Institute of Pharmaceutical Chemistry, University of Szeged, Interdisciplinary Excellent Center, Eötvös utca 6, H-6720 Szeged, Hungary.
Stereochemistry Research Group of the Hungarian Academy of Sciences, Eötvös utca 6, H-6720 Szeged, Hungary.
Int J Mol Sci. 2021 May 26;22(11):5626. doi: 10.3390/ijms22115626.
Discovery of novel antibacterial agents with new structures, which combat pathogens is an urgent task. In this study, a new library of (+)-neoisopulegol-based -benzyl derivatives of aminodiols and aminotriols was designed and synthesized, and their antimicrobial activity against different bacterial and fungal strains were evaluated. The results showed that this new series of synthetic -benzyl compounds exhibit potent antimicrobial activity. Di--benzyl derivatives showed high activity against Gram-positive bacteria and fungi, but moderate activity against Gram-negative bacteria. Therefore, these compounds may serve a good basis for antibacterial and antifungal drug discovery. Structure-activity relationships were also studied from the aspects of stereochemistry of the -benzyl group on cyclohexane ring and the substituent effects on the ring system.
发现具有新结构的新型抗菌剂以对抗病原体是一项紧迫的任务。在这项研究中，设计并合成了基于(+)-异胡薄荷醇的新型氨基二醇和氨基三醇的 -苄基衍生物文库，并评估了它们对不同细菌和真菌菌株的抗菌活性。结果表明，这一系列新型合成 -苄基化合物表现出很强的抗菌活性。二 -苄基衍生物对革兰氏阳性菌和真菌表现出高活性，但对革兰氏阴性菌表现出中等活性。因此，这些化合物可能为抗菌和抗真菌药物的发现提供良好的基础。还从环己烷环上 -苄基的立体化学和环系统上取代基的影响等方面研究了构效关系。
