Literature DB >> 15863308

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

Zhiqiang Guo1, Yongsheng Chen, Charles Q Huang, Timothy D Gross, Joseph Pontillo, Martin W Rowbottom, John Saunders, Scott Struthers, Fabio C Tucci, Qiu Xie, Warren Wade, Yun-Fei Zhu, Dongpei Wu, Chen Chen.   

Abstract

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=0.45 nM).

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Year:  2005        PMID: 15863308     DOI: 10.1016/j.bmcl.2005.03.057

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Synthesis and crystal structure of new heterocyles derived from saccharin and uracil carrying 1,2,4-oxadiazolylmethyl group.

Authors:  Yaşar Dürüst; Besra Özer; Benson M Kariuki; Benson M Cariuki
Journal:  Mol Divers       Date:  2015-03-10       Impact factor: 2.943

Review 2.  Recent Development of Non-Peptide GnRH Antagonists.

Authors:  Feng-Ling Tukun; Dag Erlend Olberg; Patrick J Riss; Ira Haraldsen; Anita Kaass; Jo Klaveness
Journal:  Molecules       Date:  2017-12-09       Impact factor: 4.411

  2 in total

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