PASTIC Dspace Repository

Synthesis of 2-[(5-benzyl-1,3,4-oxadiazole-2yl)sulfanyl]-N- (arylated/arenylated) acetamides as antibacterial and acetyl cholinesterase inhibitors

Show simple item record

dc.contributor.author Zahra Siddiqui, Sabahat
dc.contributor.author Athar Abbasi, Muhammad
dc.contributor.author Rehman, Aziz-ur
dc.contributor.author Ashraf, Muhammad
dc.contributor.author Mirza, Bushra
dc.contributor.author Ismai, Hammad
dc.date.accessioned 2022-11-23T07:54:25Z
dc.date.available 2022-11-23T07:54:25Z
dc.date.issued 2017-09-30
dc.identifier.citation Siddiqui, S. Z., Abbasi, M. A., Ashraf, M., Mirza, B., & Ismail, H. (2017). Synthesis of 2-[(5-benzyl-1, 3, 4-oxadiazole-2yl) sulfanyl]-N-(arylated/arenylated) acetamides as antibacterial and acetyl cholinesterase inhibitors. Pakistan Journal of Pharmaceutical Sciences, 30(5). en_US
dc.identifier.issn 1011-601X
dc.identifier.uri http://142.54.178.187:9060/xmlui/handle/123456789/14096
dc.description.abstract The synthetic methodology is carried out in multistep which was initiated as phase I by utilizing Fischer esterification methodology of 2-phenylacetic acid (1) to ethyl-2-phenylacetate (2). The ester was reacted with hydrazine hydrate form 2-phenylacetohydrazide (3) which underwent ring closure with carbon disulfide in alcoholic base to achieve 5-benzyl-1,3,4-oxadiazole-2-thiol (4). Phase II, involved the reaction of electrophiles with 2- bromoacetylbromide (5) with arylated/arenylated amines (6a-e) in aqueous alkaline medium under vigorous shaking to generate N-substituted-2-bromoacetamides (7a-e). Finally in phase III, the parent oxadiazole reacted with N-substituted2-bromoacetamides and in DMF/LiH to yield 2-[(5-benzyl-1,3,4-oxadiazole-2yl)sulfanyl]-N-(arylated/arenylated) acetamides (8a-e). All the derivatives were creened for their anti-enzymatic potential against acetyl/butyrylcholinesterase and lipoxygenase and for the antibacterial activity. They were found to be weak enzyme inhibitors and also possessed weak antibacterial action with the exception of 8e, which demonstrated prominent antienzymatic and antibacterial activity, which may be attributed to the presence of 3,4-dimethoxyphenylacetamide moiety. The LD50 data revealed that most of the N-substituted derivatives were found to be less cytotoxic. en_US
dc.language.iso en en_US
dc.publisher Karachi: Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi en_US
dc.subject 2-[(5-benzyl-1,3,4-oxadiazole-2yl)sulfanyl]-N-(arylated/arenylated)acetamides en_US
dc.subject anti-enzymatic analysis en_US
dc.subject antibacterial action en_US
dc.subject cytotoxicity en_US
dc.subject 1H-NMR and EI-MS en_US
dc.title Synthesis of 2-[(5-benzyl-1,3,4-oxadiazole-2yl)sulfanyl]-N- (arylated/arenylated) acetamides as antibacterial and acetyl cholinesterase inhibitors en_US
dc.type Article en_US


Files in this item

This item appears in the following Collection(s)

Show simple item record

Search DSpace


Advanced Search

Browse

My Account