Synthesis and pharmacological activity of new N,N′,N″-substituted guanidines

New potential antihypoxants based on 2-ethyl-3-(N,N-dimethylcarbamoyloxy)-6-methylpyridine

“…A new structural analog of mexidol is 2-ethyl-3-(N,N-dimethylcarbamoyloxy)-6-methylpyridine succinate [3], which has higher antihypoxic activity than emoxypin and mexidol. This compound under the name proxypin (Ia) was entered into clinical trials as a neuroprotectant for ischemic brain disease.…”

“…HX=HCl, Emoxypin HX=0.5 HOOC(CH 2 ) 2 COOH, Mexidol, mexiprim HX=0.5 HOOC(CH 2 ) 2 COOH, Proxypin (Ia), HX=HCl (Ib) Proxypin (Ia) is produced from the available sylvan (II) according to the scheme below [3,4].…”

Access to N-Carbonyl Derivatives of Iminosydnones by Carbonylimidazolium Activation

“…This is particularly true when derivatization of the exocyclic nitrogen (N6) is required. The current functionalizations on this position are amides, carbamates, sulfonamides, and ureas, whereas thiourea, phosphoramide, and guanidine derivatives are only sporadically reported. The most utilized strategy for N6 substitution is the addition of strong electrophiles (carbonates, chloroformates, or isocyanates) on ImSyd salts under slightly basic conditions (Scheme a) .…”