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Volumn 18, Issue 14, 2008, Pages 4204-4209

Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as 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;

EID: 47149102874     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.069     Document Type: Article
Times cited : (20)

References (31)
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    • 1 is necessary to avoid cardiac side-effects.
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    • note
    • All compounds in this publication were isolated and tested in free base form.
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    • note
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    • 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 Delivery Rev. 46 (2001) 3
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    • Tetrahydroisoquinolines 2i, 2j, and 10 were synthesized as described in:. Sall D.J., and Grunewald G.L. J. Med. Chem. 30 (1987) 2208 Intermediates 2e-2g are commercially available from Acros Organics, Morris Plains, NJ
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    • The synthesis of intermediate 2x is described in: Ashton, W. T.; Caldwell, C. G.; Duffy, J. L.; Mathvink, R. J.; Wang, L.; Weber, A. E. WO Patent 2004069162, 2004.
    • The synthesis of intermediate 2x is described in: Ashton, W. T.; Caldwell, C. G.; Duffy, J. L.; Mathvink, R. J.; Wang, L.; Weber, A. E. WO Patent 2004069162, 2004.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.