Domiodol; separation of cis and trans isomers and comparison of their pharmacological activity.

Cis and trans isomers of 2-iodomethyl-4-hydroxymethyl-1,3-dioxolane (domiodol, MG 13 608) were separated by preparative GLC and prepared on a larger scale by previous resolution of an intermediate. Acute toxicity and effect on respiratory tract excretion were evaluated for domiodol and for each isomer: no significant differences were found.

[Preparation and pharmacological activity of N6, 02-dipivaloyl-cyclic AMP]. / Preparazione e attività farmacologiche del N6,O2'-dipivaloil-AMPc.

The synthesis of N6,O2'-dipivaloyl-cyclic AMP is described with some pharmacological tests made in comparison with the dibutyryl homolog. The two compounds proved equally active in increasing glycemia in the rabbit whereas the dipivaloyl derivative is less effective in counteracting contractions induced by imidazole in the isolated guinea-pig trachea.

[Synthesis and antibacterial activity in vitro of some penicillins containing the phenylcyclohexanie residue]. / Sintesi e attività antibatterica in vitro di alcune penicilline contenenti il residuo fenilcicloesanico

Some penicillins with structures similar to that of ampicillin and cyclacillin bearing the phenylcyclohexane grouping were prepared. In vitro tests of antibacterial activity showed that the introduction of this residue led to reduced activity in comparison with that of the parent compound.

[Isoxazolylpenicillins with cycloaliphatic substituents in the isoxazole ring]. / Isossazolilpenicilline con sostituenti cicloalifatici nel nucleo isossazolico

Some derivatives of oxacillin were prepared containing in place of the phenyl group a cyclohexyl, cyclohexylphenyl, phenylcyclohexyl or diphenylyl moiety. In the same compounds a methylene bridge between the carboxy group and the heterocyclic ring was inserted. The results of in vitro evaluation of antibacterial activity are given.