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Relevant academic research and scientific papers

Synthesis of some 1,2,4-triazoles as potential anti-tubercular agents

A series of 5-(N-substituted carboxamidoethylthio)-3-(3'pyridyl)-4- amino-1,2,4-triazole derivatives 6a-j have been synthesized and evaluated for anti-tubercular activity. They are screened in-vitro at 10μg/mL concentration against Mycobacterium tuberculosis H37RV (ATCC 27294). All the compounds are showing antitubercular activity when compared with the standard drug Amikacin. Compounds 6e and 6h are found active as they displayed IC50 and IC90 values at 100μg/mL.

Synthesis and anticonvulsant activity of some 2/3- benzoylaminopropionanilide derivatives

In this study, the synthesis and anticonvulsant properties of sixteen 2/3-benzoylaminopropionanilide derivatives were described. Molecular design of the compounds has been based on the modification of lacosamide which is a functionalized amino acid with a novel anticonvulsant activity. The structural confirmation of the title compounds was achieved by spectral and analytical data. The anticonvulsant activity profile of synthesized compounds was determined by maximal electroshock (MES) and subcutaneous metrazole (scMet) seizure tests, whereas their neurotoxicity was examined using rotarod test. All these tests were performed in accordance with the procedures of the Antiepileptic Drug Development (ADD) program. The majority of the compounds were effective in the MES or scMet screening tests. None of the compounds showed neurotoxicity according to the rotarod test at studied doses. Most active compounds in the series were 3, 12 and 13, which bearing 2-methyl, 2-ethyl and 2-isopropyl substituent on the N-phenyl ring, respectively. Georg Thieme Verlag KG Stuttgart - New York.

Synthesis and anticonvulsant activity of some ω-(1H-imidazol-1-yl)-N- phenylacetamide and propionamide derivatives

In this study, eight new ω-(1H-imidazol-1-yl)-N-phenylacetamide and propionamide derivatives having 2,6-dimethyl, 2,6-dichloro, 2-chloro-6-methyl and 2-isopropyl substitutions on N-phenyl ring were synthesized to evaluate anticonvulsant activity against maximal electroshock test. The most active compounds in the series were the derivatives bearing 2-isopropyl and 2,6-dimethyl substituents on N-phenyl ring.

The synthesis and anticonvulsant activity of some omega-phthalimido-N-phenylacetamide and propionamide derivatives.

In this study, by combining anilide and N', N'-phthaloylglycinamide pharmacophores which are known to produce potent anticonvulsant compounds, sixteen omega-phthalimido-N-phenylacetamide and propionamide derivatives bearing substituents at positions 2 or 2, 6 on N-phenyl ring have been synthesized. The structural confirmation of the title compounds was achieved by interpretation of spectral and analytical data. The anticonvulsant activity of the title compounds was determined against maximal electroshock seizure at 100 mg/kg dose level in mice. The preliminary screening results indicated that omega-phthalimido-N-phenylacetamide and propionamide nuclei have pronounced anticonvulsant activity against maximal electroshock seizure.

N-aryl-piperazinealkanamides useful for protecting hearts from myocardial injury caused by ischaemia, anoxia or hypoxia

Novel N-aryl-piperazinealkanamides, having particular substituents attached to one of the carbon atoms of the piperazine ring, which compounds are useful to protect hearts from myocardial injury caused by ischaemia, anoxia or hypoxia.