Novel potent substance P and neurokinin A receptor antagonists. Conception,synthesis and biological evaluation of indolizine derivatives |
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Authors: | Millet Régis Domarkas Juozas Rigo Benoît Goossens Laurence Goossens Jean-François Houssin Raymond Hénichart Jean-Pierre |
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Affiliation: | Institut de Chimie Pharmaceutique Albert Lespagnol, Université de Lille 2, EA 2692, 3 rue du Professeur Laguesse, B.P. 83, F-59006, Lille, France |
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Abstract: | 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. |
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