and Lie algebra mathematics theories enable calculation of the dihedral angles from the NMR data (vicinal coupling constant 3 J HnHn+1 [Hz], chemical shift δ Cn [ppm]). Instead of 3D manifold equations on seven sets unit or six sets units are proposed equations between 4D – 2D, in function of the curvature. The relationship between the antiviral activity and the iminocyclitol structure reveals that monoalkyl chain, N -n-C 1 -dodecyl β-L-ribitol trifloroacetate salt 30 (IC 50 1.5 uM) has higher antiviral activity in tangential space, relative to three alkyl chain, N -Methyl-C 1 -butil, nonyl-L-ribitol. HCl 26 (IC 50 < 2 uM) with torus and Dupin cyclide coordinate, both with coordinates in 2D. Three alkyl chain isopropylidene protected pyrrolidine 25 has in 4D with all equations for calculation of the dihedral angles, and in protected pyrroline 19b double bond moves the coordinates in 2D.","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"62 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84048742","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-04-20DOI: 10.11648/j.ajhc.20230901.11
Mahboobeh Falahati, M. Soleimani, F. Aflatouni
{"title":"Separation and Preconcentration of Anionic Dyes Using Magnetic Nanoparticles with Modify Polymer Ionic Liquid","authors":"Mahboobeh Falahati, M. Soleimani, F. Aflatouni","doi":"10.11648/j.ajhc.20230901.11","DOIUrl":"https://doi.org/10.11648/j.ajhc.20230901.11","url":null,"abstract":"","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87625252","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-04-26DOI: 10.11648/J.AJHC.20210701.12
Jhuma Samanta, S. Bhattacharya, A. Rana
Thevetia peruviana (Pers.) K. Schum (Apocynacae) leaves have a reputation of abortifacient activity. We investigated traditional claim and found that methanolic leaf extract produce antifertility activity by lowering the progesterone level in rat model. Aim of the present study was to find out the chemical constituent (s) responsible for antifertility activity of methanolic leaf extract of Thevetia peruviana (Pers.). The ethyl acetate, chloroform and toluene fractions of methanolic extract of T. peruviana leaves freed from cardiac glycosides [TPL-Me-G] were selected for phytochemical investigation and in-vitro uterotonic activity. The methanolic extract of T. peruviana leaves (1.103g) was fractionated with toluene (100ml, n=20); chloroform (100ml, n=20); and ethyl acetate (100ml, n=20) in the successive order. These fractions were examined for phytoconstituents and evaluated for in-vitro uterotonic activity. The toluene fraction (TPL-T) was found to have triterpenes, flavonoids and phytosterols. Quercetin (0.8904%) is present in TPL-T. The chloroform fraction (TPL-Ch) was found to contain flavonoids, triterpenes and phytosterols. Presence of alkaloids and flavonoids (quercetin 0.1606%) were observed in ethyl acetate fraction (TPL-Et-Ac). In contrast to TPL-Et-Ac, the TPL-T and TPL-Ch induced dose dependent uterine contraction in the isolated estrogenized rat uterus model. Highest uterotonic activity was found with TPL-Me-G which has kaempferol as phyto-constituent additionally. The in-vitro uterotonic activity is not influenced by quercetin and primary contributor is kaempferol though some unknown phytoconstituent/s also contributes to uterotonic activity and synergizes the action of kaempferol too. So, further research is needed to identify other contributory unknown phytoconstituent/s for antifertility activity of methanolic leaf extract of Thevetia peruviana (Pers.).
{"title":"Evaluation of Ethyl Acetate, Chloroform and Toluene Fractions of Thevetia peruviana (Pers.) K. Schum Methanolic Leaf Extract for Uterotonic Activity","authors":"Jhuma Samanta, S. Bhattacharya, A. Rana","doi":"10.11648/J.AJHC.20210701.12","DOIUrl":"https://doi.org/10.11648/J.AJHC.20210701.12","url":null,"abstract":"Thevetia peruviana (Pers.) K. Schum (Apocynacae) leaves have a reputation of abortifacient activity. We investigated traditional claim and found that methanolic leaf extract produce antifertility activity by lowering the progesterone level in rat model. Aim of the present study was to find out the chemical constituent (s) responsible for antifertility activity of methanolic leaf extract of Thevetia peruviana (Pers.). The ethyl acetate, chloroform and toluene fractions of methanolic extract of T. peruviana leaves freed from cardiac glycosides [TPL-Me-G] were selected for phytochemical investigation and in-vitro uterotonic activity. The methanolic extract of T. peruviana leaves (1.103g) was fractionated with toluene (100ml, n=20); chloroform (100ml, n=20); and ethyl acetate (100ml, n=20) in the successive order. These fractions were examined for phytoconstituents and evaluated for in-vitro uterotonic activity. The toluene fraction (TPL-T) was found to have triterpenes, flavonoids and phytosterols. Quercetin (0.8904%) is present in TPL-T. The chloroform fraction (TPL-Ch) was found to contain flavonoids, triterpenes and phytosterols. Presence of alkaloids and flavonoids (quercetin 0.1606%) were observed in ethyl acetate fraction (TPL-Et-Ac). In contrast to TPL-Et-Ac, the TPL-T and TPL-Ch induced dose dependent uterine contraction in the isolated estrogenized rat uterus model. Highest uterotonic activity was found with TPL-Me-G which has kaempferol as phyto-constituent additionally. The in-vitro uterotonic activity is not influenced by quercetin and primary contributor is kaempferol though some unknown phytoconstituent/s also contributes to uterotonic activity and synergizes the action of kaempferol too. So, further research is needed to identify other contributory unknown phytoconstituent/s for antifertility activity of methanolic leaf extract of Thevetia peruviana (Pers.).","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85748131","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.11648/j.ajhc.20210702.12
Sayed Abd El-moneim Ahmed Altaweel, Ahmed Abdelhameed Khames, Abu-Bakr Abdelhady Mohamed El-Adasy, Abdallah Mahmoud Ahmed Hassane, Abdel-Haleem Mostafa Hussein
{"title":"3-Oxobutanamides in Heterocyclic Synthesis: Synthesis, Antimicrobial and Antioxidant Activity of Pyridine, Thiophene, Diazepine and Thiazole Derivatives","authors":"Sayed Abd El-moneim Ahmed Altaweel, Ahmed Abdelhameed Khames, Abu-Bakr Abdelhady Mohamed El-Adasy, Abdallah Mahmoud Ahmed Hassane, Abdel-Haleem Mostafa Hussein","doi":"10.11648/j.ajhc.20210702.12","DOIUrl":"https://doi.org/10.11648/j.ajhc.20210702.12","url":null,"abstract":"","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89617414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.11648/j.ajhc.20210702.11
Kingsley John Orie, Remy Ukachukwu Duru, Raphael I-oro Ngochindo
{"title":"Syntheses, Complexation and Biological Activity of Aminopyridines: A Mini-Review","authors":"Kingsley John Orie, Remy Ukachukwu Duru, Raphael I-oro Ngochindo","doi":"10.11648/j.ajhc.20210702.11","DOIUrl":"https://doi.org/10.11648/j.ajhc.20210702.11","url":null,"abstract":"","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"24 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80724824","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-01DOI: 10.11648/j.ajhc.20210702.13
Youssoufou Bakouan, B. Sessouma, Têeda Hamidou Ganamé, Lassané Tarpaga, Jules Yoda, K. Bayo
{"title":"Some Aspects of the Reactivity of 3-acyl-4-hydroxycoumarins","authors":"Youssoufou Bakouan, B. Sessouma, Têeda Hamidou Ganamé, Lassané Tarpaga, Jules Yoda, K. Bayo","doi":"10.11648/j.ajhc.20210702.13","DOIUrl":"https://doi.org/10.11648/j.ajhc.20210702.13","url":null,"abstract":"","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88966286","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-18DOI: 10.11648/j.ajhc.20200601.12
Jules Yoda
Coumarins or benzo-2-pyrone derivatives are one of the most significant families of natural compounds and are also important in synthetic organic chemistry. They have been widely used as starting materials or precursor molecules in the pharmaceutical, perfumery and agrochemical industries, etc. Hydroxycoumarins are an important class of coumarin compounds that possess several physical, chemical and biological properties. Among the hydroxycoumarins, 3-hydroxycoumarin seems to be the most important because of its numerous chemical, photochemical and biological properties. However, this compound remains less well known compared to others of the same class such as 7-hydroxycoumarin and 4-hydroxycoumarin. This study is therefore devoted to 3-hydroxycoumarin and its applications. The main purpose of this review is to summarize and document the recent advances on 3-hydroxycoumarin, concerning the main routes of its synthesis, its reactivity, its applications in different fields of biology. Several methods for the synthesis of 3-hydroxycoumarin have been described in the literature, most of which use salicylic aldehyde and 1-(2-hydroxyphenyl)ethanone as starting compounds. Other synthesis pathways exist, but they are based on intermediate synthesis compounds. Concerning the reactivity of 3-hydroxycoumarin, many heterocyclic compounds obtained from 3-hydroxycoumarin have been reported in the literature. Among these heterocycles are pyrido[2,3-c]coumarin derivatives, chromeno[4,3-e][1,3]oxazine derivatives, dihydropyrano[2,3-c] chromenes and 3-coumarinyl carboxylates. Various researches have also concerned the biological properties of this compound. It appears from these numerous studies that 3-hdroxycoumarin is used in fields such as genetics, pharmacology, microbiology, etc.
{"title":"Overview of Recent Advances in 3-Hydroxycoumarin Chemistry as a Bioactive Heterocyclic Compound","authors":"Jules Yoda","doi":"10.11648/j.ajhc.20200601.12","DOIUrl":"https://doi.org/10.11648/j.ajhc.20200601.12","url":null,"abstract":"Coumarins or benzo-2-pyrone derivatives are one of the most significant families of natural compounds and are also important in synthetic organic chemistry. They have been widely used as starting materials or precursor molecules in the pharmaceutical, perfumery and agrochemical industries, etc. Hydroxycoumarins are an important class of coumarin compounds that possess several physical, chemical and biological properties. Among the hydroxycoumarins, 3-hydroxycoumarin seems to be the most important because of its numerous chemical, photochemical and biological properties. However, this compound remains less well known compared to others of the same class such as 7-hydroxycoumarin and 4-hydroxycoumarin. This study is therefore devoted to 3-hydroxycoumarin and its applications. The main purpose of this review is to summarize and document the recent advances on 3-hydroxycoumarin, concerning the main routes of its synthesis, its reactivity, its applications in different fields of biology. Several methods for the synthesis of 3-hydroxycoumarin have been described in the literature, most of which use salicylic aldehyde and 1-(2-hydroxyphenyl)ethanone as starting compounds. Other synthesis pathways exist, but they are based on intermediate synthesis compounds. Concerning the reactivity of 3-hydroxycoumarin, many heterocyclic compounds obtained from 3-hydroxycoumarin have been reported in the literature. Among these heterocycles are pyrido[2,3-c]coumarin derivatives, chromeno[4,3-e][1,3]oxazine derivatives, dihydropyrano[2,3-c] chromenes and 3-coumarinyl carboxylates. Various researches have also concerned the biological properties of this compound. It appears from these numerous studies that 3-hdroxycoumarin is used in fields such as genetics, pharmacology, microbiology, etc.","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75330609","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-03-11DOI: 10.11648/J.AJHC.20190504.12
Dame Seye, M. Diop, Assane Touré, Tidiane Diop, C. Diop, M. Sidibe, A. Sarr, L. Diop,
Five new compounds are isolated from reactions carried out in solution. All the compounds are characterized by, Infrared and Mossbauer spectroscopies. Spectroscopic studies have shown the presence of different carracterristic bands, notably υ (PO) vibrations coming from triphenylphosphine oxide, with wide absorption due to the NH2 groups coming from urea and the intense doublet which show the presence of phenyl groups. The proposed structures, in the solid state, are discrete though hydrogen bonding interactions may occur. Event in this study is the dearylation evidenced, cleaved Sn-Ph bonds occurring in the presence of triphenylphosphine oxide or urea, during some reaction processes. In the presence of triphenylphosphine oxide, the dearylation is followed by the formation of Sn-Cl new bonds while in the presence of urea, the Sn-Ph bonds cleavage undergo with a deamination of the urea giving rise to the formation of Sn-N and Sn-Cl new bonds whose presence are ascertained by the Mossbauer parameters. The oxidation of tin (II) to tin (IV) as well as the coordination behavior of the oxonium, H3O+ cation is also noted in this work. In the reaction of triphenylphosphine oxide with SnCl2. 2H2O and nitric acid, we have obtained compounds in which tin has oxidized. The reactions between urea and SnPh3Cl are the site of a species exchange which can be explained by a deamination of urea and a dephenylation of SnPh3Cl Studies aimed at understanding the processes of this transformation still unknown leading to the isolation of aminochlorotin (IV) compounds and isolating their single crystals are being carried in our laboratory (LA.CHI.MI.A).
{"title":"Synthesis, Infrared and Mössbauer Characterization of Some Chloridestannate (IV) Inorganic-organic Hybrid Complexes: Sn-Ph Bonds Cleavage","authors":"Dame Seye, M. Diop, Assane Touré, Tidiane Diop, C. Diop, M. Sidibe, A. Sarr, L. Diop,","doi":"10.11648/J.AJHC.20190504.12","DOIUrl":"https://doi.org/10.11648/J.AJHC.20190504.12","url":null,"abstract":"Five new compounds are isolated from reactions carried out in solution. All the compounds are characterized by, Infrared and Mossbauer spectroscopies. Spectroscopic studies have shown the presence of different carracterristic bands, notably υ (PO) vibrations coming from triphenylphosphine oxide, with wide absorption due to the NH2 groups coming from urea and the intense doublet which show the presence of phenyl groups. The proposed structures, in the solid state, are discrete though hydrogen bonding interactions may occur. Event in this study is the dearylation evidenced, cleaved Sn-Ph bonds occurring in the presence of triphenylphosphine oxide or urea, during some reaction processes. In the presence of triphenylphosphine oxide, the dearylation is followed by the formation of Sn-Cl new bonds while in the presence of urea, the Sn-Ph bonds cleavage undergo with a deamination of the urea giving rise to the formation of Sn-N and Sn-Cl new bonds whose presence are ascertained by the Mossbauer parameters. The oxidation of tin (II) to tin (IV) as well as the coordination behavior of the oxonium, H3O+ cation is also noted in this work. In the reaction of triphenylphosphine oxide with SnCl2. 2H2O and nitric acid, we have obtained compounds in which tin has oxidized. The reactions between urea and SnPh3Cl are the site of a species exchange which can be explained by a deamination of urea and a dephenylation of SnPh3Cl Studies aimed at understanding the processes of this transformation still unknown leading to the isolation of aminochlorotin (IV) compounds and isolating their single crystals are being carried in our laboratory (LA.CHI.MI.A).","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81388927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-11DOI: 10.11648/J.AJHC.20190504.11
D. Bakhotmah
Synthesis of several new diphenyl-1',2',4'-triazin-3'-yl barbituric acid are described. The method involves addition reaction of isocyanate and isothiocyanate and 3-amino-5,6-diphenyl-1,2,4-triazine (1) to give N1,N3-disubstituted urea 2 and N1,N3-disubstituted thioureas 3 and 4 respectively. Further, ring closure reactions with malonate ester give barbituric acid 5 and thiobarbituric acid 6 and 7. The Presence of the active methylene in the skeleton of compound 5-7 at C-5 are deduced by condensation with pyridine-4-carboxyladehyde to give barbituric and thiobarbituric acids (8-10). Further fluoroacylation of compounds 5-7, afforded 1-(cyclohexyl/methyl/phenyl)-3-(5',6'-diphenyl-1',2',4'-triazin-3'-yl)-5-(trifluoracetyl)-5H-barbituric/thiobarbituric acids (11-13). Synthesis compounds of the series 5-(trifluoroacetyl) barbituric acid (11) and 5-(trifluoroacetyl) thiobarbituric acids (12 and 13) were able to inhibit activity of CDK2 in a biochemical assay with IC50 values comparable to olomoucine. In addition, a pyridine side chain at C-5 (compound 9 and 10) significantly decreases CDK2 inhibitory activity.
{"title":"Synthesis of Barbituric and Thiobarbituric Acids Bearing 5,6-Diphenyl-1,2,4-Triazin-3-yl Moiety as CDK2 Inhibitors of Tumor Cells","authors":"D. Bakhotmah","doi":"10.11648/J.AJHC.20190504.11","DOIUrl":"https://doi.org/10.11648/J.AJHC.20190504.11","url":null,"abstract":"Synthesis of several new diphenyl-1',2',4'-triazin-3'-yl barbituric acid are described. The method involves addition reaction of isocyanate and isothiocyanate and 3-amino-5,6-diphenyl-1,2,4-triazine (1) to give N1,N3-disubstituted urea 2 and N1,N3-disubstituted thioureas 3 and 4 respectively. Further, ring closure reactions with malonate ester give barbituric acid 5 and thiobarbituric acid 6 and 7. The Presence of the active methylene in the skeleton of compound 5-7 at C-5 are deduced by condensation with pyridine-4-carboxyladehyde to give barbituric and thiobarbituric acids (8-10). Further fluoroacylation of compounds 5-7, afforded 1-(cyclohexyl/methyl/phenyl)-3-(5',6'-diphenyl-1',2',4'-triazin-3'-yl)-5-(trifluoracetyl)-5H-barbituric/thiobarbituric acids (11-13). Synthesis compounds of the series 5-(trifluoroacetyl) barbituric acid (11) and 5-(trifluoroacetyl) thiobarbituric acids (12 and 13) were able to inhibit activity of CDK2 in a biochemical assay with IC50 values comparable to olomoucine. In addition, a pyridine side chain at C-5 (compound 9 and 10) significantly decreases CDK2 inhibitory activity.","PeriodicalId":7715,"journal":{"name":"American Journal of Heterocyclic Chemistry","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88194462","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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