Synthesis and biological evaluation of novel pyrazole compounds

Amal M Youssef, Edward G Neeland, Erika B Villanueva, M Sydney White, Ibrahim M El-Ashmawy, Brian Patrick, Andis Klegeris, Alaa S Abd-El-Aziz

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

41 Citationer (Scopus)

Abstract

A novel dipyrazole ethandiamide compound and acid chloride of pyrazolo[3,4-d]pyrimidine 4(5H)-one were prepared and reacted with a number of nucleophiles. The resultant novel compounds were tested in several in vitro and in vivo assays. Three compounds inhibited the secretion of neurotoxins by human THP-1 monocytic cells at concentrations that were not toxic to these cells. They also partially inhibited both cyclooxygenase-1 and -2 isoforms. In animal studies, two compounds were notable for their anti-inflammatory activity that was comparable to that of the clinically available cyclooxygenase-2 inhibitor celecoxib. Modeling studies by using the molecular operating environment module showed comparable docking scores for the two enantiomers docked in the active site of cyclooxygenase-2.

OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind18
Udgave nummer15
Sider (fra-til)5685-96
Antal sider12
ISSN0968-0896
DOI
StatusUdgivet - 1 aug. 2010
Udgivet eksterntJa

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Copyright (c) 2010 Elsevier Ltd. All rights reserved.

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