55584-01-5Relevant academic research and scientific papers
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
Boukli, Latifa,Touaibia, Mohamed,Meddad-Belhabich, Nadia,Djimde, Atime,Park, Chang-Ha,Kim, Jung-Joo,Yoon, Joo-Hyoung,Lamouri, Aazdine,Heymans, Francoise
, p. 1242 - 1253 (2008/09/17)
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).
Novel inhibitor compounds specific of secreted non-pancreatic human a2phospholipase of group II
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Page/Page column 11, (2010/02/11)
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.
FUSED PYRIMIDINES. PART 5. PYRIMIDOPYRIMIDINE ANALOGUES OF FOLIC ACID
Delia, Thomas J.,Baumann, Markus,Bunker, Amy
, p. 1397 - 1410 (2007/10/02)
Pyrimidopyrimidine analogues of folic acid have been prepared and tested for antitumor activity.Using Mannich reaction conditions, 2,4,6-triaminopyrimidine (12) or 2,4-diamino-6-oxopyrimidine (13) was treated with formaldehyde and either diethyl N--L-glutamate (18) or diethyl N--L-glutamate (24).The corresponding diester products (19, 20 and 25, 26) were converted to the diacids (5, 6 and 7, 8) by treatment with aqueous ethanolic sodium hydroxide.Compounds (5, 6, and 7) were screened against CCRF-CEM leukemiccells and found to be significantly less active than DDATHF, one of the most active compounds for this system.
Phenyl azophenyl dyestuff
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, (2008/06/13)
Dyestuff of the formula: SPC1 In which m is equal to 0 or 1, n is equal to 1, 2 or 3, A represents the residue of an aromatic or heterocyclic diazotizable amine devoid of solubilizing acid groups, the benzene ring B is unsubstituted or substituted by one
