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Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry最新文献

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2-Pyridone quinoline hybrids as potent antibacterial and antifungal agents 2-吡啶酮喹啉杂交种作为有效的抗菌和抗真菌剂
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-02-15 DOI: 10.56042/ijcb.v60i2.35076
N. Desai, J. P. Harsorab, H. Mehtaa
An efficient synthetic strategy for the synthesis of 6-amino-1-(((2-chloroquinolin-3-yl)methylene)amino)-2-oxo-4-(aryl)-1,2-dihydropyridine-3,5-dicarbonitriles is well described in this paper. Structures of synthesized compounds have been identified by standard spectroscopic techniques like 1 H NMR, 13 C NMR, IR and mass spectroscopy. Results of the biological activity reveals that electron withdrawing groups and presence of –OH group on meta position play a significant role for the increment in the antibacterial and antifungal activities respectively of 3a-j . In the present study, it has been observed that compounds 3i and 3e are the most active antimicrobials.
本文介绍了一种合成6-氨基-1-((2-氯喹啉-3-基)亚甲基)氨基-2-氧-4-(芳基)-1,2-二氢吡啶-3,5-二碳腈的高效合成策略。合成化合物的结构已通过标准的光谱技术,如1h NMR, 13c NMR, IR和质谱进行了鉴定。生物活性结果表明,吸电子基团和-OH基团的存在分别对3a-j的抗菌活性和抗真菌活性的提高起着重要作用。在本研究中,已经观察到化合物3i和3e是最有效的抗菌素。
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引用次数: 5
Computational calculations and molecular docking studies on 2-(2-ethylaminothiazol-5-oyl)benzothiazole 2-(2-乙基氨基噻唑-5-酰基)苯并噻唑的计算计算及分子对接研究
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-02-15 DOI: 10.56042/ijcb.v60i2.30557
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引用次数: 1
Prediction of agonist, partial agonist and full antagonist of H. pylori TlpB utilizing molecular docking 利用分子对接预测幽门螺杆菌TlpB激动剂、部分激动剂和完全拮抗剂
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-21 DOI: 10.56042/ijcb.v59i05.45463
{"title":"Prediction of agonist, partial agonist and full antagonist of H. pylori TlpB utilizing molecular docking","authors":"","doi":"10.56042/ijcb.v59i05.45463","DOIUrl":"https://doi.org/10.56042/ijcb.v59i05.45463","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72451496","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
A one pot, efficient and eco-friendly synthesis of 1,3,4-thiadiazolo[3,2-a] pyrimidine scaffold via Aza–Michael addition and intramolecular cyclo-elimination reactions in poly ethylene glycol (PEG) 聚乙二醇(PEG)中Aza-Michael加成和分子内环消除反应一锅高效环保合成1,3,4-噻二唑[3,2- A]嘧啶支架
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-21 DOI: 10.56042/ijcb.v59i05.45479
Akeel Ahmada, Shailendra Tiwari
Potassium carbonate in poly (ethylene glycol-400) has been found to be a highly effective and efficient medium for the straight forward, convenient, one pot and green synthesis of ethyl 2-substituted phenyl-7-oxo-7 H -[1,3,4]- thiadiazolo [3,2-a]- pyrimidine-6-corboxylate and -6-corbonitrile through intramolecular cyclo-elimination of Michael adducts formed between the reaction of 2-amino-5 substituted thiadiazoles with diethyl-2- (ethoxymethylene) malonate and ethyl-2- cyano-3-ethoxyacrylate respectively. The structures of all the new compounds have been elucidated using IR, 1 H and 13 C NMR, mass spectral data and elemental analyses.
聚乙烯醇-400中的碳酸钾是一种高效、直接、方便、通过分子内环消除2-氨基-5取代噻二唑与二乙基-2-(乙氧基亚甲基)丙二酸二乙酯和乙基-2-氰基-3-乙氧基丙烯酸酯反应形成的Michael加合物,一锅绿色合成了2-取代苯基-7-氧基-7 H -[1,3,4]-噻二唑[3,2-a]-嘧啶-6-羧酸酯和-6-腈。所有新化合物的结构已通过IR、1h和13c NMR、质谱数据和元素分析进行了鉴定。
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引用次数: 3
Synthesis, anti-tuberculosis and anti-bacterial activities of sulfonamide bearing 4-((2-(5-bromo-1H-pyrazolo[3,4-b]pyridin-1-yl)-2-oxoethyl)amino)-N-(various substitutions)benzenesulfonamide 含4-((2-(5-溴- 1h -吡唑[3,4-b]吡啶-1-基)-2-氧乙基)氨基)- n-(各种取代)苯磺酰胺的合成、抗结核及抗菌活性
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-21 DOI: 10.56042/ijcb.v59i05.45469
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引用次数: 1
Free radical scavenging and α-glucosidase inhibitory activity of (E)-methyl/ethyl-3-(2-hydroxyphenyl)acrylates (E)-甲基/乙基-3-(2-羟基苯基)丙烯酸酯的自由基清除和α-葡萄糖苷酶抑制活性
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-20 DOI: 10.56042/ijcb.v60i01.40509
{"title":"Free radical scavenging and α-glucosidase inhibitory activity of (E)-methyl/ethyl-3-(2-hydroxyphenyl)acrylates","authors":"","doi":"10.56042/ijcb.v60i01.40509","DOIUrl":"https://doi.org/10.56042/ijcb.v60i01.40509","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72517011","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
A convenient synthesis and biological activities of N-(pyridin-3-ylmethylene) benzohydrazides by the condensation of nicotinaldehydes with benzohydrazides 研究了烟醛与苯并肼缩合制备N-(吡啶-3-基亚甲基)苯并肼的简便方法及其生物活性
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-20 DOI: 10.56042/ijcb.v60i01.40586
D. Anusha, G. Praveena, A. Zehra, A. Tiwari, R. Prakasham, B. Raju
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引用次数: 0
Three-component coupling approach for the synthesis of 4H-pyrans and pyran-annulated heterocyclic scaffolds utilizing Ag/TiO2 nano-thin films as robust recoverable catalyst 以Ag/TiO2纳米薄膜为催化剂制备4h -吡喃及吡喃环杂环支架的三组分偶联方法
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-20 DOI: 10.56042/ijcb.v60i01.29388
Fatemeh Noori Sadeha, M. Lashkari, Nourallah Hazeria, Maryam Fatahpoura, Malek Taher Maghsoodloua, Mohammad Saeed Hadavic, Sahar Mahnaeic
As a segment of ongoing surveys and with the aim of expansion of environmentally benign processes, a series of biologically varied type of substituted 2-amino-3-cyano-4 H -pyrans and pyran-annulated Scaffolds have been synthesized by tandem Knoevenagel-cyclocondensation of aldehydes, malononitrile, and C-H-activated acidic compounds in aqueous ethanol in the presence of Ag/TiO 2 nano-thin films as an eco-friendly, recyclable, and, robust catalyst at 60°C. The salient features of this protocol are mild reaction conditions, producing target compounds in high yields, short reaction times, high atom economy, eco-friendly catalyst, easy isolation of products and no column chromatographic separation. Also, it is observed that the catalyst is highly stable during the reaction and several reuse times without observable loss in catalytic performance.
作为正在进行的研究的一部分,并以扩大环境友好的工艺为目的,在60°C的环境下,在Ag/ tio2纳米薄膜的存在下,通过醛、丙二腈和C-H活化的酸性化合物的串联knoevenagel -环缩合,在水乙醇中合成了一系列具有生物多样性的取代2-氨基-3-氰基-4 -H-吡喃和吡喃环支架,作为环保、可回收和强大的催化剂。该工艺具有反应条件温和、产率高、反应时间短、原子经济性高、催化剂环保、产物易于分离、无需柱层析分离等特点。此外,观察到催化剂在反应和多次重复使用中高度稳定,没有明显的催化性能损失。
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引用次数: 0
Exploration of anticancer potential of hydroxamate derivatives as selective HDAC8 inhibitors using integrated structure and ligand based molecular modeling approach 利用集成结构和配体分子模型方法探索羟酸酯衍生物作为选择性HDAC8抑制剂的抗癌潜力
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-20 DOI: 10.56042/ijcb.v60i01.31340
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引用次数: 0
Synthesis, characterization and potent antimicrobial and antifungal activity of 2-substituted benzimidazole derivatives 2-取代苯并咪唑衍生物的合成、表征及有效的抗菌和抗真菌活性
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-20 DOI: 10.56042/ijcb.v60i01.31988
R. Verma, Chitra Guptab, Ali Mohd Ganieb, S. Singha, P. K. Singhc
Benzimidazole is the heterocyclic compound formed by the fusion of benzene and imidazole ring. Benzimidazole analogs are of great significance because of their clinical application and biological activity. Benzimidazoles are considered as an optimistic class of bioactive heterocyclic compound that possesses a range of biological activities. We have synthesized five substituted Benzimidazole derivative using on both microwave irradiation and conventional heating method. The newly synthesized compounds are characterized by IR, NMR and Mass spectra analysis. In the present study, we have reported the synthesis, spectral studies and biological evaluation of some benzimidazole derivatives. Benzimidazole play important role in medical field with so many pharmacological activities such as antimicrobial, anti bacterial, etc. The potency of this clinically useful drug in treatment in microbial action and other activities has encouraged the development of some more potent and significant compounds.
苯并咪唑是由苯和咪唑环融合而成的杂环化合物。苯并咪唑类似物的临床应用和生物活性具有重要意义。苯并咪唑被认为是一类具有广泛生物活性的杂环化合物。采用微波辐照法和常规加热法合成了5个取代苯并咪唑衍生物。新合成的化合物通过IR、NMR和质谱分析进行了表征。本文报道了一些苯并咪唑衍生物的合成、光谱研究和生物学评价。苯并咪唑具有抗菌、抗菌等多种药理作用,在医学领域占有重要地位。这种临床上有用的药物在治疗微生物作用和其他活动方面的效力鼓励了一些更有效和更重要的化合物的开发。
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引用次数: 0
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Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry
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