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Volumn 17, Issue 15, 2007, Pages 4232-4241

Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists

Author keywords

MCH; MCH R1 antagonists; Melanin concentrating hormone receptor; Obesity

Indexed keywords

2 AMINOQUINOLINE; CYCLOHEXANE; CYCLOPENTANE; DIAMINE DERIVATIVE; HORMONE RECEPTOR BLOCKING AGENT; MELANIN; THIOPHENE DERIVATIVE;

EID: 34447096407     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.05.034     Document Type: Article
Times cited : (22)

References (31)
  • 12
    • 34447108618 scopus 로고    scopus 로고
    • Handlon, A. L.; Al-Barazanji, K. A.; Barvian, K. K.; Bighan, E. C.; Carlton, D. L.; Carpenter, A. J.; Cooper, J. P.; Daniels, A. J.; Garrison, D. T.; Goetz, A. S., et al. 228th American Chemical Society National Meeting, Philadelphia, PA, USA, 2004: MEDI-193.
  • 13
    • 34447096751 scopus 로고    scopus 로고
    • Iyengar, R.; Souers, A. J.; Lynch, J. K.; Judd, A. S.; Gao, J.; Freeman, J. C.; Mulhern, M.; Vasudevan, A.; Wodka, D.; Blackburn, C., et al. 230th American Chemical Society National Meeting, Washington, DC, USA, 2005: MEDI-086.
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    • 34447097607 scopus 로고    scopus 로고
    • Giordanetto, F.; Lindberg, J.; Karlsson, O.; Inghardt, T. Abstract of Papers, 232nd National Meeting of the American Chemical Society, San Francisco, CA, 2006, COMP-410.
  • 23
    • 34447100630 scopus 로고    scopus 로고
    • note
    • 19 was employed to identify central linkers that satisfied the three pharmacophoric features described (N+, Hy1, and Hy2) within a root mean square deviation of 0.75 Å.
  • 25
    • 34447103549 scopus 로고    scopus 로고
    • The preparation of representative compounds is described in: Ray, A. K.; Sigfridsson, E. M.; Linusson, A.; Stina, M.; Sandberg, P. M.; Inghardt, T.; Svensson, A. M.; Brickmann, K. WO2004/004726 (compound 9), and in: Evertsson, E.; Inghardt, T.; Lindberg, J.; Linusson, A.; Giordanetto, F. WO2005/066132 (compounds 13, 15, 23, 29, 31, 38, 41, 43, 49-55).
  • 27
    • 34447101002 scopus 로고    scopus 로고
    • note
    • A variety of structural descriptors, including log D and aqueous solubility predictions, served to profile and filter the chemical library. These were calculated using in-house developed models implemented in Pipeline Pilot version. 4.5, SciTegic: San Diego, CA.
  • 28
    • 34447100447 scopus 로고    scopus 로고
    • note
    • The preparation of tert-butyl[(1S,3S)-3-aminocyclopentyl]carbamate is detailed in Evertsson, E.; Inghardt, T.; Lindberg, J.; Linusson, A.; Giordanetto, F. WO2005/066132.
  • 29
    • 34447107655 scopus 로고    scopus 로고
    • note
    • Female C57Bl/6J mice were given ad libitum access to calorie-dense 'cafeteria' diet (soft chocolate/cocoa-type pastry, chocolate, fatty cheese, and nougat) and standard lab chow for 8-10 weeks until a body weight of 45-50 g was achieved. Compounds to be tested were then administered perorally once daily for a period of 5-12 days, and the body weights of the mice monitored on a daily basis. During this period ad libitum access to calorie-dense 'cafeteria' diet and standard lab chow was maintained.
  • 30
    • 34447106212 scopus 로고    scopus 로고
    • Wan, H.; Rehngren, M.; Giordanetto, F.; Bergström, F.; Tunek, A., J. Med. Chem., submitted for publication.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.