- Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: Synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4′-yl(oyl)] piperazines
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Among the different PLA2s identified to date, the group IIA secretory PLA2 (sPLA2 GIIA) is implied in diverse pathological conditions. In this work we describe the synthesis, inhibitory activities, and structure-activity relationships (SAR) of a new class of substituted piperazine derivatives. The in vitro fluorimetric assay using two groups of enzymes, GIB and GIIA, revealed several compounds as highly potent inhibitors (IC50 = 0.1 μM). The in vivo activity assessed by ip or per os administration in a carrageenan-induced edema test in rats showed that two compounds proved to be as potent as indomethacin (10 mg/kg).
- Boukli, Latifa,Touaibia, Mohamed,Meddad-Belhabich, Nadia,Djimde, Atime,Park, Chang-Ha,Kim, Jung-Joo,Yoon, Joo-Hyoung,Lamouri, Aazdine,Heymans, Francoise
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p. 1242 - 1253
(2008/09/17)
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- Novel inhibitor compounds specific of secreted non-pancreatic human a2phospholipase of group II
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The present invention relates to a compound of the following formula (I) and pharmaceutical compositions containing the compound of formula (I): wherein D, Y, A, B, p, q, W and R have the same meanings as defined in the specification.
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Page/Page column 4
(2010/02/11)
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