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Volumn 16, Issue 19, 2006, Pages 5217-5221

From arylureas to biarylamides to aminoquinazolines: Discovery of a novel, potent TRPV1 antagonist

Author keywords

Antagonist; Bioisostere; Pain; Quinazoline; TRPV1; Ureas; VR1

Indexed keywords

AROMATIC AMIDE; QUINAZOLINE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; UREA DERIVATIVE; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 1 ANTAGONIST;

EID: 33747375663     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.07.010     Document Type: Article
Times cited : (33)

References (15)
  • 4
    • 33747346021 scopus 로고    scopus 로고
    • Hutchison, A.; DeSimone, R. W.; Hodgetts, K.; Krause, J. E.; White, G. PCT WO 02/08221.
  • 5
    • 33747374154 scopus 로고    scopus 로고
    • Bakthavatchalam, R.; Hutchison, A.; DeSimone, R. W.; Hodgetts, K.; Krause, J. E.; White, G. U.S. Patent 6,723,730, 2004.
  • 11
    • 19944433048 scopus 로고    scopus 로고
    • The same bioisosteric replacement was recently disclosed by
    • The same bioisosteric replacement was recently disclosed by. Park H.-G., et al. Bioorg. Med. Chem. Lett. 15 (2005) 631
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 631
    • Park, H.-G.1
  • 12
    • 33747360486 scopus 로고    scopus 로고
    • note
    • High throughput solubility (HTSol) was assessed by diluting DMSO stock solutions of the test article into pH 7.4 buffer and shaking for 4 h at room temperature. Solutions are then filtered and analyzed (HPLC/MS).
  • 13
    • 33747370748 scopus 로고    scopus 로고
    • note
    • Energy minimizations were carried out using Maestro 7.0, Schrödinger, .
  • 14
    • 33747349818 scopus 로고    scopus 로고
    • note
    • These assays conveniently provided information regarding species selectivity (rat vs human) as well as the ability of compounds to block different modes of receptor activation (capsaicin or low pH). Data generated in human VR1 low pH or rat VR1 capsaicin assays (data not shown) did not yield an additional understanding of compound pharmacology.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.