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作为潜在抗菌剂的2-[1,2-二氢吡唑-4-基]-1,3,4-噻二唑衍生物的合成

Synthesis of 2-[1,2-dihydropyrazol-4-yl]-1,3,4-thiadiazole derivatives as potential antimicrobial agents.

作者信息

Auzzi G, Bruni F, Clauser M, Ciciani G, Costanzo A, Pecori Vettori L P, Donato R

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.

出版信息

Farmaco. 1990 Jan;45(1):81-92. doi: 10.1002/chin.199037192.

Abstract

The synthesis of some 2-[1,2-dihydropyrazol-4-yl]-1,3,4-thiadiazole derivatives is performed by reacting 4-dithiocarboxylic acid hydrazides of 3-amino-1,2-dihydro-5H-pyrazol-5-one and 3-amino-1,2-dihydro-1-methyl-5H-pyrazol-5-one with carboxylic acid derivatives. The unusual behaviour of 3-amino-1,2-dihydro-1-methyl-5H-pyrazol-5-one towards acetylating agents is described. The antimicrobial activity of some 2-[1,2-dihydropyrazol-4-yl]-1,3,4-thiadiazole derivatives is tested in a preliminary screening.

摘要

通过使3-氨基-1,2-二氢-5H-吡唑-5-酮和3-氨基-1,2-二氢-1-甲基-5H-吡唑-5-酮的4-二硫代羧酸酰肼与羧酸衍生物反应,合成了一些2-[1,2-二氢吡唑-4-基]-1,3,4-噻二唑衍生物。描述了3-氨基-1,2-二氢-1-甲基-5H-吡唑-5-酮对乙酰化剂的异常行为。在初步筛选中测试了一些2-[1,2-二氢吡唑-4-基]-1,3,4-噻二唑衍生物的抗菌活性。

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