Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 7, 2010, Pages 2106-2110

  He, Shuwen ^a   Ye, Zhixiong ^a   Dobbelaar, Peter H ^a   Sebhat, Iyassu K ^a   Guo, Liangqin ^a   Liu, Jian ^a   Jian, Tianying ^a   Lai, Yingjie ^a   Franklin, Christopher L ^a   Bakshi, Raman K ^a   Dellureficio, James P ^a   Hong, Qingmei ^a   Tsou, Nancy N ^a   Ball, Richard G ^a   Cashen, Doreen E ^a   Martin, William J ^a   Weinberg, David H ^a   MacNeil, Tanya ^a   Tang, Rui ^a   Tamvakopoulos, Constantin ^a   Peng, Qianping ^a   Miller, Randy R ^a   Stearns, Ralph A ^a   Chen, Howard Y ^a   Chen, Airu S ^a   Strack, Alison M ^a   Fong, Tung M ^a   MacIntyre, D Euan ^a   Wyvratt Jr , Matthew J ^a   Nargund, Ravi P ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Agonist; Erectile dysfunction; MC4R; Melanocortin subtype 4 receptor; Spiroindane

Indexed keywords

MELANOCORTIN 4 RECEPTOR; MELANOCORTIN RECEPTOR AGONIST; SPIROINDANE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CHEMICAL STRUCTURE; CONTROLLED STUDY; DRUG DESIGN; DRUG SELECTIVITY; DRUG SYNTHESIS; FEMALE; HUMAN; MALE; MODEL; MOUSE; NONHUMAN; RAT; RODENT; X RAY DIFFRACTION;

ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DOGS; ERECTILE DYSFUNCTION; HAPLORHINI; HUMANS; INDANS; MALE; MICE; MOLECULAR STRUCTURE; PROTEIN BINDING; RATS; RECEPTOR, MELANOCORTIN, TYPE 4; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP;

RODENTIA;

EID: 77949485502     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.02.058     Document Type: Article

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