Synthesis, local anaesthetic and antiarrhythmic activity of methyl N-(2-substituted aminopropanoyl)-3-cyanoanthranilates.
A series of methyl N-(2-substituted aminopropanoyl)-3-cyanoanthranilates (4a-i), that are structurally-related to tocainide and lidocaine, was synthesized and was found to be active when evaluated for local anaesthetic activity using the frog-foot withdrawal reflex, the guinea pig wheal derm and the rabbit corneal reflex tests. A selected numbers of the series were preliminarily evaluated for antiarrhythmic activity using CaCl2-induced arrhythmia test. Compounds 4a, 4c and 4f at lower doses completely protected the animals against the induced arrhythmias.
al-Obaid
A R
AR
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
D000779:Anesthetics, Local / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007509:Irritants / Q000633:toxicity; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D011817:Rabbits; D011894:Rana pipiens; D051381:Rats; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis* / Q000494:pharmacology
D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D007509:Irritants; D062367:ortho-Aminobenzoates