Henri Sentenac-Roumanou

Synthèse et activité radioprotectrice de germatranes, silatranes, oxydes et sulfures germaniés à ligande chlorhydrate de cystéamine, méthylcystéamine et N(thio-2 éthyl)diamino-1,3 propane

Resume De nouvelles structures organogermaniees et siliciees de type germatranes ou silatranes, oxydes ou sulfures de germanium a ligande chlorhydrate de cysteamine, de methylcysteamine et N (thio-2 ethyl)diamino-1,3 propane, ont ete synthetisees. Leur toxicite aigue et leur activite radioprotectrice ont ete determinees. Les germatranes semblent etre les structures les plus actives dans ce dernier domaine. La toxicite de ces derives (y compris celle des silatranes) est generalement faible.

Synthèse et activité radioprotectrice de nouveaux trithiagermatranes, trithiasilatranes, oxyde et sulfure germaniés à substituant chlorhydrate de cystéamine et N(2-thioéthyl)-1,3-diaminopropane

Resume De nouvelles structures organogermaniees et siliciees des types: trithiagermatranes ou trithiasilatranes, bicyclodithiazagermolidines et 6-aza, 1,3-dithia, 2-germaperhydrocines a ligands chlorhydrates de cysteamine et de N(2-thioethyl)-1,3-diaminopropane et oxyde ou sulfure de germanium a substituant chlorhydrate de N(2-thioethyl)-1,3-diaminopropane ont ete synthetisees. Leur toxicite aigue et leur activite radioprotectrice ont ete determinees.

Polymethylenedioxy bis(2-hydroxyiminomethylpyridinium) as in vitro reactivators of organophosphorous inhibited eeL acetylcholinesterase

The synthesis and in vitro AChE reactivating potency of 5 new bridged pyridinium-2 carbaldoximes are described. Tested as reactivators and protectors in vitro against 5 organophosphorous inhibitors, they show a particularly interesting activity against paraoxon and tabun. These oximes themselves are reversible AChE inhibitors.

A REVIEW ON THE RADIOPROTECTIVE ACTIVITY OF ORGANOGERMANIUM AND ORGANOSILICON COMPOUNDS

The present review describes the work carried out during the last 20 years in the field of the radioprotective activity and toxicity of several classes of organosilicon and organogermanium compounds (i.e. metallathiazolidines, metalladithioacetals, metallatranes and germathianes).

Production and characterization of antibodies directed against organophosphorus nerve agent VX

A strategy is described to raise high-affinity antibodies directed against the organophosphorus nerve agent VX [O-ethyl S-(2(diisopropylamino)ethyl)methyl phosponothionate]. Ten chemical derivatives of VX (haptens) have been synthesized. Their structures differ principally from VX structure by substitution of S-atom by an O-atom or CH2-group and by introduction of a reactive group (carboxylic acid, arylamine or primary amine) on the O-ethyl side chain. None of these haptens, except one, exhibit potential toxicity as tested by their inhability to inhibit acetylcholinesterase (E.C. 3.1.1.7.). After coupling with a protein carrier, they were injected intradermally to rabbits. Nine of these immunogenic conjugates led to the appearance of antibodies able to bind VX in a competitive solid phase immunoassay. The apparent titer and affinity of the antisera differed greatly depending on the hapten used. The highest affinity (9 nM) was observed with the VX derivative bearing O-S substitution and O-ethyl-carboxylic side chains. The antibodies appear specific for VX, since cross-reactivity with other nerve agents (Soman, Sarin or Tabun) was low. However, two haptens elicited antibodies with affinity to Soman or Sarin in the micromolar range. Antibodies were able to neutralize VX inhibition of acetylcholinesterase in vitro but not in vivo.

New organogermylated compounds N-substituted by naphthylmethylimidazoline hydrochloride, and imidazoline: synthesis and radioprotective activity

Abstract This work concerns the synthesis and pharmacological study (toxicity, radioprotective activity) of the N -substituted organogermylated compounds by naphthylmethylimidazoline hydrochloride and imidazoline. These new organometallic derivatives have quite low toxicity and sometimes higher radioprotective activity (compared with hydrochlorides of naphthylmethylimidazoline and imidazoline).

Radioprotective effect of low doses of 2-(1-naphthylmethyl)-2-imidazoline alone or associated with phosphorothioates

In the mouse, the intraperitoneal injection of 2-(1-naphthylmethyl)-2-imidazoline has a radioprotective effect even at low low doses. Its association with S-[2-(3-aminopropyl)aminoethyl] phosphorothioate (WR 2721) or S-[3-(3-methylaminopropyl)-amino-propyl]phosphorothioate (WR 151327) at low doses led to an enhancement of their respective radioprotective activities without any apparent side effects. These results strengthen the interest of this non-sulphur compound as a radioprotector.