Urea/thiourea derivatives of Gly/Pro conjugated 2,3-dichlorophenyl piperazine as potent anti-inflammatory agents: SAR studies

Vardhan,, D. M. Suyoga and Kumara, H. K. and Sridhara, M. B. and Channe Gowda, D. (2017) Urea/thiourea derivatives of Gly/Pro conjugated 2,3-dichlorophenyl piperazine as potent anti-inflammatory agents: SAR studies. Indian Journal Of Chemistry Section B-Organic Chemistry Including Medicinal Chemistry, 56 (11). pp. 1207-1211. ISSN 0975-0983

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Abstract

wo series of urea/thiourea derivatives of Gly/Pro conjugated 2,3-dichlorophenyl piperazine have been synthesized and characterized as novel anti-inflammatory agents. The results demonstrate that the derivatives 1f, 1g, 1j, 1k, 2g, 2j and 2k show good anti-inflammatory properties with IC50 values of 42 ± 0.32 µM, 30 ± 0.51 µM, 65 ± 0.61 µM, 60 ± 0.52 µM, 60 ± 0.22 µM, 57 ± 0.37 µM and 35 ± 0.15 µM respectively. These results reveal that compounds with electron withdrawing moieties (F and Cl) particularly at para position exhibit excellent anti-inflammatory activity compared to the standards indomethacin (IC50 = 58 ± 0.37 µM) and ibuprofin (IC50 = 67 ± 0.43 µM).

Item Type:	Article
Uncontrolled Keywords:	Amino acids; piperazine; conjugation; urea/thiourea; anti-inflammatory; SAR
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	C Swapna Library Assistant
Date Deposited:	20 Jun 2019 05:15
Last Modified:	20 Jun 2019 05:15
URI:	http://eprints.uni-mysore.ac.in/id/eprint/3437

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