Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6- methyluracils containing a substituted thiophene or thiazole at C-5

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 19, 2004, Pages 4967-4973

  Rowbottom, Martin W ^a   Tucci, Fabio C ^a   Connors Jr , Patrick J ^a   Gross, Timothy D ^a   Zhu, Yun Fei ^a   Guo, Zhiqiang ^a   Moorjani, Manisha ^a   Acevedo, Oscar ^a   Carter, Lee ^a   Sullivan, Susan K ^a   Xie, Qiu ^a   Fisher, Andrew ^a   Struthers, R Scott ^a   Saunders, John ^a   Chen, Chen ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 (THIAZOL 4 YL) 6 METHYLURACIL; 5 THIAZOLYL 6 METHYLURACIL; 5 THIENYL 6 METHYLURACIL; GONADORELIN ANTAGONIST; GONADORELIN RECEPTOR; N 1 (2,6 DIFLUOROBENZYL) 6 METHYLURACIL; THYMINE DERIVATIVE; UNCLASSIFIED DRUG; URACIL; URACIL DERIVATIVE;

ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; RECEPTOR BINDING; STRUCTURE ACTIVITY RELATION;

HUMANS; RECEPTORS, LHRH; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; THIOPHENES; URACIL;

EID: 4444368194     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.07.022     Document Type: Article

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39. Based on a docking study using a GnRH homology model obtained from the crystal structure of b-rhodopsin, we speculate that the C-5 substituent (of the uracil core) sits close to the extracellular surface of the receptor between TM domains 4 and 5. Unpublished results