Benzofuran is a fundamental structural unit in a variety of biologically active natural products, and its derivatives display various biological properties. Some benzofuran derivatives possess unique anti-tubercular and anti-bacterial action mechanism, and exhibit excellent in vitro and in vivo activities against both drug-sensitive and drug-resistant pathogens. Moreover, several benzofuran derivatives have already used in clinics for the treatment of various diseases. Thus, benzofuran is a useful pharmacophore to develop new anti-tubercular and anti-bacterial drugs. This review covers the recent advances of benzofuran derivatives as potential anti-tubercular and anti-bacterial agents, and the structure-activity relationship is also discussed to pave the way for the further rational development of this kind of derivatives.

苯并呋喃是多种具有生物活性的天然产物的基本结构单元，其衍生物具有多种生物学特性。一些苯并呋喃衍生物具有独特的抗结核和抗菌作用机制，并在体外和体内均表现出优异的性能。针对药物敏感和耐药病原体的活性。而且，几种苯并呋喃衍生物已经在临床上用于治疗各种疾病。因此，苯并呋喃是开发新的抗结核和抗菌药物的有用药效团。本文综述了苯并呋喃衍生物作为潜在的抗结核和抗菌药物的最新进展，并探讨了结构-活性关系，为进一步合理开发此类衍生物铺平了道路。