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Volumn 4, Issue 21, 1994, Pages 2545-2550

Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirements

Author keywords

[No Author keywords available]

Indexed keywords

2 BENZHYDRYL 3 (2 METHOXYBENZYLAMINO) 1 AZABICYCLO[2.2.2]OCTANE; 3 [3,5 BIS(TRIFLUOROMETHYL)BENZYLOXY] 2 PHENYLPIPERIDINE; 3 [3,5 BIS(TRIFLUOROMETHYL)BENZYLOXY] 2 PHENYLPYRROLIDINE; ETHER DERIVATIVE; NEUROKININ 1 RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; PIPERIDINE DERIVATIVE; PYRROLIDINE DERIVATIVE; SUBSTANCE P; UNCLASSIFIED DRUG;

EID: 0027997928     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(01)80280-8     Document Type: Article
Times cited : (146)

References (17)
  • 14
    • 84908842932 scopus 로고    scopus 로고
    • max = 2.13 with a weighting scheme of [[Truncated]]
  • 15
    • 84908842931 scopus 로고    scopus 로고
    • 4, pH 7, 0.9mL/min Retention times: (+)-(9) - 12.5min, (−)-(9) - 17.6min.
  • 16
    • 0037768402 scopus 로고
    • 4 reduction. For a review of the chemistry of N-protected α-amino aldehydes see:
    • (1989) Chem Rev. , vol.89 , pp. 149
    • Jurczak1    Golebiowski2
  • 17
    • 84908842930 scopus 로고    scopus 로고
    • Overlay of the minimum energy conformations of the piperidine (2) (dark lines) and pyrrolidine (15) (light lines). The minimum energy conformations were generated using Grid search within SYBYL, all conformations within 10kcal of the global minima were then minimised using the Tripos force field parameters. The minimum energy conformations were then superimposed using the basic nitrogen, the ether oxygen and the aryl centroids. It is interesting to note that although there is excellent overlap of the phenyl and benzyl rings and the ether oxygen in the two series, there is a significant deviation in the directionality of the substituent on nitrogen. The effects of nitrogen substitution will be reported in due course.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.