2-β-氧亚氨基和链烯基青霉烷酸砜衍生物作为β-内酰胺酶抑制剂的合成与评价

Synthesis and evaluation of 2 beta-oxyimino and alkenylpenicillanic acid sulfone derivatives as beta-lactamase inhibitors.

作者信息

Cho Y S, Ha Y J, Kwon J S, Pae A N, Choi K I, Koh H Y, Chang M H, Yoon C M, Lee G S

机构信息

Biochemicals Research Center, Korea Institute of Science and Technology, Seoul, Korea.

出版信息

Arch Pharm (Weinheim). 1999 Jan;332(1):7-12. doi: 10.1002/(sici)1521-4184(19991)332:1<7::aid-ardp7>3.0.co;2-m.

DOI:10.1002/(sici)1521-4184(19991)332:1<7::aid-ardp7>3.0.co;2-m

PMID:10073138

Abstract

The synthesis and in vitro synergies of 2 beta-alkenyl and oxyiminopenam sulfone derivatives are described. Most of the compounds synthesized exhibited good inhibitory activities and synergistic antibacterial activities with piperacillin and ceftriaxone, respectively, against several beta-lactamase producing strains. Particularly the 2 beta-alkenylpenam sulfone derivatives. 1e and 1g, showed good synergistic activity with ceftriaxone against Citrobacter freundi NIH 10018-68 and Proteus vulgaris 20. Also the compounds 2a, 2c, and 2f, 2 beta-oxyiminopenam sulfone derivatives, exhibited improved synergistic activity with piperacillin against Citrobacter freundi NIH 10018-68.

摘要

描述了2-β-烯基和氧亚胺青霉烷砜衍生物的合成及其体外协同作用。合成的大多数化合物分别对几种产β-内酰胺酶菌株显示出良好的抑制活性以及与哌拉西林和头孢曲松的协同抗菌活性。特别是2-β-烯基青霉烷砜衍生物1e和1g，对弗氏柠檬酸杆菌NIH 10018-68和普通变形杆菌20显示出与头孢曲松良好的协同活性。此外，2-β-氧亚胺青霉烷砜衍生物2a、2c和2f与哌拉西林对弗氏柠檬酸杆菌NIH 10018-68表现出增强的协同活性。