human P2X3 receptor antagonist compound that can penetrate the central nervous system, the compound collection of Gedeon Richter was screened. A hit series of tricyclic compounds was subjected to a rapid, two-step optimization process focusing on increasing potency, improving metabolic stability and CNS penetrability. Attempts resulted in compound 65, a potential tool compound for testing P2X3 inhibitory
Influence of solvent viscosity on the rate of hydrolysis of dipeptides by carboxypeptidase Y
作者:Yoshifumi Kanosue、Satoshi Kojima、Katsuo Ohkata
DOI:10.1002/poc.752
日期:2004.5
The influence of solventviscosity on the rate of enzymatic hydrolysis of a series of dipeptides (Z-Phe-Gly, Z-Phe-Sar, Z-Phe-Ala, Z-Phe-NMeAla, Z-Phe-Aib and Z-Phe-Pro) by carboxypeptidaseY was investigated. The effect of solventviscosity on the enzymatic hydrolysis revealed that whereas all kcat values decreased with viscosity, those of the N-alkyl peptides decreased more than those of the N-H
7-amino-3-propenylcephalosporanic acid and esters thereof
申请人:Bristol-Meyers Company
公开号:US04699979A1
公开(公告)日:1987-10-13
This invention provides novel cephalosporin intermediates, 7.beta.-amino-3-[(Z)-1-propen-1-y1]-3-cephem-4-carboxylic acid and esters thereof having the general formula ##STR1## wherein the configuration of the 3-propenyl group is Z sometimes referred to as cis- and R is hydrogen or a conventional carboxy-protected group, or a physiologically hydrolyzable esterifying group, and acid addition salts thereof and the metal salts of the foregoing substance wherein R is hydrogen. These compounds are useful as intermediates for preparation of orally active cephalosporins.