Novel potent substance P and neurokinin A receptor antagonists. Conception, synthesis and biological evaluation of indolizine derivatives.
Exploration of SAR around dual NK(1)/NK(2) antagonist Cbz-Gly-Leu-Trp-OBzl(CF(3))(2) and its derivatives disclosed the essential requirements for more potent dual NK(1)/NK(2) binding. We report here the synthesis and the biological properties of a novel series of indolizine including pharmacophoric elements.
Millet
Régis
R
Institut de Chimie Pharmaceutique Albert Lespagnol, Université de Lille 2, EA 2692, 3 rue du Professeur Laguesse, B.P. 83, F-59006, Lille, France
Domarkas
Juozas
J
Rigo
Benoît
B
Goossens
Laurence
L
Goossens
Jean-François
JF
Houssin
Raymond
R
Hénichart
Jean-Pierre
JP
D000818:Animals; D001249:Asthma / Q000188:drug therapy; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism; D006224:Cricetinae; D015195:Drug Design; D006801:Humans; D007212:Indolizines / Q000138:chemical synthesis* / Q000494:pharmacology; D064729:Neurokinin-1 Receptor Antagonists; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D007212:Indolizines; D064729:Neurokinin-1 Receptor Antagonists; D009842:Oligopeptides; D018041:Receptors, Neurokinin-2; D002118:Calcium