Alpha-Lipoic acid alleviates imidacloprid-induced neuro-behavioral deficits in rats Nrf2/HO-1 pathway.

Imidacloprid (IMI), a widely used pesticide in agriculture and a potential food contaminant, poses significant health concerns. This study sought to comprehensively evaluate its neurotoxic effects while investigating the potential protective role of alpha-lipoic acid (ALA), a naturally occurring dietary antioxidant renowned for its capacity to combat oxidative stress, support cardiovascular health, and maintain optimal nerve function. In this study, 28 rats were divided evenly into four groups and administered oral treatments of corn oil, IMI, IMI + ALA, and ALA, respectively.

Designing of 2,3-dihydrobenzofuran derivatives as inhibitors of PDE1B using pharmacophore screening, ensemble docking and molecular dynamics approach.

In recent years, the PDE1B enzyme has become a desirable drug target for the treatment of psychological and neurological disorders, particularly schizophrenia disorder, due to the expression of PDE1B in brain regions involved in volitional behaviour, learning and memory. Although several inhibitors of PDE1 have been identified using different methods, none of these inhibitors has reached the market yet. Thus, searching for novel PDE1B inhibitors is considered a major scientific challenge.

Evaluation of the acute oral toxicity and antipsychotic activity of a dual inhibitor of PDE1B and PDE10A in rat model of schizophrenia.

Phosphodiesterase 1B (PDE1B) and PDE10A are dual-specificity PDEs that hydrolyse both cyclic adenosine monophosphate and cyclic guanosine monophosphate, and are highly expressed in the striatum. Several reports have suggested that PDE10A inhibitors may present a promising approach for the treatment of positive symptoms of schizophrenia, whereas PDE1B inhibitors may present a novel mechanism to modulate cognitive deficits. Previously, we have reported a novel dual inhibitor of PDE1B and PDE10A, compound 2 [(3-fluorophenyl)(2-methyl-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)methanone] which has shown inhibitory activity for human recombinant PDE1B and PDE10A in vitro.

Computational Approaches in the Discovery and Development of Therapeutic and Prophylactic Agents for Viral Diseases.

Over the last two decades, computational technologies have played a crucial role in antiviral drug development. Whenever a virus spreads and becomes a threat to global health, it brings along the challenge of developing new therapeutics and prophylactics. Computational drug and vaccine discovery has evolved quickly over the years.