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合成含吲唑结构的新型α-氨基膦酸酯类化合物及其生物活性。

Synthesis of new α aminophosphonate system bearing Indazole moiety and their biological activity.

机构信息

Post Graduate and Research Centre, Department of Chemistry, Maulana Azad College, Rauza Bagh, Aurangabad 431 001, Maharashtra, India.

出版信息

Eur J Med Chem. 2012 Apr;50:39-43. doi: 10.1016/j.ejmech.2012.01.024. Epub 2012 Jan 30.

DOI:10.1016/j.ejmech.2012.01.024
PMID:22341789
Abstract

We are reporting herein for the first time the synthesis of α-aminophosphonates containing Indazole moiety in two steps. In the first step, imines of substituted N-benzylidene-1-methyl-1H-indazole-3-carbohydrazide are synthesized and in the next step it has converted to α-aminophosphonates using chlorotrimethylsilane (TMSCl) and triethyl phosphite. Some of the synthesized derivatives are evaluated for antibacterial activity against different bacterial strains.

摘要

我们在此首次报道了两步法合成含吲唑部分的α-氨基膦酸酯。在第一步中，合成取代的 N-苄叉-1-甲基-1H-吲唑-3-甲酰肼亚胺，然后使用三甲基氯硅烷（TMSCl）和三乙基亚膦酸酯将其转化为α-氨基膦酸酯。一些合成的衍生物被评估了对不同细菌菌株的抗菌活性。

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