Isoflavonoids in non-leguminous families: an update

This review provides a listing of isoflavonoids reported in non-leguminous families. Reviews published to date have principally focused on plants with the richest isoflavonoid contents, the family Leguminosae. After a brief recall of the structure of isoflavonoids, we present all isoflavonoid structures encountered in non-leguminous families which may, thereby, become new plant sources for these compounds. Articles reporting on their different functions in plants are presented, as well as a brief summary discussing their potential benefits for human health. A list of 135 references is given

Phenylalanine derivatives active against

The action of phenylalanine derivatives against a cyst forming strain of Toxoplasma gondii was tested in vitroand in vivo in mice. These compounds were Phe-Phe-OMe (dipeptide methyl ester) 1 and its cyclized product, 3,6-dibenzyl-2,5-dioxopiperazine 2, Boc-L-Phe 3, L-Phe-OMe 4, Boc-L-Phe-L-Phe-OMe 5. After a 48 hr incubation in vitro, the compounds 3 and 5 induced a higher inhibition than the control molecule, pyrimethamine. In the in vivo studies, the compound 3 induced a 77 % decrease in the number of cerebral cysts, comparable to pyrimethamine. Compounds 1, 5 and 4 induced a decrease of about 63 % in the cyst number. A size reduction and an alteration of the wall of treated cysts were often noted. In a histological study, a reduction in cyst size without either inflammation or intervention of the nevroglial cells was observed. The present study provides evidence on the efficacy of phenylalanine derivatives and especially Boc-Phe 3, against T. gondii brain cysts in mice

Antileishmanial activity of polycyclic derivatives

33 polycyclic derivatives have been studied and tested on Leishmania donovani and L. major promastigotes. Their antileishmanial activity was assessed in vitro and an assay of their cytotoxicity was realized on human myelomonocytic cell line. The reference molecules used in the assays were amphotericin B and pentamidine. Among the compounds tested, 29 possess an antileishmanial activity; 25 of those were more active against L. donovani than amphotericin B, and nine were as effective as amphotericin B against L. major. Many synthesized derivatives were more active against L.donovani than against L. major. The cytotoxicity studies have shown that among the thirty-three derivatives tested, 12 molecules have an IC50 towards THP-1 cells about equal than that reference drugs, the 21 other derivatives are much less toxic. A 3D QSAR study was undertaken and has permitted to predict activity against L. donovani and L. major and to highlight critical area to optimize activity against the two species

Antileishmanial activity of polycyclic derivatives

33 polycyclic derivatives have been studied and tested on Leishmania donovani and L. major promastigotes. Their antileishmanial activity was assessed in vitro and an assay of their cytotoxicity was realized on human myelomonocytic cell line. The reference molecules used in the assays were amphotericin B and pentamidine. Among the compounds tested, 29 possess an antileishmanial activity; 25 of those were more active against L. donovani than amphotericin B, and nine were as effective as amphotericin B against L. major. Many synthesized derivatives were more active against L.donovani than against L. major. The cytotoxicity studies have shown that among the thirty-three derivatives tested, 12 molecules have an IC50 towards THP-1 cells about equal than that reference drugs, the 21 other derivatives are much less toxic. A 3D QSAR study was undertaken and has permitted to predict activity against L. donovani and L. major and to highlight critical area to optimize activity against the two species

P143 Clinical observation leads to the synthesis of BG185, a new antistaphylococcal compound

International audienc

Chirality Effects in Jet-Cooled Cyclic Dipeptides

International audienc