Literature DB >> 15214774

3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.

Fabio C Tucci1, Yun-Fei Zhu, Zhiqiang Guo, Timothy D Gross, Patrick J Connors, Yinghong Gao, Martin W Rowbottom, R Scott Struthers, Greg J Reinhart, Qiu Xie, Ta Kung Chen, Haig Bozigian, Anne L Killam Bonneville, Andrew Fisher, Liping Jin, John Saunders, Chen Chen.   

Abstract

Uracils possessing N-3 side chains derived from various amino alcohols were designed and synthesized as potent human gonadotropin releasing hormone receptor antagonists. The compounds herein presented displayed superior metabolic stability than their predecessor molecules. Selected compounds from this series featured good oral bioavailability in mice and cynomolgus monkeys.

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Year:  2004        PMID: 15214774     DOI: 10.1021/jm049791w

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Design and synthesis of a novel tyrosine kinase inhibitor template.

Authors:  P Jake Slavish; Qin Jiang; Xiaoli Cui; Stephan W Morris; Thomas R Webb
Journal:  Bioorg Med Chem       Date:  2009-03-27       Impact factor: 3.641

2.  Nanorod-Shaped Basic Al2O3 Catalyzed N,N-Diformylation of Bisuracil Derivatives: A Greener "NOSE" Approach.

Authors:  Vijay K Das; Ashim J Thakur
Journal:  ISRN Org Chem       Date:  2013-06-26
  2 in total

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