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Lokwani P.,Jaipur National University | Kumar P.,Jaipur National University | Upadhyay Y.,Jaipur National University | Gupta S.,Jaipur National University | Singh N.,Rameesh Institute of Vocational and Technical Education
Journal of Applied Pharmaceutical Science | Year: 2011

Swine flu (swine influenza) is a respiratory disease caused by viruses (influenza viruses belonging to family Orthomyxoviridae) that infect the respiratory tract of pigs and result in nasal secretions, a barking-like cough, decreased appetite, and listless behaviour. Oseltamivir (Tamiflu) and zanamivir (Relenza) is the recommended drug both for prophylaxis and treatment. The best treatment for influenza infections in humans is prevention by vaccination. Source


Sinha R.,Rameesh Institute of Vocational and Technical Education | Sara U.V.S.,JKK Nataraja Dental College and Hospital | Khosa R.L.,Bharat Institute of Technology | Stables J.,U.S. National Institutes of Health | Jain J.,Rameesh Institute of Vocational and Technical Education
Medicinal Chemistry Research | Year: 2011

A series of aryl acid hydrazones of substituted aromatic acid hydrazides (D 1 to D 20) were synthesised and evaluated for anticonvulsant activity. Aryl acid hydrazones of Nicotinic acid hydrazide (D 8, D 9, and D 10) have displayed excellent protection in maximal electroshock screen. These compounds have also exhibited excellent binding properties with Lys 329 residue of gamma amino butyrate amino transferase (GABA-AT) in Lamarckian genetic algorithm based flexible docking studies. Compound D 8, N 1-(4-chlorobenzylidene) nicotinohydrazide was found to be the most potent analog with ED50 value of 16.1 mg/kg and protective index (PI = TD 50/ED 50) value of > 20, which was much greater than that of the prototype drug phenytoin (PI = 6.9). It has shown free binding energy value of -10.20 kcal/mol and inhibition constant (Ki) value of 33.30 nM for GABA-AT, indicating that aryl acid hydrazones of nicotinic acid hydrazide could be considered as a new pharmacophore in the design of novel anticonvulsant drugs. © Springer Science+Business Media, LLC 2010. Source


Sinha R.,Rameesh Institute of Vocational and Technical Education | Sara U.V.S.,Raj Kumar Goel Institute of Technology | Khosa R.L.,Bharat Institute of Technology | Stables J.,U.S. National Institutes of Health | Jain J.,Rameesh Institute of Vocational and Technical Education
Central Nervous System Agents in Medicinal Chemistry | Year: 2013

A series of twelve compounds (Compounds RNH1-RNH12) of acid hydrazones of pyridine-3-carbohydrazide or nicotinic acid hydrazide was synthesized and evaluated for anticonvulsant activity by MES, scPTZ, minimal clonic seizure and corneal kindling seizure test. Neurotoxicity was also determined for these compounds by rotarod test. Results showed that halogen substitution at meta and para position of phenyl ring exhibited better protection than ortho substitution. Compounds RNH4 and RNH12, were found to be the active analogs displaying 6Hz ED50 of 75.4 and 14.77 mg/kg while the corresponding MES ED50 values were 113.4 and 29.3 mg/kg respectively. In addition, compound RNH12 also showed scPTZ ED50 of 54.2 mg/kg. In the series, compound RNH12 with trifluoromethoxy substituted phenyl ring was the most potent analog exhibiting protection in all four animal models of epilepsy. Molecular docking study has also shown significant binding interactions of these two compounds with 1OHV, 2A1H and 1PBQ receptors. Thus, N-[(meta or para halogen substituted) benzylidene] pyridine-3-carbohydrazides could be used as lead compounds in anticonvulsant drug design and discovery. © 2013 Bentham Science Publishers. Source

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