Bioorganic and Medicinal Chemistry Letters p. 5293 - 5297 (2005)
Update date:2022-08-05
Topics:
Vasudevan, Anil
Souers, Andrew J.
Freeman, Jennifer C.
Verzal, Mary K.
Gao, Ju
Mulhern, Mathew M.
Wodka, Derek
Lynch, John K.
Engstrom, Kenneth M.
Wagaw, Seble H.
Brodjian, Sevan
Dayton, Brian
Falls, Doug H.
Bush, Eugene
Brune, Michael
Shapiro, Robin D.
Marsh, Kennan C.
Hernandez, Lisa E.
Collins, Christine A.
Kym, Philip R.
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.
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Doi:10.1021/om0508177
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