Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

Bioorganic and Medicinal Chemistry Letters

Volumn 10, Issue 5, 2000, Pages 443-447

  Walsh, Thomas F ^a   Toupence, Richard B ^a   Young, Jonathan R ^a   Huang, Song X ^a   Ujjainwalla, Feroze ^a   Devita, Robert J ^a   Goulet, Mark T ^a   Wyvratt Jr , Matthew J ^a   Fisher, Michael H ^a   Lo, Jane Ling ^a   Ren, Ning ^a   Yudkovitz, Joel B ^a   Yang, Yi Tien ^a   Cheng, Kang ^a   Smith, Roy G ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GONADORELIN ANTAGONIST; GONADORELIN RECEPTOR; QUINOLONE DERIVATIVE;

ARTICLE; DRUG POTENCY; HUMAN; NONHUMAN; RAT; RECEPTOR BLOCKING; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; CHO CELLS; CRICETINAE; HUMANS; LUTEINIZING HORMONE; PHOSPHATIDYLINOSITOLS; QUINOLONES; RATS; RECEPTORS, LHRH; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034611086     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(00)00024-X     Document Type: Article

References (15)

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10. 3 as eluent. Evaporation of the purified fractions and drying in vacuo afforded 0.125 g (54%) of compound 8y as an amorphous pale yellow powder.
11. 3OD, 125 MHz) δ 21.47 (2C), 22.95, 24.28, 29.53, 32.23, 41.63, 57.58, 64.13, 70.67, 111.78, 117.07, 117.60, 123.64, 126.18, 129.49 (2C), 130.48, 131.01, 133.45, 134.93, 139.26 (2C), 140.95, 158.26, 158.84, 159.90, 161.32, 165.62, 168.02.
12. 2151]buserelin to GnRH receptors by 50%.
13. 50value which is the antagonist concentration required to inhibit the GnRH stimulated PI hydrolysis by 50%.
14. 50value which is the antagonist concentration required to inhibit the GnRH timulated LH release by 50%.
15. 50values for GnRH receptor binding shown for 9a and 9b in Table 1 were determined using rat pituitary membranes. See refs 5 or 6 for a description of the assay.