title: Synthesis of new 3,4,5-trisubstituted isothiazoles as effective inhibitory agents of enteroviruses.
abstract: The synthesis and evaluation of 3,4,5-trisubstituted isothiazoles as antiviral agents led to the discovery of several compounds effective in vitro against enteroviruses polio 1 and ECHO 9. Structure-activity relationship studies revealed that a short thioalkyl chain in the 3-position and a methyl ester group in the 4-position are the structural components that, to a large extent, contribute to the positive biological profile in terms of both selectivity and low cytotoxicity. Under one-step growth conditions, methyl 3-methylthio-5-phenyl-4-isothiazolecarboxilate caused the greatest activity if added within 1 h after poliovirus adsorption. These data suggest interference with early events of viral replication.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Catania, Italy.
authors.forename: C C
authors.initials: CC
authors.lastname: Cutrì
authors.forename: A
authors.initials: A
authors.lastname: Garozzo
authors.forename: M A
authors.initials: MA
authors.lastname: Siracusa
authors.forename: M C
authors.initials: MC
authors.lastname: Sarvà
authors.forename: A
authors.initials: A
authors.lastname: Castro
authors.forename: E
authors.initials: E
authors.lastname: Geremia
authors.forename: M R
authors.initials: MR
authors.lastname: Pinizzotto
authors.forename: F
authors.initials: F
authors.lastname: Guerrera
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology; D004770:Enterovirus / Q000187:drug effects*; D029822:Enterovirus B, Human / Q000187:drug effects; D008956:Models, Chemical; D017955:Poliovirus / Q000187:drug effects; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D000998:Antiviral Agents; D013844:Thiazoles