Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers

[Display omitted] Uracil derivatives were designed and synthesized to avoid atropisomers observed in the 6-methyluracils as antagonists of the human GnRH receptor. Optimization at the 1- and 5-positions of the uracil resulted in potent compounds such as 24 (Ki=0.45nM).

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-05, Vol.15 (10), p.2519-2522
Hauptverfasser:	Guo, Zhiqiang, Chen, Yongsheng, Huang, Charles Q., Gross, Timothy D., Pontillo, Joseph, Rowbottom, Martin W., Saunders, John, Struthers, Scott, Tucci, Fabio C., Xie, Qiu, Wade, Warren, Zhu, Yun-Fei, Wu, Dongpei, Chen, Chen
Format:	Artikel
Sprache:	eng
Schlagworte:	antagonist Atropisomer Biological and medical sciences GnRH Hormones. Endocrine system Humans Isomerism Medical sciences Miscellaneous Molecular Structure Pharmacology. Drug treatments Receptors, LHRH - antagonists & inhibitors Uracil Uracil - chemistry Uracil - pharmacology X-Ray Diffraction
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Beschreibung
Zusammenfassung:	[Display omitted] Uracil derivatives were designed and synthesized to avoid atropisomers observed in the 6-methyluracils as antagonists of the human GnRH receptor. Optimization at the 1- and 5-positions of the uracil resulted in potent compounds such as 24 (Ki=0.45nM).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.03.057