Synthesis and Analgesic Properties of Lidocaine Derivatives with Substituted Aminobenzothiazoles

Author(s): Abbas Ahmadi, Mohsen Khalili, Mohammad Kazem Mohammadinoude, Babak Nahri-Niknafs

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 19 , Issue 6 , 2016


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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.

Keywords: Lidocaine, local anesthetics, aminobenzothiazole, acute and chronic pains, tail immersion and formalin tests.

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Article Details

VOLUME: 19
ISSUE: 6
Year: 2016
Published on: 16 May, 2016
Page: [507 - 512]
Pages: 6
DOI: 10.2174/1386207319666160517115310
Price: $65

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