EMAIL THIS PAGE TO A FRIEND

Journal of medicinal chemistry

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.


PMID 17228859

Abstract

A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

634786
(S)-(+)-N-Boc-3-pyrrolidinol, 97%
C9H17NO3
SML1116
PQ-10, ≥98% (HPLC)
C22H21N5O3