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新型苯并恶嗪磺酰胺衍生物的合成及其抗菌活性

Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.

作者信息

Konda Saidulu, Raparthi Srujana, Bhaskar K, Munaganti Rajesh Kumar, Guguloth Vijayacharan, Nagarapu Lingaiah, Akkewar Dattatray M

机构信息

Organic Chemistry Division-II (CPC), CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, A.P., India.

Organic Chemistry Division-II (CPC), CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, A.P., India.

出版信息

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1643-6. doi: 10.1016/j.bmcl.2015.01.026. Epub 2015 Jan 20.

DOI:10.1016/j.bmcl.2015.01.026
PMID:25754493
Abstract

A new series of benzoxazine-6-sulfonamide derivatives were synthesized in excellent yields and the resulting compounds were evaluated for their antimicrobial activities. All the synthesized compounds were assessed for their antibacterial and antifungal activities. Among them 1a, 1b, 1c, 1e, 1h, 2c, 2d, 2e, 2g, 2h, 2i, 2j, 2k and 2l showed low inhibitory concentration (MIC of 31.25 and 62.5 μg/mL) against Gram-positive bacteria, Gram-negative bacteria and fungi, which are comparable to the inhibitory effect of standard drugs.

摘要

合成了一系列新的苯并恶嗪-6-磺酰胺衍生物,产率优异,并对所得化合物的抗菌活性进行了评估。对所有合成化合物的抗菌和抗真菌活性进行了评估。其中,1a、1b、1c、1e、1h、2c、2d、2e、2g、2h、2i、2j、2k和2l对革兰氏阳性菌、革兰氏阴性菌和真菌显示出低抑制浓度(MIC为31.25和62.5μg/mL),与标准药物的抑制效果相当。

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