In Silico Screening, Synthesis And Pharmacological Screening of Quinazolinones Containing Oxazepinone Ring as NMDA Receptor Antagonists for Anticonvulsant Activity: Part -I

In silico Screening and Evaluation of the Anticonvulsant Activity of Docosahexaenoic Acid-Like Molecules in Experimental Models of Seizures

Background: Resistance to antiepileptic drugs as well as intolerability in 20-30% of the patients raises demand for developing new drugs with improved efficacy and safety. Acceptable anticonvulsant activity, good tolerability, and inexpensiveness of docosahexaenoic acid (DHA), make it as a good candidate for designing and development of the new anticonvulsant medications. Methods: Ten DHA-based...

Synthesis and Screening of Some New Isatin Containing Thiazole Derivatives for Antimicrobial Activity

In the present work, a series of new N’-[{5-(4-aryl) 1,3-thiazol-2yl}carbohydrazide-methyl]- 3(4-arylimino) indol-2-one analogs (5a-g) had heen synthesized from 3-(4-arylimino)-2-oxo- 1-indole-acetylthiosemicarbazide (4a-g) in ethanol, in the presence of phenacyl bromide or substituted phenacyl bromides. The compound 5e was characterized by its elemental analysis, IR, 1 HNMR and Mass Spectrosco...

in silico screening and evaluation of the anticonvulsant activity of docosahexaenoic acid-like molecules in experimental models of seizures

background: resistance to antiepileptic drugs as well as intolerability in 20-30% of the patients raises demand for developing new drugs with improved efficacy and safety. acceptable anticonvulsant activity, good tolerability, and inexpensiveness of docosahexaenoic acid (dha), make it as a good candidate for designing and development of the new anticonvulsant medications. methods: ten dha-based...

Limits of Ligand Selectivity from Docking to Models: In Silico Screening for A1 Adenosine Receptor Antagonists

G protein-coupled receptors (GPCRs) are attractive targets for pharmaceutical research. With the recent determination of several GPCR X-ray structures, the applicability of structure-based computational methods for ligand identification, such as docking, has increased. Yet, as only about 1% of GPCRs have a known structure, receptor homology modeling remains necessary. In order to investigate th...

synthesis and screening of some new isatin containing thiazole derivatives for antimicrobial activity