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Title: Urea/thiourea derivatives of Gly/Pro conjugated 2,3-dichlorophenyl piperazine as potent anti-inflammatory agents: SAR studies
Authors: Vardhan, D M Suyoga
Kumara, H K
Sridhara, M B
Gowda, D Channe
Keywords: Amino acids;Piperazine;Conjugation;Urea/Thiourea;Anti-inflammatory;SAR
Issue Date: Nov-2017
Publisher: NISCAIR-CSIR, India
Abstract: Two 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).
Page(s): 1207-1211
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.56B(11) [November 2017]

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