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Volumn 16, Issue 11, 2006, Pages 3043-3048

Identification of an indole series of prostaglandin D2 receptor antagonists

Author keywords

DP receptor antagonist; Indole; PGD2; Prostaglandin D2

Indexed keywords

CYCLIC AMP; INDOLE DERIVATIVE; PROSTAGLANDIN D2; PROSTAGLANDIN D2 RECEPTOR ANTAGONIST; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; DRUG DERIVATIVE; IMMUNOGLOBULIN RECEPTOR; INDOLE; PROSTAGLANDIN D2 RECEPTOR; PROSTAGLANDIN RECEPTOR; SAFROLE; SULFOXIDE;

EID: 33746640958     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.02.062     Document Type: Article
Times cited : (22)

References (18)
  • 11
    • 33748253031 scopus 로고    scopus 로고
    • note
    • The absolute stereochemistry of the acetic acid side chain present in 35 and 36 was established by X-ray analysis of the following acid which was obtained from ester hydrolysis and resolution of 45: {A figure is presented} Crystallographic data (excluding structure factors) for the structures in this paper have been deposited with the Cambridge Crystallographic Data Centre as supplementary publication numbers CCDC 297169 (17) and CCDC 297363 (48). Copies of the data can be obtained, free of charge, on application to CCDC, 12 Union Road, Cambridge, CB2 1EZ, UK [e-mail: deposit@ccdc.cam.ac.uk].
  • 12
    • 33748273075 scopus 로고    scopus 로고
    • note
    • 125I]cAMP scintillation proximity assay (SPA) (RPA556, Amersham).
  • 13
    • 33748283926 scopus 로고    scopus 로고
    • note
    • TP functional assay was performed as follows: Test compounds were assessed for their ability to inhibit platelet aggregation in human PRP using aggregometry. Two hundred and fifty microliters of PRP was stirred in a cuvette at 37 °C for 3 min. Twenty-five microliters of the test compound diluted in buffer [0.9% (w/v) or 0.15 M NaCl containing 0.25% (w/v) BSA] or vehicle (buffer), as control was added to 250 μL stirring platelets for a 10 min preincubation period. Twenty microliters of agonist (1.36 μM U46619, final concentration) was then added to the stirring PRP mixture to induce aggregation and the incubation continued for five additional minutes. Maximum aggregation was determined at approximately 5 min. The maximum extent of aggregation achieved in the presence of U46619 was set to 100%.
  • 14
    • 33748250442 scopus 로고    scopus 로고
    • note
    • All new compounds provided satisfactory spectral data along with mass spectral and/or elemental analysis.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.