Synthesis and sar studies of bisthiourea derivatives of dipeptides lys/lys-asp, lys/lys-trp conjugated benzodisoxazole as promising antioxidants

Kumara, H. K. and Channe Gowda, D. (2017) Synthesis and sar studies of bisthiourea derivatives of dipeptides lys/lys-asp, lys/lys-trp conjugated benzodisoxazole as promising antioxidants. International Journal of Peptide Research and Therapeutics, 23 (2). pp. 259-267. ISSN 1573-3904

Text Synthesis and Sar Studies of Bisthiourea Derivatives of Dipeptides Lyslys-Asp Lyslys-Trp Conjugated Benzo[d]isoxazole as Promising Antioxidants.pdf - Published Version Restricted to Registered users only Download (425kB) | Request a copy

Abstract

A novel series of bisthiourea derivatives of four dipeptides consisting of Lys-Asp, lys-Asp, Lys-Trp and lys-Trp conjugated to 6-fluoro-3-(piperidin-4-yl)benzodisoxazole were synthesized and characterized by physical method and spectroscopic data. The molecules 1--24 were evaluated for their in vitro antioxidant activity and compared with commercial antioxidants ascorbic acid (AA) and gallic acid (GA), employing 1,1-diphenyl-2-picryl-hydrazyl (DPPH), N,N-dimethyl-p-phenylenediamine dihydrochloride (DMPD) and 2,2-azinobis-(3-ethylbenzothiazoline-6-sufonic acid) (ABTS) assays. The results revealed that IC50 of 8, 11, 20 and 23 with electron donating OCH3 group were lower than the IC50 of commercial standards AA and GA in all the three performed antioxidant assays indicating the good activities of these compounds. The analogues with Trp (13--24) showed better activity than the corresponding analogues with Asp (1--12). Further, the dipeptide derivatives with d-configuration (lys) were found to be more potent than the dipeptide derivatives with l-configuration (Lys).

Item Type:	Article
Uncontrolled Keywords:	Conjugation, Bisthiourea, Antioxidant, Dipeptides, Configuration
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	C Swapna Library Assistant
Date Deposited:	10 Jun 2019 06:15
Last Modified:	10 Jun 2019 06:15
URI:	http://eprints.uni-mysore.ac.in/id/eprint/2891

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