STUDIES ON ORALLY-ACTIVE CEPHALOSPORINS .1. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NEW 3-SUBSTITUTED CARBAMOYLOXYMETHYL CEPHALOSPORINS
STUDIES ON ORALLY-ACTIVE CEPHALOSPORINS .1. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NEW 3-SUBSTITUTED CARBAMOYLOXYMETHYL CEPHALOSPORINS
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DOI：
10.7164/antibiotics.47.1507
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发表时间：
1994-12-01
影响因子：
3.3
通讯作者：
MACHIDA, Y
中科院分区：
文献类型：
--
作者：
NEGI, S;YAMANAKA, M;MACHIDA, Y
报道了7 β -[2-（2-氨基噻唑-4-酰基）-2-羟基亚胺]-3- n， n -二甲基氨基氧基甲基-3-头孢烷-4-羧酸（E1100）及其类似物的合成和抗菌活性，以及1-（异丙氧基羰基）乙酯（E1101）及其类似物的口服吸收性和体内活性。在3-氨基酰基氧甲基头孢醚的n位引入无环和低环烷基影响其抗菌活性，特别是对流感嗜血杆菌的抗菌活性，以及其前药酯的口服吸收性。并讨论了构效关系。
The synthesis and antibacterial activities of 7 beta-[2-(2-aminothiazol-4-yl)-2-hydroxyimido]-3-N,N-dimethylcarbamoyloxymethyl-3-cephem-4-carboxylic acid (E1100) and its analogs are described, as well as oral absorbability and in vivo activities of the 1-(isopropoxycarbonyloxy)ethyl ester (E1101) and its analogous esters. The introduction of acyclic and cyclic lower alkyl groups at the N-position of 3-carbamoyloxymethyl cephems influences antibacterial activities, especially against H. influenzae, and oral absorbability of their prodrug esters. The structure-activity relationships are also discussed.