Improvements in or relating to naphthylglycyl cephalosporin derivatives
申请人:ELI LILLY AND COMPANY
公开号:EP0122155A2
公开(公告)日:1984-10-17
Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and particularly useful in the oral treatment of upper respiratory infections.
萘乙酰基和四氢萘乙酰基头孢菌素是强效抗菌剂,尤其适用于口服治疗上呼吸道感染。
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid
作者:Stjepan Kukolja、Susan E. Draheim、Janice L. Pfeil、Robin D. G. Cooper、Bernard J. Graves、Richard E. Holmes、David A. Neel、George W. Huffman、J. Alan Webber
DOI:10.1021/jm00150a022
日期:1985.12
A structure-activity relationship study of a number of orally absorbed cephalosporins together with their syntheses is described. These new cephalosporins are benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid. Several different synthetic methods for the glycine side chains, their protection, and the final acylations are reported. Several of these analogues were more active than cephalexin both in vitro and in vivo against commonly encountered Gram-positive bacteria. (R)-7-(3-Benzothienylglycylamido)-3-methyl-3-cephem-4-carboxylic acid (1R) has emerged as a potent antibacterial agent and is currently undergoing preclinical evaluation.
作者:Anna Munder、Yoni Moskovitz、Aviv Meir、Shirin Kahremany、Laura Levy、Michal Kolitz-Domb、Guy Cohen、Efrat Shtriker、Olga Viskind、Jean-Paul Lellouche、Hanoch Senderowitz、Steven D. Chessler、Edward E. Korshin、Sharon Ruthstein、Arie Gruzman
DOI:10.1039/c8md00419f
日期:——
The nanoscale composite improved β-cell functions in terms of rate of proliferation, glucose-stimulated insulin secretion, resistance to cellular stress and functional maturation.