186347-51-3Relevant academic research and scientific papers
Cyclic imides as potent and selective α-1A adrenergic receptor antagonists
DiPardo, Robert M.,Patane, Michael A.,Newton, Randall C.,Price, RoseAnn,Broten, Theodore P.,Chang, Raymond S.L.,Ransom, Richard W.,Di Salvo, Jerry,Freidinger, Roger M.,Bock, Mark G
, p. 1959 - 1962 (2007/10/03)
We disclose a new compound class of potent and selective α-1A adrenergic receptor antagonists exemplified by the geminally, disubstituted cyclic imide 7. The optimization of lead compounds resulting in the cyclic imide motif is highlighted. The results of in vitro and in vivo studies of selected compounds are presented.
Phenylacetamides as selective α-1A adrenergic receptor antagonists
Patane, Michael A.,DiPardo, Robert M.,Newton, Randall C.,Price, RoseAnn P.,Broten, Theodore P.,Chang, Raymond S.L.,Ransom, Richard W.,Di Salvo, Jerry,Nagarathnam, Dhanapalan,Forray, Carlos,Gluchowski, Charles,Bock, Mark G.
, p. 1621 - 1624 (2007/10/03)
A novel class of potent and selective α-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known α-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described. (C) 2000 Elsevier Science Ltd. All rights reserved.
