Epilepsy is a neurological condition which is characterized by unprovoked seizures resulting from abnormal discharge of cerebral neurons and affecting at least 50 million people worldwide. There is continuing demand for new anticonvulsant agents as it has not been possible to control every kind of seizure with existing antiepileptic drugs. Moreover, conventional antiepileptic drugs exhibited un...

New 3-[(2,4-dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile derivatives 8-37 were synthesized and their pharmacological activities were determined with the objective to better understand their structure-activity relationship (SAR) for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) and pentylen...

It is often felt that poorly controlled epileptic patients, who are taking anticonvulsant medication, are over represented in A&E departments compared to the general population. This A&E based study set out to determine whether such patients do have inadequate serum anticonvulsant levels, when they present following a seizure, to A&E departments. All epileptic patients, taking medication, who p...

UNLABELLED The aim of this study was to assess bone mineral density and vitamin D metabolism in patients on chronic anticonvulsant therapy. METHODS Sixty-nine men, outpatients on chronic anticonvulsant therapy, who had been treated for at least 5 years, were studied, comparing them to thirty healthy controls. Bone mineral density was measured as well as serum levels of calcium, ionized calciu...

This study investigated the anticonvulsant activity of a new phthalazine tetrazole derivative, QUAN-0808 (6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine), in the mouse maximal electroshock (MES) seizure model. The neurotoxicity of QUAN-0808 was investigated using the rotarod neurotoxicity test in mice. QUAN-0808 exhibited higher activity (median effective dose, ED(50) = 6.8 mg/kg) and lower ne...

OBJECTIVES To evaluate a novel series of quinoxaline 1,4-di-N-oxides for in vitro activity against Mycobacterium tuberculosis and for efficacy in a mouse model of tuberculosis (TB). METHODS Ketone and amide derivatives of quinoxaline 1,4-di-N-oxide were evaluated in in vitro and in vivo tests including: (i) activity against M. tuberculosis resistant to currently used antitubercular drugs incl...

Isatin is a heterocyclic molecule that belongs to one of the most important classes organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted lot attention in medicinal chemistry. itself, shows various biological activities such antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, anticonvulsant. Bis- containing moie...

Tuberculosis still remains a leading cause of death in the world. Currently considerable interest in natural products and their derivatives in the area of drug research for multidrug resistant tuberculosis (MDR-TB). The present investigation focused on identification, isolation, characterization of lead constituents and to determine the antitubercular activity of their enriched fractions and is...

Pyridazine plays a significant role in pharmaceuticals particularly in the field of medicinal chemistry. Several 4-substituted-benzylidene-6-substituted-phenyl-dihydro-pyridazin-3(2H)-one derivatives (3a-q) were synthesized and evaluated for their antimicrobial activities with an aim to obtain promising antitubercular agents. In the first step, 6-aryl-tetrahydro-pyridazin-3-ones (2) were prepar...

In the recent years there has been an increased interest in the pyridazinone ring system. Many investigations indicated that the presence of at least one aryl group, one or two electron donor atoms and/or an NH group in a special spatial arrangement is necessary for anticonvulsant activity. Many investigations indicated that the presence of at least one aryl group, one or two electron donor ato...