首页> 外文期刊>International Journal of Pharmacy and Pharmaceutical Sciences >SYNTHESIS OF NOVEL N-(ARYL) DIAZENYL THIAZOL-2-AMINES AND BEZYLIDENE-THIAZOLIDIN-4-ONES LINKED TO INDOLE NUCLEUS AS ANTIOXIDANT, ANTIMICROBIAL, ANTIMYCOBACTERIAL AND CYTOTOXIC AGENTS
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SYNTHESIS OF NOVEL N-(ARYL) DIAZENYL THIAZOL-2-AMINES AND BEZYLIDENE-THIAZOLIDIN-4-ONES LINKED TO INDOLE NUCLEUS AS ANTIOXIDANT, ANTIMICROBIAL, ANTIMYCOBACTERIAL AND CYTOTOXIC AGENTS

机译:新型N-(芳基)二氮杂噻唑-2-酰胺和苯并二氮杂噻吩丁-4-酮类化合物的合成,与吲哚核苷为抗氧化剂,抗微生物剂,抗细菌和细胞毒性剂。

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Objective: Synthesis of Some of the novel indole derivatives viz., N-4-aryl-N-{[(aryl)diazenyl](2-phenyl-1H-indol-3-yl)methylene}thiazol-2-amines 4a-f and 5-(4-substituted bezylidene)-3-[4-(arylthiazol-2-yl)-2-(2-phenyl-1H-indol-3-yl)]thiazolidin-4-ones 6a-i. The structures of all the newly synthesized compounds were characterized by their IR, PMR, CMR and mass spectral studies, Methods: All these newly synthesized compounds were screened for their in-vitro antimicrobial activity by broth micro-dilution method, anti-TB activity by alamar blue dye method, Antioxidant activities: like, 1,1-Diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity (RSA), Ferric ions (Fe3 +) reducing antioxidant power (FRAP), Ferrous (Fe2 +) metal ion chelating activity and in-vitro growth effect o f cytotoxic activity was assessed by calorimetric method. Results: Compounds 4b, 4e and 6f exhibited good radical scavenging activity (RSA) (MIC <25 μg/ml), 6a displayed good ferric ions (Fe3 +) reducing antioxidant power (FRAP) at a concentration 100 μg/ml, compounds 4a and 6a exhibited good activity against all the screened bacteria and fungi, 4a exhibited excellent anti-mycobacterial activity (MIC 0.2 μg/ml), where as compound 4a, 4d and 6g showed promising cytotoxic activity (MIC <10 μg). Conclusion: Compounds 4a and 6a exhibited potent anti-microbial activity against all the screened bacteria and fungi, compound 4a shown potent anti-mycobacterial activity
机译:目的:合成一些新颖的吲哚衍生物,即N-4-芳基-N-{[((芳基)二氮烯基](2-苯基-1H-吲哚-3-基)亚甲基}噻唑-2-胺4a- f和5-(4-取代的亚苄基)-3- [4-(芳基噻唑-2-基)-2-(2-苯基-1H-吲哚-3-基)]噻唑烷-4-酮6a-i。通过IR,PMR,CMR和质谱研究对所有新合成的化合物的结构进行表征。方法:通过肉汤微稀释法筛选所有这些新合成的化合物的体外抗菌活性,通过HPLC筛选其抗TB活性。阿马尔玛蓝染料法,抗氧化活性:像1,1-二苯基-2-吡啶基肼基(DPPH)自由基清除活性(RSA),铁离子(Fe3 +)降低抗氧化能力(FRAP),亚铁(Fe2 +)金属离子通过量热法评估了螯合活性和细胞毒性活性的体外生长作用。结果:化合物4b,4e和6f表现出良好的自由基清除活性(RSA)(MIC <25μg/ ml),化合物6a表现出良好的三价铁离子(Fe3 +),降低浓度为100μg/ ml的抗氧化能力(FRAP),化合物4a化合物6a和6a对所有筛选出的细菌和真菌均表现出良好的活性,化合物4a具有出色的抗分枝杆菌活性(MIC 0.2μg/ ml),而化合物4a,化合物4d和6g则显示出有希望的细胞毒性活性(MIC <10μg)。结论:化合物4a和6a对所有经筛选的细菌和真菌均具有有效的抗菌活性,化合物4a具有对分枝杆菌的有效抗菌活性

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