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Volumn 21, Issue 7, 2011, Pages 1991-1996

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor

Author keywords

Antipsychotic; NK3 antagonist; Pyrazole

Indexed keywords

3 ARYL 5 ACYLPIPERAZINYL PYRAZOLE DERIVATIVE; GSK 183390A; N (ALPHA ETHYLBENZYL) 3 METHYL 2 PHENYL 4 QUINOLINECARBOXAMIDE; NEUROKININ 3 RECEPTOR; NEUROKININ 3 RECEPTOR ANTAGONIST; OSANETANT; PIPERAZINE DERIVATIVE; PYRAZOLE DERIVATIVE; TALNETANT; UNCLASSIFIED DRUG;

EID: 79952488963     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.033     Document Type: Article
Times cited : (18)

References (19)
  • 7
    • 0036194079 scopus 로고    scopus 로고
    • 2+] causes a conformational change in the aequorin protein thereby eliciting a quantifiable luminescent signal. This method is adapted to detect agonist, antagonist or allosteric modulators of receptor activity
    • 2+] causes a conformational change in the aequorin protein thereby eliciting a quantifiable luminescent signal. This method is adapted to detect agonist, antagonist or allosteric modulators of receptor activity.
    • (2002) J. Biomol. Screen. , vol.7 , pp. 57
    • Le Poul, E.1    Hisada, S.2    Mizuguchi, Y.3    Dupriez, V.J.4    Burgeon, E.5    Detheux, M.6
  • 10
    • 79952490349 scopus 로고    scopus 로고
    • note
    • Given the good agreement between the radioligand binding and aequorin functional assays, the latter set of results will be principally used in foregoing SAR discussions.
  • 12
    • 79952487514 scopus 로고    scopus 로고
    • No appreciable solubility difference between 4 and 5 was detectable at pH 7, although at pH 5 benzylpiperazine analog 5 was decidedly more soluble
    • No appreciable solubility difference between 4 and 5 was detectable at pH 7, although at pH 5 benzylpiperazine analog 5 was decidedly more soluble.
  • 13
    • 79952487806 scopus 로고    scopus 로고
    • C log P values cited herein are calculated using ChemBioDraw (CambridgeSoft, v.12)
    • C log P values cited herein are calculated using ChemBioDraw (CambridgeSoft, v.12).
  • 19
    • 55549146766 scopus 로고    scopus 로고
    • For example: Compound 7 (GSK183390A) in the cited reference is depicted below and has been reported to have a clean 7-day toxicology profile in rats with no safety issues. (Chemical Equation Presented)
    • For example: Martres, P.; Faucher, N.; Laroze, A.; Pineau, O.; Fouchet, M.-H.; Potvain, F.; Grillot, D.; Beneton, V. Bioorg. Med. Chem. Lett. 2008, 18, 6251. Compound 7 (GSK183390A) in the cited reference is depicted below and has been reported to have a clean 7-day toxicology profile in rats with no safety issues. (Chemical Equation Presented)
    • (2008) Bioorg. Med. Chem. Lett. , vol.18 , pp. 6251
    • Martres, P.1    Faucher, N.2    Laroze, A.3    Pineau, O.4    Fouchet, M.-H.5    Potvain, F.6    Grillot, D.7    Beneton, V.8


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.