A series of novel 5-amino-1,3,4-thiadiazole-2-thiol and 1,3,4-thiadiazole-2,5-dithiol derivatives of benzimidazole were synthesized through nucleophilic substitution reaction of 5-substituted-2-(chloromethyl)-1H-benzimidazole, structures of the synthesized compounds were proved by spectral methods of analysis ( FT-IR, 1 H and 13 C NMR ). All the target compounds were screened for their antibacterial activity toward gram-negative (E.coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria, most of the synthesized derivatives exhibited good to moderate activity toward both Gram-positive (B. subtilis, S. aureus) and Gram-negative (E.coli, P. aeruginosa) bacteria.
Serious of some novel bis benzimidazole derivatives were designed and synthesized by nucleophilic substitution reaction of 5-(un)substituted-2-chloromethyl-1H-benzimidazole and 5-(un)substituted-2-mercapto-1H-benzimidazole in the presence of sodium in methanol. Spectral methods of analysis (FT-IR, 1H-NMR, and 13C-NMR) were used to confirm the structures of the synthesized compounds. Antibacterial activity were evaluated for most of the target compounds against four strains of bacteria including (
E.coli, P. aeruginosa
) as gram-negative bacteria and (
B. subtilis, S. aureus
) as gram-positive bacteria, the tested compounds showed various activity against both gram-negative and gram-positive bacteria used.
Two Schiff base ligands L1 and L2 have been obtained by condensation of salicylaldehyde respectively with leucylalanine and glycylglycine then their complexes with Zn(II)were prepared and characterized by elemental analyses , conductivity measurement , IR and UV-Vis .The molar conductance measurement indicated that the Zn(II) complexes are 1:1 non-electrolytes. The IR data demonstrated that the tetradentate binding of the ligands L1 and L2 . The in vitro biological screening effect of the investigated compounds have been tested against the bacterial species Staphlococcus aureus, Escherichia coil , Klebsiella pneumaniae, Proteus vulgaris and Pseudomonas aeruginosa by the disc diffusion method . A comparative study of inhibition values of the Schiff base ligands and their complexes indicated that the complexes exhibit higher antimicrobial activity than the free ligands . Zinc ions are proven to be essential for the growth-inhibitor effect. The extent of inhibition appeared to be strongly dependent on the initial cell density and on the growth medium .
A new series of benzimidazole containing Schiff base moiety has been synthesized. The reaction was achieved through cyclocondensation reaction of the substituted 1,2-phenylenediamines and amino acids (glycine, alanine and tyrosine) to gave substituted benzimidazole derivatives 1(a-f). Asian Journal of Chemistry; Vol. 30, No. 2 (2018), 381-385
EXPERIMENTALMelting points were taken in an electrically heated using Stuart SMP3 instrument and are uncorrected. FT-IR spectra were recorded on Shimadzu (FTIR-8400 S) Infrared spectrophotometer by KBr disc. The
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