A.M. Butlerov Chemical Institute, Kazan Federal University, Kremlevskaya, 18, 420008 Kazan, Russia.
Federal State Budgetary Scientific Institution, Federal Center for Toxicological, Radiation, and Biological Safety, Nauchny Gorodok-2, 420075 Kazan, Russia.
Org Biomol Chem. 2023 Jun 14;21(23):4863-4873. doi: 10.1039/d3ob00528c.
Terpenes and their derivatives are natural antifungal and antimicrobial agents. In this paper, potential antifungal agents were developed on the basis of farnesol, geraniol, myrtenol, perillyl alcohol, cedrol and phytol. The synthesized compounds exist in aqueous solutions as stable associates ( = 142-216 nm, PDI 0.04-0.16, = +0.9-+46 mV). Formation of stable associates of the compounds in solution promotes compaction and dosed release of the drug. The membranotropic activity of the compounds was also investigated to open up their possible application in the treatment of skin diseases. The relationship between membranotropism and lipophilicity coefficient (log ) has been established. The antifungal and antimicrobial activities of the obtained compounds were studied on the clinical isolate of sp., , yeast , Gram-negative () and Gram-positive (, ) bacteria. sp. (0.0781 mg mL) and (0.0049 mg mL) showed the highest sensitivity to the agents.
萜类化合物及其衍生物是天然的抗真菌和抗菌剂。在本文中，以法呢醇、香叶醇、桃金娘醇、紫苏醇、雪松醇和植醇为基础开发了潜在的抗真菌剂。合成的化合物在水溶液中作为稳定的缔合物存在（= 142-216nm，PDI 0.04-0.16，= +0.9-+46mV）。化合物在溶液中形成稳定的缔合物促进了药物的压缩和定量释放。还研究了化合物的膜转导活性，以开辟其在皮肤病治疗中的可能应用。已经建立了膜转导性和脂溶性系数（log）之间的关系。研究了所得化合物对临床分离株 sp.、、酵母、革兰氏阴性（）和革兰氏阳性（、）细菌的抗真菌和抗菌活性。 sp.（0.0781mgmL）和 （0.0049mgmL）对这些药物表现出最高的敏感性。
