合成茚[1,2-c]喹啉類衍生物為抗結核菌試劑

Abstract

The first-line drugs currently used for the treatment of tuberculosis (TB) infection are streptomycin, isoniazid (INH), ethambutol, pyrazinamide, and rifampicin. However, the current TB treatment regimens, although highly effective, are far from ideal. Recently, the emergence of multi-drug resistant (MDR) strains and the global human immunodeficiency virus (HIV) pandemic have created an urgent need for alternative drug treatments for Mycobacterium tuberculosis infection. Over the past few years, we have been particularly interested in the synthesis of condensed quinolines such as indeno[1,2-c]quinoline, indolo[2,3-b]quinoline, and benzofuro[2,3-b]quinoline derivatives for anti-TB and anticancer evaluations. This thesis describes synthesis of certain indeno[1,2-c]quinoline derivatives for anti-TB evaluations. Among them, compound 40c exhibited a minimum inhibitory concentration (MIC) of < 0.5 ?慊/mL which was more active the positive INH (MIC = 0.8 - 1.2 μg/mL). Compound 40c belongs to a novel structure type and was not cytotoxic against the growth of Vero cells and therefore, could serve as a potential lead for the development of novel anti-TB drug candidate.