Title:Synthesis and Analgesic Properties of Lidocaine Derivatives with Substituted Aminobenzothiazoles
VOLUME: 19 ISSUE: 6
Author(s):Abbas Ahmadi, Mohsen Khalili, Mohammad Kazem Mohammadinoude and Babak Nahri-Niknafs
Affiliation:Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran; No 99, Yakhchal, Gholhak, Shariati, Tehran, Iran.
Keywords:Lidocaine, local anesthetics, aminobenzothiazole, acute and chronic pains, tail immersion and formalin tests.
Abstract:Local anesthetics are the most widely consumed drugs in the practice of medicine which
provide a loss of sensation in a certain body part without loss of consciousness or impairment of
central control of essential functions. Lidocaine (I) is the most commonly local anaesthetic drug which
is widely used in all species due to its fabulous diffusing and penetrating properties as well as prompt
onset of surgical analgesia. In this study, new aminobenzothiazole (with many useful biological and
pharmacological properties) analogues were synthesized by changing of amine moiety of I. Both acute
and chronic pain properties of new compounds (II-VI) were studied by using the tail immersion and formalin tests on
mice and the outcomes were compared with control and lidocaine groups. According to the results, aminobenzothiazole
derivatives are better candidates than diethylamine group for replacement on amine moiety of I. Also, derivatives with
electron-withdrawing groups on this amine (V and VI) could decrease pain better than electron-donating ones (II and III)
(specially on position 6 of this amine, II and V) which may be of concern for blockade of specific sodium channels by
these new compounds.
