{"id":2798,"date":"2015-12-05T14:08:00","date_gmt":"2015-12-05T14:08:00","guid":{"rendered":"https:\/\/chempublishers.com\/pjc\/?p=2798"},"modified":"2025-06-14T05:36:09","modified_gmt":"2025-06-14T05:36:09","slug":"pjc-1615","status":"publish","type":"post","link":"https:\/\/chempublishers.com\/Pakistan-journal-of-chemistry\/2015\/12\/05\/pjc-1615\/","title":{"rendered":"2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases"},"content":{"rendered":"\t\t
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Research Article | Open Access<\/strong><\/div>\n
Volume 5 | Issue 3 | https:\/\/doi.org\/10.15228\/2015.v05.i03.p02<\/a><\/span><\/div>\n<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n
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2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases<\/h4>\n
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\n

S.Z. Siddiqui<\/span><\/p>\n

Department of Chemistry, Government College University, Lahore-54000, Pakistan<\/p>\n

M.A. Abbasi<\/span><\/p>\n

Department of Chemistry, Government College University, Lahore-54000, Pakistan<\/p>\n

Aziz Ur Rehman<\/span><\/p>\n

Department of Chemistry, Government College University, Lahore-54000, Pakistan<\/p>\n

M. Irshad<\/span><\/p>\n

Department of Chemistry, Government College University, Lahore-54000, Pakistan<\/p>\n

M. Ashraf<\/span><\/p>\n

Department of Biochemistry and Biotechnology; The Islamia University of Bahawalpur, Bahawalpur- 63100, Pakistan<\/p>\n

Qurat Ul Ain<\/span><\/p>\n

Department of Biochemistry and Biotechnology; The Islamia University of Bahawalpur, Bahawalpur- 63100, Pakistan<\/p>\n

Bushra Mirza<\/span><\/p>\n

Department of Biochemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan<\/p>\n

H. Ismail<\/span><\/p>\n

Department of Biochemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan<\/p>\n

<\/p>\n\n\n\n
Received<\/strong>
15 Mar, 2015<\/td>\n		Accepted<\/strong>
30 Sep, 2015<\/td>\n		Published<\/strong>
15 Dec, 2015<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n
\n

1, 3, 4-Oxadiazoles are known to possess diverse biological activities and proposed synthetic methodology was aimed to synthesize biologically active 1, 3, 4-oxadiazole-2-thiols derivatives. It was instigated by converting 2-phenylacetic acid (1) to ethyl-2-phenylacetate (2) by Fischer esterification method. The ester underwent hydrazinolysis to afford 2-phenylacetohydrazide (3) which was transformed via ring closure with carbon disulfide in alcoholic base to achieve 5-benzyl-1,3,4-oxadiazole-2-thiol (4). Finally, the parent oxadiazole 4 was reacted with a variety of aralkylated\/arylated\/arenylated halides (5a-i) in polar aprotic solvent; N,N\u02c8-dimethylformamide (DMF) and lithium hydride (LiH) which acted as base under to afford 2- (aralkylated\/arylated\/arenylatedthio) 5-benzyl-1,3,4-oxadiazoles (6a-i). The synthesized derivatives were screened against acetyl\/butyrylcholinesterases for enzyme inhibitory potential. The incorporation of 3-nitro\/4-nitrophenyl moieties on S-position of parent oxadiaozle demonstrated decent inhibitory potential against cholinesterases while rest displayed weak inhibition relative to reference standard Eserine. The LD50<\/sub> data revealed that most of the derivatives were found to be less cytotoxic relative to standard doxorubicin<\/p>\n<\/div>\n

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How to Cite this paper?<\/h3>\n
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APA-7 Style<\/strong>
Siddiqui, S.Z., Abbasi, M.A., Rehman, A.U., Irshad, M., Ashraf, M., Ain, .U., Mirza, B., Ismail, H. (2015). 2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases. Pakistan Journal of Chemistry<\/em>, 5(3), 104-110<\/a>. https:\/\/doi.org\/10.15228\/2015.v05.i03.p02<\/p>\n

ACS Style<\/strong>
Siddiqui, S.Z.; Abbasi, M.A.; Rehman, A.U.; Irshad, M.; Ashraf, M.; Ain, .U.; Mirza, B.; Ismail, H. 2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases. Pak. J. Chem.<\/em> 2015, 5, 104-110<\/a>. https:\/\/doi.org\/10.15228\/2015.v05.i03.p02<\/p>\n

AMA Style<\/strong>
Siddiqui SZ, Abbasi MA, Rehman AU, Irshad M, Ashraf M, Ain U, Mirza B, Ismail H. 2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases. Pakistan Journal of Chemistry<\/em>. 2015; 5(3): 104-110<\/a>. https:\/\/doi.org\/10.15228\/2015.v05.i03.p02<\/p>\n

Chicago\/Turabian Style<\/strong>
Siddiqui, S., Z., M. A. Abbasi, Aziz Ur Rehman, M. Irshad, M. Ashraf, Qurat Ul Ain, Bushra Mirza, and H. Ismail. 2015. “2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases” Pakistan Journal of Chemistry<\/em> 5, no. 3: 104-110<\/a>. https:\/\/doi.org\/10.15228\/2015.v05.i03.p02<\/p>\n<\/div>\n<\/div>\n<\/div>\n

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\"Creative<\/a><\/p>\n

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Research Article | Open Access Volume 5 | Issue 3 | https:\/\/doi.org\/10.15228\/2015.v05.i03.p02 2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases S.Z. Siddiqui Department of Chemistry, Government College University, Lahore-54000, Pakistan M.A. Abbasi Department of Chemistry, Government College University, Lahore-54000, Pakistan Aziz Ur Rehman Department of Chemistry, Government College University, Lahore-54000, Pakistan M. […]<\/p>\n","protected":false},"author":2,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[1],"tags":[],"class_list":["post-2798","post","type-post","status-publish","format-standard","hentry","category-uncategorized"],"acf":[],"yoast_head":"\n2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases - Pakistan Journal of Chemistry<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/chempublishers.com\/Pakistan-journal-of-chemistry\/2015\/12\/05\/pjc-1615\/\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases - Pakistan Journal of Chemistry\" \/>\n<meta property=\"og:description\" content=\"Research Article | Open Access Volume 5 | Issue 3 | https:\/\/doi.org\/10.15228\/2015.v05.i03.p02 2-(Aralkylated\/Arylated\/Arenylatedthio) 5-Benzyl-1, 3, 4-Oxadiazoles: As Less Cytotoxic And Moderate Inhibitors Of Cholinesterases S.Z. 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