Synthesis and local anesthetic activity of alkylaminoacyl derivatives of 2-amino-1,3,4-thiadiazole.
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.
Mazzone
G
G
Cattedra di Tecnica e Legislazione Farmaceutica, Università di Catania, Italy.
Pignatello
R
R
Mazzone
S
S
Panico
A
A
Pennisi
G
G
Castana
R
R
Mazzone
P
P
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*
D000779:Anesthetics, Local; D013830:Thiadiazoles; C010852:2-amino-1,3,4-thiadiazole