Design of new potent and selective secretory phospholipase A 2 inhibitors. 6-Synthesis, structure–activity relationships and molecular modelling of 1-substituted-4-[4, …

N Meddad-Belhabich, D Aoun, A Djimdé…

Index: Meddad-Belhabich, Nadia; Aoun, Darina; Djimde, Atime; Redeuilh, Catherine; Dive, Georges; Massicot, France; Chau, Francois; Heymans, Francoise; Lamouri, Aazdine Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 10 p. 3588 - 3600

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Abstract

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 biological activity. Several modifications were explored. Various linkers, such as amide, urea, carbamate, or alkoxyphenyl were inserted between the piperazine and the lipophilic chain ...