Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity

Bioorganic and Medicinal Chemistry Letters

Volumn 11, Issue 19, 2001, Pages 2597-2602

  Ashton, Wallace T ^a   Sisco, Rosemary M ^a   Kieczykowski, Gerard R ^a   Yang, Yi Tien ^a   Yudkovitz, Joel B ^a   Cui, Jisong ^a   Mount, George R ^a   Ren, Rena Ning ^a   Wu, Tsuei Ju ^a   Shen, Xiaolan ^a   Lyons, Kathryn A ^a   Mao, An Hua ^a   Carlin, Josephine R ^a   Karanam, Bindhu V ^a   Vincent, Stella H ^a   Cheng, Kang ^a   Goulet, Mark T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 METHYLPYRIDIN 2(1H) ONE DERIVATIVE; 7 AZANORBORNANE LEAD; AMIDE; AMINE; AZETIDINE DERIVATIVE; BUSERELIN; DIPYRONE; GONADORELIN; GONADORELIN RECEPTOR; HORMONE RECEPTOR BLOCKING AGENT; INDOLE DERIVATIVE; INOSITOL PHOSPHATE; ISOQUINUCLIDINE AMIDE; LEAD; LUTEINIZING HORMONE; METHOXYPYRIDINE; METHYL GROUP; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; PYRIDINE; PYRROLIDINE DERIVATIVE; TRYPTAMINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CHEMICAL MODIFICATION; CHEMICAL REACTION; CHO CELL; CONTROLLED STUDY; DOG; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG COMPETITION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; HORMONE BLOOD LEVEL; HORMONE RECEPTOR INTERACTION; HYDROLYSIS; IC 50; MALE; NONHUMAN; PROTEIN EXPRESSION; RAT; REACTION ANALYSIS; RHESUS MONKEY; SPECIES DIFFERENCE; STEREOSPECIFICITY;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; DOGS; INDOLES; LUTEINIZING HORMONE; MACACA MULATTA; MODELS, ANIMAL; RATS; RECEPTORS, LHRH; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPTAMINES;

CANIS FAMILIARIS;

EID: 17944383430     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(01)00512-1     Document Type: Article

References (30)