N.F. Salakhutdinov

New possibilities of isoprenoids chemistry when using a heterogeneous catalyst: Askanite—bentonite clay

Abstract We showed that new heterocyclization reactions resulting in the compounds of a unique structure and a potential biological activity proceed when hydroxyolefins of menthane and carane seriies are allowed to react with salicylaldehyde 1 on askanite—bentonite clay at room temperature. Slight changes in isoprenoid structure yield significantly different reaction products.

Untargeted search and identification of metabolites of antiviral agent camphecene in rat urine by liquid chromatography and mass spectrometry and studying their distribution in organs following peroral administration of the compound

Graphical abstract Figure. No Caption available. HighlightsMajor metabolites of a new antiviral agent camphecene were found and identified by HPLC‐MS method followed by multivariate statistical analysis.Camphecene glucuronide, sulfate and iminoacid were found to be the metabolites excreting with urine along with intact compound.Distribution of camphecene and its metabolites in liver, kidney, lungs and brain after peroral administration to rats was studied. ABSTRACT Major metabolites of camphecene, a new effective antiviral agent, formed after its oral administration to rats and excreted in the urine, were found and identified using liquid chromatography coupled to mass spectrometry as well as multivariate analysis of HPLC‐MS data. The metabolites were found to be camphecene glucuronide, camphecene sulfate and the corresponding iminoacid. A study of the dynamics of accumulation of camphecene and its metabolites in the liver, kidneys, lungs and brain of animals was performed. Maximum concentration of camphecene in blood and organs was reached after 1.5–2 h of its administration, and the maximal content of the agent in the organs investigated was observed in the kidneys. The content of the substance in the lungs was comparable to that in the liver. Also, camphecene was found in brain in high concentration, thus allowing assumption of its ability to penetrate the blood‐brain barrier and to exert its antiviral properties in the organ. Camphecene glucuronide and iminoacid had concentration‐time profiles similar to that of their precursor, their content being maximal in kidney and liver and 2–3 orders of magnitude higher than in lungs and brain. The content of camphecene sulfate was of similar level in all organs studied. The results obtained made it possible to develop recommendations for therapy with the use of camphecene.

Cytotoxic and cancer preventive activity of benzotrithioles and benzotrithiole oxides, synthetic analogues of varacins

The cytotoxic and cancer preventive activities of synthetic analogs of natural varacins with polysulfide groups were studied. Presence of a sulfoxide group was found to have no significant effect on the cytotoxicity of these compounds. At the same time, this group is important for inhibition of colony formation of tumor cells treated with tumor promoter thus demonstrating cancer preventive activity. The most promising compound appears to be a synthetic varacin C analog, sulfoxide 10a, which exhibits the cancer preventive activity at dose into 100 times lower than its cytotoxic concentrations.