[EN] RENIN INHIBITORS AND METHOD OF USE THEREOF<br/>[FR] INHIBITEURS DE LA RÉNINE ET PROCÉDÉ D'UTILISATION CORRESPONDANT
申请人:VITAE PHARMACEUTICALS INC
公开号:WO2009154766A1
公开(公告)日:2009-12-23
Disclosed are aspartic protease inhibitors represented by the following Formula: wherein R1 , R2, R3, R4, R5, R6, R7a, R7b and n are as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods for treating an aspartic protease mediated disorder using the same.
Synthesis and evaluation of some stable multisubstrate adducts as specific inhibitors of spermidine synthase
作者:Kuo-Chang Tang、Roy Mariuzza、James K. Coward
DOI:10.1021/jm00143a003
日期:1981.11
were assayed as inhibitors of spermidine synthase, and both 2b and 3b were found to be potent inhibitors of the enzyme. The thioether 2b is the most potent inhibitor of spermidine synthase described to date and is almost totally devoid of inhibitory activity against the closely related aminopropyltransferase, spermine synthase. This type of compound should have use as a specific inhibitor of spermidine
t-Butyl methyl iminodicarboxylate potassium salt: a modified Gabriel reagent for the introduction of t-butoxycarbonylamino groups
作者:John D. Elliott、John H. Jones
DOI:10.1039/c39770000758
日期:——
t-Butylmethyliminodicarboxylatepotassiumsalt is a stable, easily prepared, non hygroscopic compound; it undergoes smooth N-alkylation in dipolar aprotic solvents to give derivatives which suffer loss of the methoxycarbonyl group on mild treatment with alkali, enabling the direct conversion R–X → R–NHBoc (Boc = t-butoxycarbonyl) to be achieved.
Pyridonecarboxylic Acids as Antibacterial Agents. VII. Synthesis and Structure-Activity Relationship of Amino- and Hydroxyl-Substituted 7-Cycloalkyl and 7-Vinyl Derivatives of l-Cyclopropyl-6-fluoro-4- quinolone-3-carboxylic Acid.
Novel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylicacid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, comparable to that of ciprofloxacin, against gram-negative bacteria including P. aeruginosa