title: Synthesis and local anesthetic activity of alkylaminoacyl derivatives of 2-amino-1,3,4-thiadiazole.
abstract: We prepared some series of 2-(alkylaminoacyl) derivatives of 2-amino-1,3,4-thiadiazoles. Most terms were subjected to a biological screening showing a local anesthetic activity both in infiltration and trunkular tests. For some of the assayed derivatives, the activity was comparable to that of lidocaine, taken as the reference molecule. From the obtained results an acceptable relationship between some structural features and activity was drawn.
authors.affiliation: Cattedra di Tecnica e Legislazione Farmaceutica, Università di Catania, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Mazzone
authors.forename: R
authors.initials: R
authors.lastname: Pignatello
authors.forename: S
authors.initials: S
authors.lastname: Mazzone
authors.forename: A
authors.initials: A
authors.lastname: Panico
authors.forename: G
authors.initials: G
authors.lastname: Pennisi
authors.forename: R
authors.initials: R
authors.lastname: Castana
authors.forename: P
authors.initials: P
authors.lastname: Mazzone
mesh_terms: D000779:Anesthetics, Local / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D005260:Female; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000779:Anesthetics, Local; D013830:Thiadiazoles; C010852:2-amino-1,3,4-thiadiazole