Synthesis and in vivo evaluation of novel benzimidazole‐sulfonamide hybrids and Lucilia cuprinamaggots' excretion/secretion topical gels for wound healing

Autor: Sayed, Asmaa M., Saleh, Nashwa M., El‐Gaby, Mohamed S. A., Abdel‐Samad, Mohammad R. K., Taher, Fatma A.
Zdroj: Journal of the Chinese Chemical Society; July 2021, Vol. 68 Issue: 7 p1291-1301, 11p
Abstrakt: A novel series of benzimidazole‐sulfonamide hybrids (6a–g) was designed, synthesized, and their structures were characterized by 1H NMR and 13C NMR spectral data. Further, all compounds were evaluated for their antibacterial effects. The synthesized benzimidazole‐sulfonamide hybrid (6d) showed the highest antibacterial activity against Staphylococcus aureus, Staphylococcus epidermis, Escherichia coli, and Klebsiella pneumonia. Different gel formulations for 6dwere prepared and physically investigated. After in vivo evaluation for wound healing, the 6dgel formulation delayed the wound healing in animal model. But interestingly, a combination of 6dand Lucilia cuprinamaggots' excretion/secretion showed remarkable enhancement in wound healing compared with 6donly. This combination opens up promising prospects for wound healing formulations. N‐(4‐substituted sulfamoylphenyl)‐1H‐benzo[d]imidazole‐2‐carbohydrazonoyl‐cyanide series were synthesized by coupling of diazotized 4‐aminobenzenesulfonamides with 2‐cyanomethylbenzimidazole in the presence of sodium acetate. This series wes tested against some bacterial strains, and the compound 6dderivative showed the best antibacterial activity. In vivo, the sulfonamide 6dgel derivative delayed the wound contraction, while its activity was enhanced by combination with excretion/secretion of Lucilia cuprinamaggots.
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