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Cardiotonic ‘C’ Ring Modified Isomazole Analogues
Author(s) -
Barraclough Paul,
Black James W.,
Cambridge David,
Demaine Derek A.,
Paul Gerskowitch V.,
Giles Heather,
Hill Alan P.,
Hull Robert A. D.,
Lyer Ramachandran,
Richard King W.,
Livingstone David J.,
Nobbs Malcolm S.,
Randall Peter,
Shah Gita P.,
Whiting Mark V.
Publication year - 1990
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.19903230812
Subject(s) - chemistry , inotrope , ring (chemistry) , stereochemistry , in vivo , chemical synthesis , bicyclic molecule , structure–activity relationship , in vitro , biochemistry , medicine , organic chemistry , biology , microbiology and biotechnology
Isomazole analogues which have achiral electron withdrawing substituents at the 4′‐position and analogues with heterocyclic ‘C’ rings have been synthesized and evaluated as inotropic agents. It was found that pyridyl could replace phenyl in the ‘C’ ring without loss of activity. The 4′‐methylsulphonyl, ‐cyano, ‐carboxamido, and acetyl analogues had similar inotropic potencies to Isomazole whilst displaying superior cardiovascular profiles in in vivo studies.