A new class of 5-HT 2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties

…, A Kahrs, P Loke, O Meyn, R Nagaraja, S Napier…

Index: Moss, Neil; Choi, Younggi; Cogan, Derek; Flegg, Adam; Kahrs, Andreas; Loke, Pui; Meyn, Orietta; Nagaraja, Raj; Napier, Spencer; Parker, Ashley; Thomas Peterson; Ramsden, Philip; Sarko, Christopher; Skow, Donna; Tomlinson, Josh; Tye, Heather; Whitaker, Mark Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 8 p. 2206 - 2210

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Citation Number: 20

Abstract

We have been exploring the potential of 5-HT2B antagonists as a therapy for chronic heart failure. To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes:(a) potent and selective antagonism of the 5-HT2B receptor,(b) low impact of serum proteins on potency, and (c) desirable pharmacokinetic properties. This Letter describes our investigation of a biphenyl benzimidazole class of ...