WuXi AppTec, Wuhan, Hubei, PR China.
WuXi AppTec, Wuhan, Hubei, PR China.
Eur J Med Chem. 2019 Feb 1;163:404-412. doi: 10.1016/j.ejmech.2018.12.001. Epub 2018 Dec 3.
Tetrazole, a bioisostere of the carboxylic acid group, can replace the carboxyl group in drugs to increase the lipophilicity, bioavailability and reduce side effects. Tetrazole derivatives possess a broad-spectrum of biological properties including anti-tubercular and anti-malarial activities, and some tetrazole-based compounds have already been used in clinics for the treatment of various diseases. Therefore, tetrazole is an important pharmacophore in the development of new drugs. This review covers the recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents, and the structure-activity relationship is also discussed for the further rational design of tetrazole derivatives.
四唑是羧酸基团的生物等排体，可以替代药物中的羧基，增加亲脂性、生物利用度并降低副作用。四唑衍生物具有广泛的生物学特性，包括抗结核和抗疟疾活性，一些基于四唑的化合物已在临床上用于治疗各种疾病。因此，四唑是开发新药的重要药效团。本综述涵盖了四唑衍生物作为潜在抗结核和抗疟药物的最新进展，并讨论了构效关系，以进一步合理设计四唑衍生物。
