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Volumn 20, Issue 17, 2010, Pages 5080-5084

Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor

Author keywords

Antagonist; P2X7; Pain; SAR

Indexed keywords

(1H PYRAZOL 4 YL)ACETAMIDE DERIVATIVE; ACETAMIDE DERIVATIVE; AMIDE; CELECOXIB; GABAPENTIN; N [(2,4 DICHLOROPHENYL)METHYL] 2 (3,5 DIMETHYL 1H PYRAZOL 4 YL)ACETAMIDE; N ETHYL PRYROGLUTAMIDE DERIVATIVE; PURINERGIC P2X7 RECEPTOR; PYROGLUTAMIC ACID; UNCLASSIFIED DRUG;

EID: 77955653157     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.07.033     Document Type: Article
Times cited : (63)

References (34)
  • 12
    • 77955658669 scopus 로고    scopus 로고
    • ClinicalTrial.gov Identifier: NCT00628095
    • ClinicalTrial.gov Identifier: NCT00628095.
  • 15
    • 77955654780 scopus 로고    scopus 로고
    • max values of 100%. Full details of the assay protocol can be found in patent application WO 2007 141267 A1
    • max values of 100%. Full details of the assay protocol can be found in patent application WO 2007 141267 A1.
  • 17
    • 77955660511 scopus 로고    scopus 로고
    • Calculated log D values were obtained using ACD Labs software v8.0
    • Calculated log D values were obtained using ACD Labs software v8.0.
  • 24
    • 77955657829 scopus 로고    scopus 로고
    • 50 of greater than two- to threefold was considered to be significant and, depending on the baseline degree of inhibition, to potentially represent a developability risk
    • 50 of greater than two- to threefold was considered to be significant and, depending on the baseline degree of inhibition, to potentially represent a developability risk.
  • 25
    • 77955662349 scopus 로고    scopus 로고
    • The overlay was generated using the software FLO (Thistlesoft, Colebrook, CT06021, USA)
    • The overlay was generated using the software FLO (Thistlesoft, Colebrook, CT06021, USA).
  • 26
    • 77955653985 scopus 로고    scopus 로고
    • 24 and annotated with simple calculated properties (e.g., molecular weight, hydrogen-bond donor and acceptor counts)
    • 24 and annotated with simple calculated properties (e.g., molecular weight, hydrogen-bond donor and acceptor counts).
  • 30
    • 77955658734 scopus 로고    scopus 로고
    • Also see WO 2008/003697A1 for additional synthetic details
    • Also see WO 2008/003697A1 for additional synthetic details.
  • 31
    • 77955657047 scopus 로고    scopus 로고
    • http://www.cerep.fr.
  • 33
    • 77955659941 scopus 로고    scopus 로고
    • 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
    • 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.