Synthesis and pharmacological screening of new phenylpiperazinepropane derivatives and their enantiomers

Enantiomers of phenylpiperazinepropane-1,2-diol derivatives were synthesized with the purpose to obtain a better antitussive activity/sedative effect ratio. (S)-isomers showed better pharmacological profiles than (R)-isomers and corresponding racemates. Among the (S)-isomers, the unsubstituted compound, levodropropizine (S(-)-3-(4-phenyl-piperazin-1-yl)-propane-1,2-diol, DF 526), has the most favourable antitussive activity/sedative effect ratio and was selected for pharmaco-toxicological evaluation.     

Synthesis and pharmacological action of some N-alkyl morpholines and their salts

The preparation is described of some 2-hydroxy-2- and 4-alkylmorpholines by ring closure of the corresponding phenacyl hydroxyalkylamines. The influence of structure upon the ring closure reaction is examined and the weak pharmacological action of the title compounds on leptazol convulsions, the autonomic nervous system and in the mouse hot-plate test is discussed in relation to the reversed esters of pethidine.     

Synthesis,antibacterial, antifungal and genotoxic activity of bis-1,3,4-oxadiazole derivatives

In the present investigation, four 1,3,4-bis-oxadiazole derivatives were synthesized as potential antimicrobial agents. The compounds are: 5,5'-dimercapto-bis-[1,3,4-oxadiazol-2-yl]propane (2a), 5,5'-dimercapto-bis-[1,3,4-oxadiazol-2-yl]butane (2b), 5,5'-dimercapto-bis-[1,3,4-oxadiazol-2-yl]octane (2c) and 5,5'-dibenzylthio-bis-[1,3,4-oxadiazol-2-yl]butane (3). The above newly synthesized compounds were investigated for their antibacterial, antifungal and mutagenic activities. The results of the biological activities revealed that the compounds 2a-c exhibited both antibacterial and antifungal activities against S. aureuss and B. subtilis. Compound 2a also showed activity against P. aeureoginosa. All the above compounds and compound 3 exhibited activity against C. albicans. Genotoxic studies showed that compound 2a had a weak base pair substitution mutagenicity but none of them exhibited a frameshift mutagenic action using Ames test.     

Synthesis and pharmacological properties of 2-aminomethyl derivatives of benzofuran

Pharmaceutical Chemistry Journal -     

Synthesis and pharmacological properties of new N-aminoalkyl-2-pyrrolidinone derivatives

The paper describes the mode of obtaining and physico-chemical properties of new 1-(beta-hydroxy-gamma-aminopropyl)-2-pyrrolidinone derivatives and their antiarrhythmic effect and the action on the circulatory system.     

Synthesis and pharmacological activity of derivatives of 3-aminomethylenindolin-2-one

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 28, No. 4, pp. 22–26, April, 1994.