173899-63-3Relevant academic research and scientific papers
Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials
Praveen Kumar,Gut, Jiri,Guedes, Rita C.,Rosenthal, Philip J.,Santos, Maria M.M.,Moreira, Rui
experimental part, p. 927 - 933 (2011/04/16)
The design, synthesis and evaluation of 3-methylene-substituted indolinones as falcipain inhibitors and antiplasmodial agents are described. These compounds react readily with thiols via an addition-elimination mechanism, indicating their potential as cys
The Bsmoc group as a novel scaffold for the design of irreversible inhibitors of cysteine proteases
Iley, Jim,Moreira, Rui,Martins, Luisa,Guedes, Rita C.,Soares, Claudio M.
, p. 2738 - 2741 (2007/10/03)
Carbamate and ester derivatives of the 1,1-dioxobenzo[b]thiophen-2-ylmethyloxycarbonyl (Bsmoc) scaffold react readily with thiols via a Michael addition at rates not significantly affected by the nature of the carboxylic or carbamic acid leaving group. These Michael acceptors are irreversible inhibitors of the cysteine proteases papain and human liver cathepsin B, displaying first-order kinetics with respect to inhibitor concentration. In contrast, none of the Bsmoc derivatives inhibited porcine pancreatic elastase, a serine protease.
Cell adhesion antagonists: Synthesis and evaluation of a novel series of phenylalanine based inhibitors
Harriman, Geraldine C. B.,Schwender, Charles F.,Gallant, Debra,Cochran, Nancy A.,Briskin, Michael J.
, p. 1497 - 1499 (2007/10/03)
Several phenylalanine based inhibitors were synthesized as antagonists of the leukocyte cell adhesion process that is mediated through the interactions of the mucosal addressin cell adhesion molecule (MAdCAM) and the intgerin α4β7. Analogues 20, 21, 22 and 24 displayed inhibition of adhesion in a cell based assay in the low micromolar range. (C) 2000 Published by Elsevier Science Ltd.
AZIRIDINE DERIVATIVES, THEIR PRODUCTION AND USE
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, (2008/06/13)
The present invention relates to a compound of the formula: STR1 wherein R 1 and Q are independently an optionally esterified or amidated carboxyl group; R 2 is hydrogen, an acyl group or an optionally substituted hydrocarbon residue; X is a divalent hydrocarbon residue which may be substituted; or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as agents for inhibiting thiol protease.
