Acetamide scanning around bicyclic thiazoles: SAR at the H₃ receptor.

Frédéric Denonne,Sylvain Célanire,Bernard Christophe,Sabine Defays,Christel Delaunoy,Marie-Laure Delporte,Eric Detrait,Véronique Durieu,Michel Gillard,Yves Lamberty,Geneviève Lorent,Jean-Marie Nicolas,Alain Vanbellinghen,Nathalie Van Houtvin,Laurent Provins

CHEMMEDCHEM（2011）

Cited 6|Views14

No score

Abstract

A surprisingly homogeneous SAR against the H3 receptor was revealed for positional acetamide isomers of bicyclic thiazoles fused to various cyclic amines. Pyrroline and azepine rings were used to probe the central position of the amide. In vitro ADMET parameters were measured, and the isomer with the best overall properties was assessed in vivo.

Translated text

Key words

bicyclic thiazoles,cognitive disorders,drug-like properties,histamine H-3 receptor,structure-activity relationships

AI Read Science

Must-Reading Tree

Example

Generate MRT to find the research sequence of this paper

Chat Paper

Summary is being generated by the instructions you defined