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1.
Pakistan Journal of Pharmaceutical Sciences. 2018; 31 (5): 1783-1790
in English | IMEMR | ID: emr-199557

ABSTRACT

A number of novel 5-substituted-2-[[6-bromo-3,4-methylenedioxybenzyl]thio]-1,3,4-Oxadiazole derivatives [6a-l] have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids [1a-l] as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols [4a-l] were yielded in good amounts.The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride [5] in DMFto synthesize the required compounds. All the synthesized molecules were well characterized by IR, [1]H-NMR, [13]C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential

2.
Pakistan Journal of Pharmaceutical Sciences. 2016; 29 (1): 27-34
in English | IMEMR | ID: emr-177264

ABSTRACT

The most emerging class among the heterocyclic compounds is 1,3,4-oxadiazoles for their diverse biological activities. In the present research work, piperonylic acid [1] was converted consecutively into corresponding ester [2], hydrazide [3] and 1,3,4-oxadiazole [4] through intermolecular cyclization. The synthesized compound 4 was subjected further to S-alkylation/aralkylation, using alkyl/aralkyl halides [5a-m] and S-substituted-1,3,4-oxadiazole derivatives were synthesized [6a-m]. The structure elucidation of the synthesized molecules was processed through [1]H-NMR, IR and mass spectral data. The antibacterial activity showed these molecules moderately good inhibitors of gram-negative and gram-positive bacteria

3.
Pakistan Journal of Pharmaceutical Sciences. 2016; 29 (6): 2109-2117
in English | IMEMR | ID: emr-184158

ABSTRACT

The various p-substituted benzenesulfonyl chlorides [2a-e] were treated with [3,4-methylenedioxy] benzylamine [1] in the presence of aqueous Na2CO3 solution to synthesize N-[3,4-methylenedioxybenzyl]-4-substitutedbenzenesulfonamides [3a-e]. The synthesized molecules were further converted into corresponding Nethyl/benzyl/4-flourobenzyl-N-[3,4-methylenedioxybenzyl]-4-substitutedbenzenesulfonamides [7a-e, 8a-e, 9a-e] on reaction with ethyl iodide [4], benzyl chloride [5] and 4-flourobenzyl chloride [6] in the presence of sodium hydride using N,N-dimethylformamide as solvent. The structure elucidation was processed through different spectral techniques including IR, [1]H-NMR and EIMS. The screening of the synthesized molecules against Gram-bacterial strains, to evaluate antibacterial activity, showed them moderately good inhibitors as shown by their low MIC values

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