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Acetamide Scanning around Bicyclic Thiazoles: SAR at the H 3 Receptor
Author(s) -
Dene Frédéric,
Célanire Sylvain,
Christophe Bernard,
Defays Sabine,
Delaunoy Christel,
Delporte MarieLaure,
Detrait Eric,
Durieu Véronique,
Gillard Michel,
Lamberty Yves,
Lorent Geneviève,
Nicolas JeanMarie,
Vanbellinghen Alain,
Van Houtvin Nathalie,
Provins Laurent
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100248
Subject(s) - bicyclic molecule , acetamide , azepine , amide , stereochemistry , chemistry , in vivo , combinatorial chemistry , organic chemistry , biology , microbiology and biotechnology
A surprisingly homogeneous SAR against the H 3 receptor was revealed for positional acetamide isomers of bicyclic thiazoles fused to various cyclic amines. Pyrroline and azepine rings were used to probe the central position of the amide. In vitro ADMET parameters were measured, and the isomer with the best overall properties was assessed in vivo.