ACS Medicinal Chemistry Letters p. 414 - 418 (2013)
Update date:2022-08-05
Topics:
Qian, Yimin
Corbett, Wendy L.
Berthel, Steven J.
Choi, Duk Soon
Dvorozniak, Mark T.
Geng, Wanping
Gillespie, Paul
Guertin, Kevin R.
Haynes, Nancy-Ellen
Kester, Robert F.
Mennona, Francis A.
Moore, David
Racha, Jagdish
Radinov, Roumen
Sarabu, Ramakanth
Scott, Nathan R.
Grimsby, Joseph
Mallalieu, Navita L.
To resolve the metabolite redox cycling associated with our earlier clinical compound 2, we carried out lead optimization of lead molecule 1. Compound 4 showed improved lipophilic ligand efficiency and demonstrated robust glucose lowering in diet-induced obese mice without a liability in predictive preclinical drug safety studies. Thus, it was selected as a clinical candidate and further studied in type 2 diabetic patients. Clinical data suggests no evidence of metabolite cycling, which is consistent with the preclinical profiling of metabolism.
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