Quinazolino-thiadiazoles as antimicrobial agents

Harun Patel , Atul Shirkhedkar , Sanjay Bari , Kamalkishor Patil , Amit Arambhi , Chandrakantsing Pardeshi , Abhijeet Kulkarni , Sanjay Surana
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引用次数: 13

Abstract

In the present research, we report the synthesis and in vitro antimicrobial activity of a new series of novel quinazolino-thiadiazoles as fused pharmacophore (3–20). In general, the results of the in vitro antibacterial activity are encouraging, as out of 18 compounds tested, Compounds 3 and 8 with a 4-chlorophenyl and 4-nitro phenyl at C-2 of thiadiazole and chloromethyl substituent at C-2 of quinazolinone displayed a broad spectrum antimicrobial activity against all the strains, while compounds 13 and 16 again with a 4-chlorophenyl and 4-nitrophenyl at C-2 of thiadiazole and ethyl substituent at C-2 of quinazolinone showed the same potency but with a narrower spectrum (Bacterial and Fungal strains) with MIC values of 62.5 µg/ml. The structures of the compounds were confirmed by IR, 1H NMR, 13C NMR and Mass analysis. It is worth to mention that the combination of two biologically active moieties quinazoline and thiadiazole profoundly influences the biological activity.

喹唑啉-噻二唑类抗菌药物
在本研究中,我们报道了一系列新的喹唑啉-噻二唑作为融合药效团的合成及其体外抗菌活性(3-20)。结果表明,化合物3和8在噻二唑的C-2处含有4-氯苯基和4-硝基苯基,在喹唑啉酮的C-2处含有氯甲基取代基,对所有菌株均具有广谱抗菌活性。而化合物13和16在噻二唑的C-2处含有4-氯苯基和4-硝基苯基,在喹唑啉酮的C-2处含有乙基取代基,具有相同的效价,但光谱较窄(细菌和真菌菌株),MIC值为62.5 µg/ml。化合物的结构经IR、1H NMR、13C NMR和质谱分析证实。值得一提的是,两种生物活性基团喹唑啉和噻二唑的结合对生物活性产生了深远的影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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