1. Academic Validation
  2. Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers

Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers

  • Bioorg Med Chem Lett. 2010 Feb 15;20(4):1436-9. doi: 10.1016/j.bmcl.2009.12.085.
John Lloyd 1 Heather J Finlay Wayne Vacarro Tram Hyunh Alexander Kover Rao Bhandaru Lin Yan Karnail Atwal Mary Lee Conder Tonya Jenkins-West Hong Shi Christine Huang Danshi Li Huabin Sun Paul Levesque
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, USA. john.lloyd@bms.com
Abstract

Design and synthesis of pyrazolodihydropyrimidines as KV1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed atrial selective prolongation of effective refractory period in rabbits and was selected for clinical development.

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