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合成和评价新型氯吡咯分子,通过常见药效团的分子杂交设计,作为潜在的抗菌剂。

Synthesis and evaluation of novel chloropyrrole molecules designed by molecular hybridization of common pharmacophores as potential antimicrobial agents.

机构信息

Institute of Chemical Technology, Matunga, Mumbai 400019, India.

出版信息

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5681-5. doi: 10.1016/j.bmcl.2010.08.026. Epub 2010 Aug 10.

Abstract

In an attempt to identify new potential lead as antimicrobial agent, 31 novel chloropyrrole derivatives of aroyl hydrazones and chalcones incorporating common pharmacophore of pyoluteorin derivatives were synthesized. Antimicrobial activity of the synthesized compounds was evaluated using broth dilution technique. Based on biological evaluation data it was observed that activity increases as the number of chlorines on pyrrole core increases. Few 1H-pyrrole-2-carbohydrazide derivatives shows activity equivalent to the standard drug ciprofloxacin. Thus, these compounds can act as potential lead for further antibacterial studies.

摘要

为了寻找新的潜在抗菌先导化合物,我们合成了 31 种新型氯代吡咯甲酰腙和查尔酮类化合物,这些化合物包含了吡咯霉素类衍生物的常见药效团。采用肉汤稀释法评估了合成化合物的抗菌活性。根据生物评价数据,我们观察到,随着吡咯核上氯原子数量的增加,活性也随之增加。一些 1H-吡咯-2-甲酰肼衍生物的活性与标准药物环丙沙星相当。因此,这些化合物可以作为进一步抗菌研究的潜在先导化合物。

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