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2 -（吡啶基）青霉烯类化合物的合成及其构效关系

Synthesis and structure-activity relations in the class of 2-(pyridyl)penems.

作者信息

Bedeschi A, Visentin G, Perrone E, Giudici F, Zarini F, Franceschi G, Meinardi G, Castellani P, Jabes D, Rossi R

机构信息

Farmitalia Carlo Erba SpA, R. & D., Infectious Diseases Dept., Milan, Italy.

出版信息

J Antibiot (Tokyo). 1990 Mar;43(3):306-13. doi: 10.7164/antibiotics.43.306.

DOI:10.7164/antibiotics.43.306
PMID:2182592
Abstract

The isosteric CH----N substitution in the class of 2-arylpenems results in improved antibacterial activity, with retention of the favorable characteristic of stability towards renal dehydropeptidase. High therapeutic efficacy was demonstrated in experimental mice septicemias with the 2-(3-pyridyl) derivative 2b and its orally absorbed acetoxymethyl ester prodrug 4n.

摘要

在2-芳基青霉烯类化合物中，等排体CH----N取代导致抗菌活性提高，同时保留了对肾脱氢肽酶稳定的有利特性。2-(3-吡啶基)衍生物2b及其口服吸收的乙酰氧基甲酯前药4n在实验性小鼠败血症中显示出高治疗效果。

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