title: Synthesis and Analgesic Properties of Lidocaine Derivatives with Substituted Aminobenzothiazoles.
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.
authors.affiliation: Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran; No 99, Yakhchal, Gholhak, Shariati, Tehran, Iran. ahmadikiau@yahoo.com.
authors.forename: Abbas
authors.initials: A
authors.lastname: Ahmadi
authors.forename: Mohsen
authors.initials: M
authors.lastname: Khalili
authors.forename: Mohammad Kazem
authors.initials: MK
authors.lastname: Mohammadinoude
authors.forename: Babak
authors.initials: B
authors.lastname: Nahri-Niknafs
mesh_terms: D000588:Amines / Q000737:chemistry; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry*; D004583:Electrons; D008012:Lidocaine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D051379:Mice; D010147:Pain Measurement; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D000700:Analgesics; D052160:Benzothiazoles; D008012:Lidocaine