Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. Part 1: study of the structural features for BZR recognition

S Selleri; F Bruni; C Costagli; A Costanzo; G Guerrini; G Ciciani; B Costa; C Martini

doi:10.1016/s0968-0896(99)00232-1

Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. Part 1: study of the structural features for BZR recognition

Bioorg Med Chem. 1999 Dec;7(12):2705-11. doi: 10.1016/s0968-0896(99)00232-1.

Authors

S Selleri¹, F Bruni, C Costagli, A Costanzo, G Guerrini, G Ciciani, B Costa, C Martini

Affiliation

¹ Department of Pharmaceutical Sciences, University of Firenze, Florence, Italy. [email protected]

PMID: 10658575
DOI: 10.1016/s0968-0896(99)00232-1

Abstract

Examination of the pharmacophoric points of the pyrazolo[1,5-a]pyrimidine derivatives, ligands for BZR, previously published led us to the design of a novel class of 3,6-diaryl-4,7-dihydro-pyrazolo[1,5-a]pyrimidin-7-ones and to determine the groups involved in the BZR recognition.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Affinity Labels / chemical synthesis*
Affinity Labels / chemistry
Affinity Labels / metabolism*
Animals
Binding Sites
Drug Design
GABA-A Receptor Antagonists
In Vitro Techniques
Kinetics
Ligands
Models, Molecular
Molecular Conformation
Pyrazoles / chemical synthesis*
Pyrazoles / chemistry
Pyrazoles / metabolism*
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / metabolism*
Receptors, GABA-A / metabolism*
Structure-Activity Relationship

Substances

Affinity Labels
GABA-A Receptor Antagonists
Ligands
Pyrazoles
Pyrimidines
Receptors, GABA-A