Premium
Inotropic Polyazapentalene Sulmazole Analogues
Author(s) -
Barraclough Paul,
Black James W.,
Cambridge David,
Firmin David,
Gerskowitch V. Paul,
Glen R. C.,
Giles Heather,
Gillam Janet M.,
Hull Robert A. D.,
Iyer Ramachandran,
Randall Peter,
Shah Gita P.,
Smith Steven,
Whiting Mark V.
Publication year - 1992
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19923250407
Subject(s) - inotrope , chemistry , imidazole , tautomer , in vivo , thiazole , stereochemistry , chemical synthesis , aryl , biological activity , in vitro , medicine , biochemistry , organic chemistry , alkyl , microbiology and biotechnology , biology
Abstract Aryl substituted 1 H ‐imidazo[1, 2‐ a ]imidazole 8 , imidazo[2,1‐ b ]thiazole 9 , 1,4‐dihydroimidazo[4,5‐ d ]imidazole 11 , and 1(2),4‐dihydroimidazo[4,5‐ c ]pyrazoles 12–17 have been prepared. An X‐ray crystallographic study confirmed the structure of 8 and showed this analogue to exist as the 1 H ‐tautomer. These heterocycles were evaluated as inotropic agents and analogues 12, 15 , and 17 found to display inotropic properties which were less potent in vitro , but more potent in vivo , than those of sulmazole. Structure‐activity relationships are discussed.