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7-(2-取代苯基噻唑烷-2-酮基)-苯并吡喃-2-酮衍生物的合成与抗菌活性。

Synthesis and antimicrobial activity of 7-(2-substituted phenylthiazolidinyl)-benzopyran-2-one derivatives.

机构信息

Department of Pharmaceutical chemistry, KLE's College of Pharmacy, Vidyanagar, Hubli-580031, Karnataka, India.

出版信息

Eur J Med Chem. 2010 Jan;45(1):85-9. doi: 10.1016/j.ejmech.2009.09.028. Epub 2009 Sep 23.

DOI:10.1016/j.ejmech.2009.09.028
PMID:19837487
Abstract

A series of 7-(2-substituted phenylthiazolidinyl)-benzopyran-2-one derivatives have been synthesized by reaction of 7-amino-4-methyl-benzopyran-2-one (1) with an appropriate substituted aldehydes to obtain various Schiff bases (3a-k) which on treatment with thioglycolic acid afforded the title compounds (4a-k). Purity of the compounds has been confirmed by TLC. Structure of these compounds were established on the bases IR, 1H NMR, 13C NMR and Mass spectral data. Schiff bases and title compounds were evaluated for antibacterial and antifungal activities against various bacterial and fungal strains. The results showed that compounds 3d, 3f, 4d, 4f and 4i (100 microg/ml) exhibited good antibacterial and antifungal activity as that of standard antibiotics Ciprofloxacin and Griseofulvin.

摘要

已经通过将 7-氨基-4-甲基苯并吡喃-2-酮(1)与适当取代的醛反应合成了一系列 7-(2-取代苯基噻唑烷-2-酮)苯并吡喃-2-酮衍生物,以获得各种席夫碱(3a-k),将其与硫代乙醇酸处理后得到标题化合物(4a-k)。通过 TLC 确认了化合物的纯度。这些化合物的结构是基于 IR、1H NMR、13C NMR 和质谱数据确定的。对席夫碱和标题化合物进行了针对各种细菌和真菌菌株的抗菌和抗真菌活性评估。结果表明,化合物 3d、3f、4d、4f 和 4i(100μg/ml)表现出与标准抗生素环丙沙星和灰黄霉素相当的良好的抗菌和抗真菌活性。

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