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Volumn 16, Issue 18, 2006, Pages 4723-4727

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists

Author keywords

MCH; MCH antagonist; MCH R1; MCH R1 antagonist; Melanin concentrating hormone

Indexed keywords

GW 803430; HORMONE ANTAGONIST; MELANIN CONCENTRATING HORMONE RECEPTOR 1 ANTAGONIST; PYRIMIDINONE DERIVATIVE; SIBUTRAMINE; UNCLASSIFIED DRUG;

EID: 33746820210     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.07.008     Document Type: Article
Times cited : (49)

References (22)
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    • Several patents describing MCH R1 patents have been published. For reviews on the subject, please see:
    • Several patents describing MCH R1 patents have been published. For reviews on the subject, please see:. Dyke H.J., and Ray N.C. Expert Opin. Ther. Patents 15 (2005) 1303
    • (2005) Expert Opin. Ther. Patents , vol.15 , pp. 1303
    • Dyke, H.J.1    Ray, N.C.2
  • 9
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    • Witty, D. R.; Bateson, J.; Hervieu, G. J.; Jeffrey, P.; Johnson, C. N.; Muir, A. I.; O'Hanlon, P. J.; Stemp, G.; Stevens, A. J.; Thewlis, K.; Winborn, K. Y. Bioorg. Med. Chem. Lett., in press.
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    • Witty, D. R.; Bateson, J.; Hervieu, G. J.; Al-Barazanji, K.; Jeffrey, P.; Hamprecht, D.; Haynes, A.; Johnson, C. N.; Muir, A. I.; O'Hanlon, P. J.; Stemp, G.; Stevens, A. J.; Thewlis, K.; Winborn, K. Y. Bioorg. Med. Chem. Lett., in press.
  • 11
    • 33746831323 scopus 로고
    • Prepared through Jones oxidation of the corresponding aldehyde found in
    • Prepared through Jones oxidation of the corresponding aldehyde found in. Sone C., and Matsuki Y. Bull. Chem. Soc. Japan 36 (1963) 618
    • (1963) Bull. Chem. Soc. Japan , vol.36 , pp. 618
    • Sone, C.1    Matsuki, Y.2
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    • note
    • 80 thrombin response in the host cells. All compounds were assayed with n ≥ 4.
  • 15
    • 33746854037 scopus 로고    scopus 로고
    • note
    • Molecular models of the structures in Figure 1 were created using the Maestro Version 7.5 interface from Schrödinger, LLC. In Maestro, conformation searches and energy minimizations were carried out with the MacroModel application using the OPLS-2005 force field. The atoms of the pyrimidinone ring were superimposed to demonstrate the variation in the position of the 4-chlorophenyl substituent on the fused heterocyclic ring.
  • 18
    • 33746839823 scopus 로고    scopus 로고
    • Tavares, F. X.; Al-Barazanji, K. A.; Bigham, E. C.; Bishop, M. J.; Britt, C. S.; Carlton, D. L.; Feldman, P. L.; Goetz, A. S.; Grizzle, M. K.; Guo, Y. C.; Handlon, A. L.; Hertzog, D. L.; Ignar, D. M.; Lang, D. G.; Ott, R. J.; Peat, A. J.; Zhou, H-Q. J. Med. Chem., in press.
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    • Handlon, A. L.; Al-Barazanji, K.; Barvian, K. K.; Bigham, E. C.; Carlton, D. L.; Carpenter, A. J.; Cooper, J. P.; Daniels, A. J.; Garrison, D. T.; Goetz, A. S.; Green, G. M.; Grizzle, M. K.; Guo, Y. C.; Hertzog, D. L.; Hyman, C. E.; Ignar, D. M.; Peckham, G. E.; Speake, J. D.; Britt, C.; Swain, W. R. Abstracts of Papers. In 228th National Meeting of the American Chemical Society; American Chemical Society: Washington, DC, 2004, p. 193.
  • 20
    • 33746835885 scopus 로고    scopus 로고
    • note
    • The maleate salts of compound 7c and related analogs were often made to provide easily handled solids that were not hygroscopic.
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    • note
    • 1-({[4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2- yl)phenyl]oxy}acetyl)pyrrolidine has the following structure:{A figure is presented}.
  • 22
    • 33746788290 scopus 로고    scopus 로고
    • The weight loss achieved with GW803430 (compound 7c) was due entirely to fat mass loss as determined by dual-energy X-ray absorptiometry (DEXA) scanning. See Al-Barazanji, K.; Grizzle, M.; Britt, C.; Lancaster, M.; Daniels, A.; Ignar, D.; Cooper, J; Hertzog, D. Obesity Res. 2004, 12, 56-OR.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.