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 …

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 …

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 …

Synthesis of New Pyrazolo[1,5‐a]pyrimidines as Potential Antibacterial Agents: In Vitro and In Silico Study

AEM Mekky, SMH Sanad - ChemistrySelect, 2023 - Wiley Online Library
In this study, we aimed to establish two new series of pyrazolo [1, 5‐a] pyrimidines starting
from 1H‐pyrazole‐3, 5‐diamine. The first series was prepared by reacting 1H‐pyrazole‐3, 5 …

Three-component regioselective synthesis and antibacterial evaluation of new arene-linked bis(pyrazolo[1,5-a]pyrimidine) hybrids

SMH Sanad, AEM Mekky - Synthetic Communications, 2023 - Taylor & Francis
In the current study, a three-component protocol was adopted to efficiently synthesize
butane-linked bis (pyrazolo [1, 5-a] pyrimidines) 1 attached to arene units in 74–81% yields …

Synthesis and pharmacological assessment of derivatives of isoxazolo [4, 5-d] pyrimidine

E Wagner, L Becan, E Nowakowska - Bioorganic & medicinal chemistry, 2004 - Elsevier
A series of new 5-alkyl and 5-arylisoxazolo [4, 5-d] pyrimidinones (5a–g, 6–8) were
prepared from 4-amino-3-oxo-isoxazolidine-5-carboxylic acid amide. Some of the aryl …

A Novel Selective GABAA α1 Receptor Agonist Displaying Sedative and Anxiolytic-like Properties in Rodents

S Selleri, F Bruni, C Costagli, A Costanzo… - Journal of medicinal …, 2005 - ACS Publications
In our pursuit to identify selective ligands for Bz/GABAA receptor subtypes, a novel pyrazolo
[1, 5-a] pyrimidine derivative (4), the azaisostere of zolpidem, was synthesized and …

GABAA/Bz receptor subtypes as targets for selective drugs

F Da Settimo, S Taliani, ML Trincavelli… - Current medicinal …, 2007 - ingentaconnect.com
The γ-aminobutyric acid type A (GABAA) receptors are the major inhibitory neuronal
receptors in the mammalian brain. Their activation by GABA opens the intrinsic ion channel …

Development of pyrazolo[1,5-a]pyrimidine-based antibacterial agents

AEM Mekky, NAS Taha, NG Mohammed… - Synthetic …, 2023 - Taylor & Francis
In the present study, a facile method was adopted to efficiently prepare new pyrazolo [1, 5-a]
pyrimidin-2-amines linked to arene units in good to excellent yields. A mixture of …

Allosteric GABAA Receptor Modulators—A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

BA Vega Alanis, MT Iorio, LL Silva, K Bampali, M Ernst… - Molecules, 2020 - mdpi.com
GABAA receptor modulators are structurally almost as diverse as their target protein. A
plethora of heterocyclic scaffolds has been described as modulating this extremely important …