IN283358: Synthesis of trycyclic thiazolo[4,3-e] pyrimidine fused 1,2,4-triazole/1,3-imidazole derivatives
Abstract
Novel thiazolotriazolopyrimidine (25-36) and thiazoloimidazolo pyrimidine (39-44) designed as potential adenosine A2A receptor (A2AR) antagonists were synthesized. Molecular docking studies revealed that all compounds (25-36) and (39-44) exhibited strong interaction with A2AR. The strong interaction of the compounds (23-33) with A2AR in silico was confirmed by their high binding affinity with human A2AR stably expressed in HEK293 cells using radioligand binding assay. The compounds 25-36 demonstrated substantial binding affinity and selectivity for A2AR as compared to SCH58261, a standard A2AR antagonist. A decline in A2AR-coupled release of endogenous cAMP in treated HEK293 cells demonstrated in vitro A2AR antagonist potential of the compounds 25-36. Attenuation in haloperidol-induced motor impairments (catalepsy and akinesia) in Swiss albino male mice pre-treated with compounds 25-36 further support their role in the alleviation of PD symptoms.
Filing Date:
31-05-2010
Issue Date:
17-05-2017
Applicant:
CSIR(SCH)
Patent No:
IN283358
Application No:
1240DEL2010
Inventor(s):
Pratibha Mehta Luthra; Chandra Bhushan Mishra
IPC Classification:
C07D
Country:
India
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