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新型吡唑并[3,4-d]嘧啶衍生物的合成及抗菌活性研究。

Synthesis and antimicrobial activity of novel pyrazolo[3,4-d]pyrimidin derivatives.

机构信息

Swami Ramanand Teerth Marathawada University, School of Life Sciences, Nanded 431606, India.

出版信息

Eur J Med Chem. 2010 Apr;45(4):1635-8. doi: 10.1016/j.ejmech.2009.12.040. Epub 2009 Dec 28.

Abstract

Pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidin-4-one derivatives have been prepared by cyclocondensation of ethyl 2-cyano-3,3-bis(methylthio)prop-2-enoate with 2-amino-4-(substitutedphenyl)thiazole to give 3-cyano-2-methylthio-4-oxo-4H-6-(substitutedphenyl)thiazolo[3,2-a]pyrimidin (2a-j) and further reacting with hydrazine hydrate to yield the target compounds (3a-j). The chemical structure of the compounds was confirmed by IR and (1)H NMR spectral data. All the compounds of the series have been screened for their antibacterial and antifungal activity studies. The result revealed that all compounds showed significant antimicrobial activity.

摘要

吡唑并[3,4-d]噻唑并[3,2-a]嘧啶-4-酮衍生物是由乙基 2-氰基-3,3-双(甲硫基)-2-丙烯酸酯与 2-氨基-4-(取代苯基)噻唑环缩合得到的,得到 3-氰基-2-甲硫基-4-氧代-4H-6-(取代苯基)噻唑并[3,2-a]嘧啶(2a-j),然后与水合肼进一步反应得到目标化合物(3a-j)。化合物的化学结构通过 IR 和 1H NMR 光谱数据得到确认。对该系列的所有化合物进行了抗菌和抗真菌活性研究。结果表明,所有化合物均表现出显著的抗菌活性。

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