E. Ya. Lukevits

Derivatives of aziridine-1,2-dicarboxylic acid

The corresponding esters and amides of aziridine-1,2-di-carboxylic acid were obtained by the reaction of esters and amides of aziridine-2-carbocylic acid with esters and amides of chlorocarbonic acid, isocyanates, and isothiocyanates. The reaction of 2-methoxycarbonylaziridine with diisocyanates and chlorides of the dicarboxylic acids leads to the formation of bisaziridines.

X-ray structural investigation of novel azabicyclic systems containing aziridine rings

Successive conversion reactions of methyl aziridine-2-carboxylate have been used to prepare novel azabicyclic derivatives, namely, 2-carbamoylmethyl-1,3-diazabicyclo [3.1.0]hexan-4-one and 2,2-dimethyl-1,3,4-triazabicyclo[4.1.0]heptan-5-one, whose structures were established unequivocally by x-ray structure analysis.

N- and O-carbamoyl and thiocarbamoyl derivatives of B-lactam antibiotics

New N-acylureido and N-acylthioureido derivatives of β-lactam antibiotics were obtained by the reaction of 6-ureido and 6-thioureidopenicillanic and 7-thioreidodeacetoxycephalosporanic acids with acyl halides of carboxylic acids and benzoyl isocyanate. 6-Carbamoylhydroxypenicillanic acid, 6-thiocarbamoyl-hydroxypenicillanic acid, and its trichloroethyl ester were obtained by treatment of 6-α-hydroxypenicillanic acid and its trichloroethyl ester with isocyanatosilanes with subsequent hydrolysis of the N-silylcyanato groups.

Nitrogen-containing organosilicon compounds. CXXII. Synthesis and pharmacological studies of trialkylsilylalkylaminoethyl dicarboxylate methiodides

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Synthesis and biological activity of semisynthetic silicon-containing penicillins and cephalosporins

The structure of the obtained compounds was confirmed by elemental analysis and spectrometry. UV spectra of the semisynthetic cephalosporins contain a characteristic absorption band in the 260-262 nm region. Three bands were detected in the IR spectra of penicillins and cephalosporins in the region of 1610-1600, 1690-1670, and 1780-1770 cm-: assigned to carbonyl stretching vibrations of amide, ionized carboxyl, and 8-1actam groups, respectively. In addition to the chemical shifts of protons of 8-1actam, thiazolidine, and A3-dihydrothiazine rings a multiplet of type AsBm was observed in the PMR spectra of the antibiotics which was characteristic for protons of ethyl groups linked to silicon.

Nitrogen-containing organosylicon compounds. LXI. Cybernetic analysis of the interrelationship between the structure and antimicrobial activity of organosilicon amines

In an investigation of the antimicrobial activity of organosilicon amines [1-4] we observed that compounds containing methyldibutylsilyl groupings in the y position relative to the nitrogen atom have high fungistatic activity. Having a large collection of data on the antimicrobial activity of primary, secondary, and tertiary aliphatic and heterocyclic organosilicon amines (128 compounds and four test microbes), we decided to subject them to cybernetic analysis under conditions of active interaction of the investigator and the computer in order to establish more general dependences between the structure and the composition and statistically evaluating the exposed regularities.