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Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.

作者信息

Kukolja S, Draheim S E, Graves B J, Hunden D C, Pfeil J L, Cooper R D, Ott J L, Counter F T

出版信息

J Med Chem. 1985 Dec;28(12):1896-903. doi: 10.1021/jm00150a023.

DOI:10.1021/jm00150a023
PMID:3877809
Abstract

Three positional analogues (4-, 5-, and 7-) of benzothienylglycine and (N-acetylindolinyl)-5-glycine were prepared and coupled to 7-aminodeacetoxycephalosporanic acid (7-ADCA) to give the cephalosporins 17a-c. In addition two isomeric (2,3-b and 3,2-b) thienothiopheneglycines were synthesized and coupled to 7-ADCA to yield cephalosporins 30d and 30e. In vitro testing of these new cephalosporins indicates good activity against Gram-positive bacteria. Against Streptococcus pneumoniae infections compound 25 displayed better mouse protection (both orally and subcutaneously) than cephalexin.

摘要

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