International Union of Basic and Clinical Pharmacology. CVI: GABAA receptor subtype-and function-selective ligands: key issues in translation to humans

W Sieghart, MM Savić - Pharmacological reviews, 2018 - ASPET
GABAA receptors are the major inhibitory transmitter receptors in the brain. They are ligand-
gated chloride channels and the site of action of benzodiazepines, barbiturates, neuroactive …

Tests of unconditioned anxiety—Pitfalls and disappointments

A Ennaceur - Physiology & behavior, 2014 - Elsevier
The plus-maze, the light–dark box and the open-field are the main current tests of
unconditioned anxiety for mice and rats. Despite their disappointing achievements, they …

The 18 kDa translocator protein, microglia and neuroinflammation

GJ Liu, RJ Middleton, CR Hatty, WWY Kam… - Brain …, 2014 - Wiley Online Library
The 18 kDa translocator protein (TSPO), previously known as the peripheral
benzodiazepine receptor, is expressed in the injured brain. It has become known as an …

An insight on synthetic and medicinal aspects of pyrazolo [1, 5-a] pyrimidine scaffold

S Cherukupalli, R Karpoormath… - European journal of …, 2017 - Elsevier
Abstract Pyrazolo [1, 5-a] pyrimidine scaffold is one of the privileged hetrocycles in drug
discovery. Its application as a buliding block for developing drug-like candidates has …

Tuberculosis: an overview of the immunogenic response, disease progression, and medicinal chemistry efforts in the last decade toward the development of potential …

A Sharma, M De Rosa, N Singla, G Singh… - Journal of medicinal …, 2021 - ACS Publications
Tuberculosis (TB) is a slow growing, potentially debilitating disease that has plagued
humanity for centuries and has claimed numerous lives across the globe. Concerted efforts …

Antibiofilm and Anti-Quorum-Sensing Activities of Novel Pyrazole and Pyrazolo[1,5-a]pyrimidine Derivatives as Carbonic Anhydrase I and II Inhibitors: Design …

A Ragab, SA Fouad, YA Ammar, DS Aboul-Magd… - Antibiotics, 2023 - mdpi.com
Nowadays, searching for new anti-infective agents with diverse mechanisms of action has
become necessary. In this study, 16 pyrazole and pyrazolo [1, 5-a] pyrimidine derivatives …

A comprehensive review of N-heterocycles as cytotoxic agents

D Kumar, S Kumar Jain - Current Medicinal Chemistry, 2016 - ingentaconnect.com
Scientific community is striving to understand the role of heterocycles and fused
heterocycles in drug discovery programme due to its impact on multi-drug resistance (MDR) …

Structure-based design, synthesis and biological evaluation of a newer series of pyrazolo [1, 5-a] pyrimidine analogues as potential anti-tubercular agents

P Modi, S Patel, M Chhabria - Bioorganic Chemistry, 2019 - Elsevier
In-depth study of structure-based drug designing can provide vital leads for the development
of novel, clinically active molecules. In this present study, twenty six novel pyrazolo [1, 5-a] …

Design, synthesis, anticancer evaluation, molecular docking and cell cycle analysis of 3-methyl-4, 7-dihydropyrazolo [1, 5-a] pyrimidine derivatives as potent histone …

NH Metwally, MS Mohamed, EA Ragb - Bioorganic chemistry, 2019 - Elsevier
A novel series of pyrazolo [1, 5-a] pyrimidines were synthesized and proved by their spectral
and elemental analysis, some elected of the newly synthesized compounds were examined …

Insights into the medicinal chemistry of heterocycles integrated with a pyrazolo [1, 5-a] pyrimidine scaffold

MM Hammouda, HE Gaffer, KM Elattar - RSC Medicinal Chemistry, 2022 - pubs.rsc.org
Pyrazolo [1, 5-a] pyrimidines are the dominant motif of many drugs; for instance, zaleplon
and indiplon are sedative agents and ocinaplon was identified as an anxiolytic agent. The …