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Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
He, Shuwen; Ye, Zhixiong; Dobbelaar, Peter H; Sebhat, Iyassu K; Guo, Liangqin; Liu, Jian; Jian, Tianying; Lai, Yingjie; Franklin, Christopher L; Bakshi, Raman K; Dellureficio, James P; Hong, Qingmei; Tsou, Nancy N; Ball, Richard G; Cashen, Doreen E; Martin, William J; Weinberg, David H; Macneil, Tanya; Tang, Rui; Tamvakopoulos, Constantin; Peng, Qianping; Miller, Randy R; Stearns, Ralph A; Chen, Howard Y; Chen, Airu S; Strack, Alison M; Fong, Tung M; Macintyre, D Euan; Wyvratt, Matthew J; Nargund, Ravi P.
Affiliation
  • He S; Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. shuwen_he@merck.com
Bioorg Med Chem Lett ; 20(7): 2106-10, 2010 Apr 01.
Article in En | MEDLINE | ID: mdl-20207541
ABSTRACT
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Spiro Compounds / Receptor, Melanocortin, Type 4 / Erectile Dysfunction / Indans Limits: Animals / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Spiro Compounds / Receptor, Melanocortin, Type 4 / Erectile Dysfunction / Indans Limits: Animals / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: United States