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

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Synthesis, DFT calculations, NBO analysis and docking studies of 3-(2-arylamino-4-aminothiazol-5-oyl)pyridine derivatives 3-(2-芳基氨基-4-氨基噻唑-5-酰基)吡啶衍生物的合成、DFT计算、NBO分析及对接研究
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-05 DOI: 10.56042/ijcb.v60i7.29123
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引用次数: 0
Modulation of morphology and efficacy of new CB1 receptor antagonist using simple and benign polymeric additives 新型CB1受体拮抗剂的形态和疗效的简单和良性聚合物添加剂调节
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-05 DOI: 10.56042/ijcb.v60i7.29319
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引用次数: 0
Montmorillonite K-10 supported palladium nanoparticles: A catalyst for the preparation of α-aminoynones employing copper free acyl Sonogashira reaction 蒙脱土K-10负载钯纳米颗粒:用无铜酰基Sonogashira反应制备α-氨基酮的催化剂
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-05 DOI: 10.56042/ijcb.v60i7.37777
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引用次数: 0
Synthesis of isomeric Naphtho furanyl Coumarins as Anti-inflammatory and Analgesic Agents 抗炎镇痛异构体萘呋喃基香豆素的合成
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-05 DOI: 10.56042/ijcb.v60i7.29262
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引用次数: 0
Design and synthesis of new quinoline hybrid derivatives and their antimicrobial, antimalarial and antitubercular activities 新型喹啉杂化衍生物的设计与合成及其抗菌、抗疟、抗结核活性
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-05 DOI: 10.56042/ijcb.v60i7.28981
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引用次数: 1
Synthesis, molecular docking and biological evaluation of new quinoline analogues as potent anti-breast cancer and antibacterial agents 新型喹啉类抗乳腺癌抗菌剂的合成、分子对接及生物学评价
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-01 DOI: 10.22034/IJPS.2020.120884.1637
S. V. Rathod, Kailas W. Shinde, P. Kharkar, C. Shah
A series of new class of quinoline analogues were synthesized from isatin through two steps in good yields. All compounds were further evaluated for their anticancer activity against triple-negative breast cancer cell line (MDA-MB-231) using MTT assay and antibacterial activity against Gram-positive bacteria (Staphylococcus aureus 6538p and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) using agar well diffusion method. All synthesized compounds were confirmed by spectral characterization viz FT-IR, MS, 1H-NMR and 13C-NMR. Results indicated that in vitro anticancer evaluation, IC50 values of all target compounds were found to be in the range of 11.50-37.99 µM and compound 4h showed better promising anti-breast cancer activity among all synthesized derivatives. In vitro antibacterial evaluation, compounds 4d, 4f, 4h and 4j exhibited moderate antibacterial activity against all tested organisms. Molecular docking analysis demonstrated good interaction of compound 4h with the active site residue of Human Carbonic Anhydrase I, Protein Kinase A and Kinesin Spindle Protein (KSP).
以鸢尾素为原料,经过两步合成了一系列新的喹啉类似物,收率较高。采用MTT法检测化合物对乳腺癌三阴性细胞株MDA-MB-231的抑癌活性,采用琼脂孔扩散法检测化合物对革兰氏阳性菌(金黄色葡萄球菌6538p和枯草芽孢杆菌)和革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)的抑菌活性。所有合成的化合物均通过FT-IR, MS, 1H-NMR和13C-NMR进行了光谱表征。结果表明,在体外抗癌评价中,所有目标化合物的IC50值均在11.50 ~ 37.99µM范围内,化合物4h的抗乳腺癌活性在所有合成的衍生物中表现出较好的前景。体外抗菌评价表明,化合物4d、4f、4h和4j对所有被试生物均表现出中等抑菌活性。分子对接分析表明,化合物4h与人碳酸酐酶I、蛋白激酶A和激酶纺锤体蛋白(KSP)活性位点残基具有良好的相互作用。
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引用次数: 0
Design, synthesis and antibacterial activity of 9-aryl-6-(2-naphthyl) [1,2,4]triazolo[4,3-a][1,8]naphthyridines 9-芳基-6-(2-萘基)[1,2,4]三唑[4,3-a][1,8]萘啶的设计、合成及抑菌活性研究
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-29 DOI: 10.56042/ijcb.v60i6.43827
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引用次数: 0
Synthesis, characterization, cytotoxicity evaluation and physicochemical properties of some novel N4-substituted aminobenzenesulfonamides 几种新型n4取代氨基磺酰胺的合成、表征、细胞毒性评价及理化性质
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-29 DOI: 10.56042/ijcb.v60i6.43707
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引用次数: 1
Ammonium chloride catalyzed Knoevenagel condensation in PEG-400 as ecofriendly solvent 氯化铵作为环保溶剂在PEG-400中催化Knoevenagel缩合
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-29 DOI: 10.56042/ijcb.v60i6.28094
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引用次数: 1
Analogues designing for dephosphorylation of acetylcholinesterase enzyme 乙酰胆碱酯酶去磷酸化类似物的设计
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-29 DOI: 10.56042/ijcb.v60i6.28544
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引用次数: 0
期刊
Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry
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