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Volumn 64, Issue 48, 2008, Pages 10802-10809

Design, chemical synthesis, and biological evaluation of novel triazolyl analogues of taranabant (MK-0364), a cannabinoid-1 receptor inverse agonist

Author keywords

Anti obesity; Evans asymmetric reaction; Hydride reduction; Taranabant

Indexed keywords

ALPHA BROMOKETONE; CANNABINOID 1 RECEPTOR; CANNABINOID 1 RECEPTOR ANTAGONIST; KETONE DERIVATIVE; TARANABANT; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 53449097224     PISSN: 00404020     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tet.2008.09.057     Document Type: Article
Times cited : (9)

References (27)
  • 17
    • 0000454231 scopus 로고    scopus 로고
    • Reider P.J. Chimia 51 (1997) 306-308
    • (1997) Chimia , vol.51 , pp. 306-308
    • Reider, P.J.1
  • 22
    • 53449096478 scopus 로고    scopus 로고
    • Coburn, C.; Espeseth, A. S.; Stachel, S. J.; Olsen, D. B.; Hazuda, D.; Holloway, M. K. WO2005/097767, 2005.
    • Coburn, C.; Espeseth, A. S.; Stachel, S. J.; Olsen, D. B.; Hazuda, D.; Holloway, M. K. WO2005/097767, 2005.
  • 25
    • 53449095719 scopus 로고    scopus 로고
    • note
    • 50=4.50 nM via in-house assay.
  • 26
    • 53449102062 scopus 로고    scopus 로고
    • note
    • Triazole is small and constitutes three nitrogens in the ring. Thus, by substituting H into a triazole, hydrophilicity of a molecule increases. Concurrent alteration of physicochemical properties including solubility was observed.
  • 27
    • 53449088508 scopus 로고    scopus 로고
    • note
    • Currently, Merck's taranabant is in Phase 3 clinical trial for the treatment of obesity in USA. Taranabant is not toxic per se, but people speculate that it might have potential problem to cause depression or anxiety in human beings when it is used in medium to high dose.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.