Peptide Science Laboratory, School of Chemistry and Physics, University of KwaZulu-Natal, Durban 4001, KwaZulu-Natal, South Africa.
School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4041, KwaZulu-Natal, South Africa.
Int J Mol Sci. 2024 May 28;25(11):5883. doi: 10.3390/ijms25115883.
Peptides displaying antimicrobial properties are being regarded as useful tools to evade and combat antimicrobial resistance, a major public health challenge. Here we have addressed dendrimers, attractive molecules in pharmaceutical innovation and development displaying broad biological activity. Triazine-based dendrimers were fully synthesized in the solid phase, and their antimicrobial activity and some insights into their mechanisms of action were explored. Triazine is present in a large number of compounds with highly diverse biological targets with broad biological activities and could be an excellent branching unit to accommodate peptides. Our results show that the novel peptide dendrimers synthesized have remarkable antimicrobial activity against Gram-negative bacteria ( and ) and suggest that they may be useful in neutralizing the effect of efflux machinery on resistance.
具有抗菌特性的肽被视为克服和对抗抗微生物药物耐药性的有用工具，这是一个主要的公共卫生挑战。在这里，我们研究了树枝状大分子，它们是药物创新和开发中具有广泛生物活性的有吸引力的分子。基于三嗪的树枝状大分子已在固相全合成，并研究了它们的抗菌活性和一些作用机制的见解。三嗪存在于大量具有广泛生物活性和多种生物靶标的化合物中，可能是容纳肽的极好的分支单元。我们的研究结果表明，合成的新型肽树枝状大分子对革兰氏阴性菌（和）具有显著的抗菌活性，并表明它们可能有助于中和外排机制对耐药性的影响。
