BACKGROUND AND PURPOSE Midazolam is a short-acting benzodiazepine that is widely used as an i.v. sedative and anticonvulsant. Besides interacting with the benzodiazepine site associated with GABA(A) receptors, some benzodiazepines act as agonists of translocator protein (18 kDa) (TSPO) to enhance the synthesis of steroids, including neurosteroids with positive modulatory actions on GABA(A) rece...

considerable interest has been focused on the triazole structure, which has been known to possess a broad spectrum of biological activities such as antitumor, anti-inflammatory, antimicrobial, antiviral, and anticonvulsant activities. before this, several heterocyclic compounds containing triazole were synthesized that had shown considerable anticonvulsant activity. as part of our continuous re...

The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study. Characteristic features of all active compounds were rapid onset of action and long lasting effect. Structure-activity observations showed that the probability of obtaining compounds exerting anticonvulsant activity was much higher when at least one...

Artocarpus heterophyllus Lam. (Jackfruit) is traditionally used as anticonvulsant. The aqueous and methanol extracts of leaves of Artocarpus heterophyllus Lam. was evaluated for anticonvulsant activity by using Maximal electroshock (MES) and Strychnine induced convulsions models on Swiss albino mice. The methanol extracts of leaves of Artocarpus heterophyllus Lam. were found to be more signific...

In the present study, a series of 4-(4-substituted aryl) semicarbazones were synthesized from substituted anilines and subsequently evaluated for their anticonvulsant activities. The anticonvulsant activities were established by the anticonvulsant drug development (ADD) programme NIH, USA using experimental animal, adult male FCM mice (20-25 g) and adult Sprague-Dawley rats (100-150 g) and scre...

A series of aroxyacetamides and aroxyethylamines were prepared and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). Most of them exhibited anticonvulsant activity in the MES screen (mice, i.p.) in the doses up to 300 mg/kg b.w. The most active compound was XVI, which ...

Non-selective benzodiazepines, such as diazepam, interact with equivalent affinity and agonist efficacy at GABA(A) receptors containing either an alpha1, alpha2, alpha3 or alpha5 subunit. However, which of these particular subtypes are responsible for the anticonvulsant effects of diazepam remains uncertain. In the present study, we examined the ability of diazepam to reduce pentylenetetrazoLe ...

PURPOSE. A new series of substituted quinoline-2(1H)-one and 1,2,4triazolo[4,3-a]-quinoline derivatives were designed and synthesized to meet the structural requirements essential for anticonvulsant properties. METHODS. 4-substituted-phenyl3,4-dihydro-2(1H)-quinolines, 5-substitutedphenyl-4,5-dihydro-1,2,4-triazolo[4,3a]quinolines and 5-substituted-phenyl-4,5-dihydro-1,2,4triazolo-[4,3-a]quinol...

The occurrence of Mycobacterium tuberculosis resistance encourages the discovery new antitubercular candidates. Microbes including fungi and bacteria are well known reservoir for isolating antibiotic compounds, among natural product resources. In this review, we report promising compounds from marine-derived entomopathogenic fungi, reported 2000 to 2022. A comprehensive literature search was co...