Meddad-Belhabich, Nadia published the artcileDesign of new potent and selective secretory phospholipase A2 inhibitors. 6-Synthesis, structure-activity relationships and molecular modelling of 1-substituted-4-[4,5-dihydro-1,2,4-(4H)-oxadiazol-5-one-3-yl(methyl)]-functionalized aryl piperazin/one/dione derivatives, Computed Properties of 67914-60-7, the publication is Bioorganic & Medicinal Chemistry (2010), 18(10), 3588-3600, database is CAplus and MEDLINE.
The group IIA human non-pancreatic secretory phospholipase A2 (hnp-sPLA2) is one of the enzymes implied in the inflammatory process. In the course of our work on inhibitors of this enzyme we investigated the influence of rigidity of the piperazine region on the biol. activity. Several modifications were explored. Various linkers, such as amide, urea, carbamate, or alkoxyphenyl were inserted between the piperazine and the lipophilic chain. Also, modification of the piperazine core to incorporate carbonyl groups was studied. In an in vitro fluorimetric assay using the human GIIA (HPLA2) and porcine pancreatic GIB enzymes, compound 60a (I) had the optimal activity with an IC50 = 30 nM on HPLA2. By means of mol. modeling we attempted to get informations towards comprehension of differences in activity.
Bioorganic & Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Computed Properties of 67914-60-7.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics