FioCruz-Fundacao Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro-RJ, Brazil.
Curr Top Med Chem. 2019;19(8):567-578. doi: 10.2174/1568026619666190305130809.
Nowadays, tuberculosis (TB) is an important global public health problem, being responsible for millions of TB-related deaths worldwide. Due to the increased number of cases and resistance of Mycobacterium tuberculosis to all drugs used for the treatment of this disease, we desperately need new drugs and strategies that could reduce treatment time with fewer side effects, reduced cost and highly active drugs against resistant strains and latent disease. Considering that, 4H-1,3-benzothiazin-4-one is a promising class of antimycobacterial agents in special against TB-resistant strains being the aim of this review the discussion of different aspects of this chemical class such as synthesis, mechanism of action, medicinal chemistry and combination with other drugs.
如今,结核病(TB)是一个重要的全球公共卫生问题,导致了全世界数百万人与结核病相关的死亡。由于病例数量的增加以及结核分枝杆菌对所有用于治疗这种疾病的药物的耐药性,我们急需新的药物和策略,这些药物和策略能够减少治疗时间,减少副作用,降低成本,并对耐药菌株和潜伏性疾病具有高度活性。考虑到这一点,4H-1,3-苯并噻嗪-4-酮是一类有前途的抗分枝杆菌药物,特别是针对耐多药结核分枝杆菌菌株。因此,本次综述的目的是讨论该化学类别的不同方面,如合成、作用机制、药物化学以及与其他药物的联合使用。