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Bulletin of Pharmaceutical Sciences-Assiut University. 2011; 34 (1): 77-92
in English | IMEMR | ID: emr-135653

ABSTRACT

Three new series of N-[aryl or heteroarylmethylidene]-2-[1H-1,2,4-triazolo[2,3-a] benzimidazol-2-ylsuljanyl] acetohydrazides [4a-k], N-[alpha-arylethylidene]-2-[1H-1, 2, 4-triazolo[2,3-aJbenzimidazol-2-ylsuljanyl] acetohydrazides [5a-d], and 2-[[[5-[alkyl or aralkylsulfanyl]-1, 3, 4-oxadiazol-2-yl]methyl]sulfanyl]-1 H-1, 2, 4-triazolo[2,3-alpha] benzimidazoles [7a-e] were synthesized. Reaction of compound [1] with methyl bromoacetate afforded [2], which when refluxed with hydrazine hydrate yielded [3]. The latter was condensed with aromatic aldehydes and substituted acetophenones to afford compounds [4a-k] and [5a-d] respectively. Treatment of compound [3] with carbon disulfide in the presence of potassium hydroxide resulted in the formation of [6]. The latter was alkylated with the appropriate alkyl or aralkyl halides to afford compounds [7a-e]. The purity of all new compounds was checked by TLC and elucidation of their structures was confirmed by IR, [1]HNMR, and mass spectrometry along with elemental microanalyses. All the target compounds were evaluated for their in-vitro antimicrobial and in-vivo anti-inflammatory activities in comparison with ampicillin, fluconazole, and indomethacin as reference drugs respectively. In addition to molecular docking of compound 5c was performed


Subject(s)
Triazoles/chemistry , Anti-Infective Agents , Anti-Inflammatory Agents
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