Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, UP, India.
Chem Biol Drug Des. 2021 Nov;98(5):787-827. doi: 10.1111/cbdd.13934. Epub 2021 Sep 16.
Tuberculosis (TB) is an infection caused by Mycobacterium tuberculosis (Mtb) and one of the deadliest infectious diseases in the world. Mtb has the ability to become dormant within the host and to develop resistance. Hence, new antitubercular agents are required to overcome problems in the treatment of multi-drug-resistant Tb (MDR-Tb) and extensively drug-resistant Tb (XDR-Tb) along with shortening the treatment time. Several efforts are being made to develop very effective new drugs for Tb, within the pharmaceutical industry, the academia and through public-private partnerships. This review will address the antitubercular activities, biological target, mode of action, synthetic approaches and thoughtful concept for the development of several new drugs currently in the clinical trial pipeline (up to October 2019) for tuberculosis. The aim of this review may be very useful in scheming new chemical entities (NCEs) for Mtb.
结核病(TB)是由结核分枝杆菌(Mtb)引起的感染,是世界上最致命的传染病之一。Mtb 具有在宿主体内休眠并产生耐药性的能力。因此,需要新的抗结核药物来克服多药耐药结核病(MDR-TB)和广泛耐药结核病(XDR-TB)治疗中的问题,同时缩短治疗时间。制药行业、学术界和公私合作伙伴关系都在努力开发非常有效的新型结核病药物。本综述将介绍目前处于临床试验阶段(截至 2019 年 10 月)的几种新型药物的抗结核活性、生物靶点、作用机制、合成方法和开发思路,这些药物用于结核病的治疗。本综述的目的可能对设计针对 Mtb 的新化学实体(NCE)非常有用。