A series of novel substituted benzimidazole (7a -n) derivatives were synthesized and characterized by 1 H, 13 C Nuclear Magnetic Resonance (NMR) spectra and High Resolution Mass Spectrometry (HRMS). The substitution was done in position -1 and -2 by appropriate groups. These compounds are obtained by N-alkylation reaction with thiomethyl-1H-benzimidazole intermediates (5a -g). Design of intermediates (5a -g) was made by condensation reaction between 2-methylbenzimidazole thiourunium salt (3) and functionalized halides (4) in the presence of sodium hydroxide (NaOH). Among the twenty-one compounds synthesized, ten were evaluated for their antimicrobial activity on three bacterial strains namely: Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853. Only E. coli ATTC 25922 was susceptible to the synthesized derivatives 5g, 7f and 7h with a significant antibacterial activity (CMI is between 250 and 500 μg/mL).

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A series of 2-(benzylthio)pyrimidines (6a-l) and 2-(benzimidazolylmethylthio)pyrimidines derivatives (6m and 6n) analogues of ethyl 2-(benzylthio)-6-methyl-4-phenyl-1,4-dihydropyrimidine-5-carboxylates and ethyl 2-(((1H-benzimidazol-2-yl)methyl)thio)-6-methyl-4-phenyl-1,4-dihydropyri-midine-5-carboxylates were prepared and evaluated for antibacterial activity. These compounds were obtained by condensation of 2-thiopyrimidines (4) with benzyl halides or 2-(chloromethyl)-1H-benzimidazole (5) in the presence of a base. All compounds were characterized by 1 H, 13 C and HRMS spectra. Out of fourteen, only eight compounds were screened against multi-resistant strains of Escherichia coli and Staphylococcus aureus. The results revealed that all of them were found to possess significant antibacterial activity against the germs tested. Compounds 6c, 6d, 6h and 6m were more active on S. aureus and compounds 6h and 6m more active on E. coli.

Two sterols namely β-sitosterol (1) and stigmasterol (2) were isolated from methanolic extract of the fruit barks of Coelocaryon klainei Pierre ex Heckel (Myristicaceae). They were isolated for the first time from this species. It is the first isolation of compounds in this genus Coelocaryon. The structures were elucidated on the basis of one and two-dimensional NMR, SM, IR and UV.Akoubet et al., International Current Pharmaceutical Journal, August 2017, 6(9): 49-52http://www.icpjonline.com/documents/Vol6Issue9/01.pdf