Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents
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Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents. / Youssef, Amal M; White, M Sydney; Villanueva, Erika B; El-Ashmawy, Ibrahim M; Klegeris, Andis.
In: Bioorganic & Medicinal Chemistry, Vol. 18, No. 5, 01.03.2010, p. 2019-28.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents
AU - Youssef, Amal M
AU - White, M Sydney
AU - Villanueva, Erika B
AU - El-Ashmawy, Ibrahim M
AU - Klegeris, Andis
N1 - Copyright 2010 Elsevier Ltd. All rights reserved.
PY - 2010/3/1
Y1 - 2010/3/1
N2 - Novel pyrazolyl-2,4-thiazolidinediones were prepared via the reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinediones and substituted benzyl-2,4-thiazolidinediones. The resultant compounds were first evaluated for their anti-inflammatory and neuroprotective properties in vitro. The active compounds were further studied in vivo by using the formalin-induced paw edema and the turpentine oil-induced granuloma pouch bioassays. We identified four novel compounds that showed protective effects in vitro at non-toxic concentrations, and were also effective in the animal models of acute and sub-acute inflammation.
AB - Novel pyrazolyl-2,4-thiazolidinediones were prepared via the reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinediones and substituted benzyl-2,4-thiazolidinediones. The resultant compounds were first evaluated for their anti-inflammatory and neuroprotective properties in vitro. The active compounds were further studied in vivo by using the formalin-induced paw edema and the turpentine oil-induced granuloma pouch bioassays. We identified four novel compounds that showed protective effects in vitro at non-toxic concentrations, and were also effective in the animal models of acute and sub-acute inflammation.
KW - Animals
KW - Anti-Inflammatory Agents/chemical synthesis
KW - Cell Line, Tumor
KW - Cyclooxygenase 1/metabolism
KW - Cyclooxygenase 2/metabolism
KW - Edema/chemically induced
KW - Granuloma/chemically induced
KW - HL-60 Cells
KW - Humans
KW - Neuroprotective Agents/chemical synthesis
KW - Rats
KW - Thiazolidinediones/chemical synthesis
U2 - 10.1016/j.bmc.2010.01.021
DO - 10.1016/j.bmc.2010.01.021
M3 - Journal article
C2 - 20138770
VL - 18
SP - 2019
EP - 2028
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
SN - 0968-0896
IS - 5
ER -
ID: 236610080