Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of [beta-(Aroylamino)ethyl]piperazines and -piperidines an...
Basic Information
ID: ALA1125003
Journal: J Med Chem
Title: Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of [beta-(Aroylamino)ethyl]piperazines and -piperidines and [2-[(Arylamino)carbonyl]ethyl]piperazines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines. A new class of potent H1 antagonists.
Authors: Saxena M, Agarwal SK, Patnaik GK, Saxena AK.
Abstract: Some [beta-(Aroylamino)ethyl]piperazines and -piperidines and [2-[(Arylamino)carbonyl]ethyl]piperazines, -piperidines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines have been synthesized and their H1-antagonistic activity studied in isolated guinea pig ileum. Quantitative structure-activity relationship analysis indicates that the hydrophobicity of the side chain of these compounds plays a major role in their activity while steric and electronic factors are of secondary importance. All these compounds act on a common receptor and appear to interact similarly with the receptor.
CiteXplore: 1977909
DOI: 10.1021/jm00173a011
Patent ID: ┄