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2-(Aralkylated/Arylated/Arenylatedthio) 5-Benzyl-1, 3, 4-oxadiazoles: as less cytotoxic and moderate inhibitors of Cholinesterases.
Author(s)
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. Irshad Department of Chemistry, Government College University, Lahore-54000, Pakistan
M. Ashraf Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur- 63100, Pakistan
Qurat-ul-Ain Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur- 63100, Pakistan
Bushra Mirza Department of Biochemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan
H. Ismail Department of Biochemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan
Abstract
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'-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 data revealed that most of the derivatives were found to be less cytotoxic relative to standard doxorubicin.
Publication Details
Page(s) 101-107
DOI DOI not available
Published Journal: Pakistan Journal of Chemistry, Volume: 5, Issue: 3, Year: 2015
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