Abstract
The aim of the present study is to synthesize cationic salts from a relatively toxic compound named 2-mercaptobenzimidazole and to evaluate some of their pharmacological properties. The acute toxicity of these salts is evaluated according to OECD 423 Guidelines at the doses of 300 and 2000 mg/kg; their peripheral analgesic effect is studied using the Koster test at the therapeutic dose of 200 mg/kg and their sedative action is evaluated using Traction, Chimney, Hole-board, and Rotarod tests at the doses of 200 and 400 mg/kg. All synthesized molecules show no acute toxicity according to OECD Code 423 guidelines at doses ranging from 300 to 2000 mg/kg and do not cause any obesity or anorexia. Also, the results of the Koster test show that the studied compounds have an average analgesic effect at the dose of 200 mg/kg compared to acetylsalicylic acid. In addition, the elaborated compounds have shown a moderate sedative effect at the dose of 400 mg/kg, in comparison to 2-mercaptobenzimidazole (400 mg/kg) and Bromazepam (20 mg/kg). These compounds have no cataleptic and hypnotic effects on the central nervous system at the doses of 200 and 400 mg/kg. These results argue in favor of a possible integration of the most active salts tested in the pharmaceutical industry owing to their analgesic and sedative effects.
Highlights
Heterocyclic organic chemistry accounts for a large part of organic chemistry research conducted around the world
All synthesized 2–5 molecules show no acute toxicity according to OECD Code 423 guidelines at doses ranging from 300 to 2000 mg/kg (Scheme 2). is could be related to the weight of these molecules, which would influence their bioavailability in the body and the total dose acting on the animal
For this test, impaired motor coordination and impaired tensile force were observed in animals dosed with 400 mg/kg of 2-mercaptobenzimidazole 1 (Table 3). is is manifested by the falls of all the animals used with an average time of fall of 10.38 ± 0.14 s. is observation indicates that this product has a strong sedative effect at this dose on the central nervous system
Summary
Heterocyclic organic chemistry accounts for a large part of organic chemistry research conducted around the world. E literature reports a large body of work showing that benzimidazole derivatives are Biochemistry Research International good corrosion inhibitors [31,32,33]. For example, mention the benzodiazepines marketed for their psychotropic effects on the central nervous system (Bromazepam, Diazepam, Clobazam, and Prazepam) and the benzimidazoles sold for their antihelminthic, antisecretory gastric, and antipsychotic effects (Mebendazole, Flubendazole, Timoprazole, Lanzoprazole, and Pimozide): these are biologically active nitrogenous heterocycles. It is with this in mind that Latyfa El Ouasif et al [34, 35] synthesized 2-mercaptobenzimidazole derivatives, in the form of dialkyl derivatives and surfactants, to study their antioxidant and antimicrobial activities and their corrosion inhibiting ability. The long-chain benzimidazolium constitutes a very interesting family of cationic amphiphiles whose structure and the nature of the counterion can be modulated. is makes them interesting for biological and especially pharmacological applications
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