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Volumn 18, Issue 14, 2008, Pages 4199-4203

Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists

Author keywords

A2A; A2A antagonist; A2A receptor; A2A receptor antagonist; Adenosine; Parkinson's Disease; SCH 58261

Indexed keywords

5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; 5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE DERIVATIVE; ADENOSINE A2A RECEPTOR ANTAGONIST; SCH 85261;

EID: 47149111966     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.074     Document Type: Article
Times cited : (20)

References (21)
  • 4
    • 36148955045 scopus 로고    scopus 로고
    • 2A Receptors in Parkinson's Disease and Other CNS Disorders.
    • 2A Receptors in Parkinson's Disease and Other CNS Disorders.
  • 8
    • 47149106072 scopus 로고    scopus 로고
    • 1 is necessary to avoid cardiac side effects.
    • 1 is necessary to avoid cardiac side effects.
  • 12
    • 47149118177 scopus 로고    scopus 로고
    • Also see Ref. 4.
    • Also see Ref. 4.
  • 15
    • 47149096405 scopus 로고    scopus 로고
    • note
    • All of the final compounds in this publication were synthesized by the mesylate alkylation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine 4 shown in Scheme 1. A mixture of 7- and 8-alkylated products was formed. The N-8 alkylated analogs were generally inactive.
  • 18
    • 47149114013 scopus 로고    scopus 로고
    • Inhibition of haloperidol-induced catalepsy is an in vivo assay used to evaluate Parkinson's drugs (>30% inhibition is considered to be active in this assay).
    • Inhibition of haloperidol-induced catalepsy is an in vivo assay used to evaluate Parkinson's drugs (>30% inhibition is considered to be active in this assay).
  • 21
    • 0035289779 scopus 로고    scopus 로고
    • The nephelometric (light scattering) method was used to determine the kinetic solubility of compounds. The test compound (1.0 mg) was dissolved in DMSO at 25 mM. A serial dilution into DMSO was performed and 3 μl of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of material that did not scatter light.
    • The nephelometric (light scattering) method was used to determine the kinetic solubility of compounds. The test compound (1.0 mg) was dissolved in DMSO at 25 mM. A serial dilution into DMSO was performed and 3 μl of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of material that did not scatter light. Lipinski C.A., Lombardo F., Dominy B.W., and Feeney P.J. Adv. Drug Deliv. Rev. 46 (2001) 3
    • (2001) Adv. Drug Deliv. Rev. , vol.46 , pp. 3
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.