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Volumn 20, Issue 10, 2010, Pages 3161-3164

Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor

Author keywords

Lead optimisation; P2X7; P2X7 antagonist

Indexed keywords

(1H PYRAZOL 4 YL)ACETAMIDE; 2 (3,5 DIMETHYL 1 PHENYL 1H PYRAZOL 4 YL)ACETAMIDE DERIVATIVE; ANTIINFLAMMATORY AGENT; PURINERGIC P2X7 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

EID: 77952105608     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.096     Document Type: Article
Times cited : (26)

References (32)
  • 21
    • 77952108399 scopus 로고    scopus 로고
    • ClinicalTrial.gov Identifier: NCT00628095.
    • ClinicalTrial.gov Identifier: NCT00628095.
  • 25
    • 77952109618 scopus 로고    scopus 로고
    • note
    • max values of 100%. Full details of the assay protocol can be found in patent application WO 2007 141267 A1.
  • 26
    • 77952109415 scopus 로고    scopus 로고
    • note
    • Compound 12 was prepared from commercial 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylic acid. Compound 13 was prepared from commercial [(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methyl]amine. Compound 14 was prepared from commercial 3,5-dimethyl-1-phenyl-1H-pyrazol-4-amine. Compound 15 was prepared via cyclodehydration of an intermediate hydrazide.
  • 27
    • 77952105642 scopus 로고    scopus 로고
    • note
    • The preparation of compounds 16 and 17 is described in patent application WO 2008 138876 A1. Compound 18 was prepared via alkylation of commercial 3-phenyl-2,4-imidazolidinedione. Compounds 19-21 were prepared from commercially available acetic acids.
  • 28
    • 77952103562 scopus 로고    scopus 로고
    • note
    • The synthesis and optimisation of compound 22 will be described in a forthcoming publication.
  • 29
    • 77952107173 scopus 로고    scopus 로고
    • note
    • metasite v3.0, developed by Molecular Discovery, predicts metabolic transformations related to cytochrome-mediated reactions in phase I metabolism.
  • 31
    • 77952105715 scopus 로고    scopus 로고
    • note
    • Calculated log D values were obtained using ACD Labs software v8.0.
  • 32
    • 77952106670 scopus 로고    scopus 로고
    • note
    • All experiments were performed in accordance with the United Kingdom Animals (Scientific Procedures) Act, 1986 under Project Licence as well as under the review and approval of the GlaxoSmithKline Procedures Review Panel. GlaxoSmithKline safety regulations were adhered to at all times.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.