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Biomedical subjects

S Grasso

Publications and source records attributed to S Grasso.

At least 181 records · Page 10Linked to original sources
PubMedDate not supplied

Anti-HIV agents II. Synthesis and in vitro anti-HIV activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles.

A series of 1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles was synthesized starting from o-phenylenediamine, disubstituted aromatic aldehydes and 2-mercaptoacetic acid. Their antiviral activity against human immunodeficiency virus (HIV) was explored: the 1-(2',6'-dichlorophenyl) (4c), 1-(2',6'-difluorophenyl) (4i), 1-(2'-chloro,6'-fluorophenyl) (4K) and 1-(2'-chloro,5'-nitrophenyl) (4m) derivatives significantly inhibit in vitro the viral cytopathic effect in HIV-infected CEM cells. Compound 4i was selected by NCI's Review Committee for initial preclinical development studies.

Antiviral Agents↗
PubMedDate not supplied

Synthesis and anticonvulsant properties of 3-(1,3,4-thiadiazol-2-yl) thiazolidin-4-ones.

A series of 2-substituted 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-ones were synthesized and evaluated for anticonvulsant activity in a genetic model of reflex epilepsy (sound-induced seizures in DBA/2 mice). The combination of preferred substituents in the 2-position coupled with the introduction of a mercapto group on the thiadiazole moiety led to a number of active compounds. The anticonvulsant activity of most derivatives is better than that of the clinically useful anticonvulsant sodium valproate and some of them appear to possess potencies in the same range as phenytoin and clobazam.

Acoustic Stimulation↗