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Volumn 16, Issue 18, 2006, Pages 4872-4878

Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849

Author keywords

Antagonist; Anxiety; Benzotriazinone; Bicyclic heterocycle; Biphenylcarboxamide; Cyclisation; Feeding; MCH; MCH R1; Melanin concentrating hormone; Obesity; Quinazolinone; Stress; Thienopyrimidinone

Indexed keywords

HORMONE RECEPTOR BLOCKING AGENT; LIGAND; MELANIN CONCENTRATING HORMONE RECEPTOR 1; MELANIN CONCENTRATING HORMONE RECEPTOR ANTAGONIST; PHTHALIMIDE DERIVATIVE; PYRIMIDINONE DERIVATIVE; QUINAZOLINONE DERIVATIVE; SB 568849; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 33746837233     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.06.061     Document Type: Article
Times cited : (25)

References (13)
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    • Witty, D. R.; Bateson, J. H.; Hervieu, G. J.; Jeffrey, P.; Johnson, C. J.; Muir, A. I.; O'Hanlon, P. J.; Stemp, G.; Stevens, A. J.; Thewlis, K. M.; Wilson S.; Winborn, K. Y. Bioorg. Med. Chem. Lett., preceeding paper, doi:10.1016/j.bmcl.2006.06.056.
  • 9
    • 33746814731 scopus 로고    scopus 로고
    • Armstrong, S. A.; Hamprecht, D. W.; Jones, M.; Witty, D. R.; Al-Barazanji, K. A.; Tadayyon, M. WO 2003033480; Chem. Abstr. 2003 138, 338173.
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    • Overman, L.E.1    Sugai, S.2
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    • Compound 5: Halazy, S.; Perez, M.; Briley, M.; Pauwels, P. WO 9514004; Chem. Abstr. 1995 123, 340183.
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    • note
    • i values reported are given for an n of ≥3 and a standard error of the mean of <0.25.
  • 13
    • 33746793071 scopus 로고    scopus 로고
    • note
    • Intrinsic clearance (CLi) assay: a liver microsomal incubation of known volume (V) at an initial compound concentration of 0.5 μM with a microsomal protein concentration of 0.5 mg/mL is carried out to characterise the compound loss in the form of a concentration-time profile. The first-order elimination rate constant (K) is determined from the profile and CLi is then calculated using the relationship CLi = KV, scaled appropriately and reported in units of milliliters per minute per gram liver.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.