Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 21, Pages 7602-7620Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm200939b
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The discovery of two histamine H-3 antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success in identifying these clinical candidates was the development of a compound design strategy that leveraged medicinal chemistry knowledge and traditional assays in conjunction with computational and in vitro safety tools. Overall, clinical compounds 6 and 7 exceeded conservative safety margins and possessed optimal pharmacological and pharmacokinetic profiles, thus achieving our initial goal of identifying compounds with fully aligned oral drug attributes, best-in-class molecules.
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