The invention discloses an iso-cryptolepine analogue as well as a preparation method and application thereof. The
chemical structure of the iso-cryptolepine analogue is shown as a formula I, wherein a
substituent group R in the formula I can be independently -H, -OCH3, -F, -Cl or -SO2NH2. According to the isocryptolepine analogue disclosed by the invention, enoxacin is taken as a
raw material, so that effective chemical construction from a fluoroquinolone structure to an indolonaphthyridine skeleton is realized, and a new way for structural modification of isocryptolepine is expanded. By means of the method, the complementary
advantage structures of fluoroquinolone medicines and natural indoloquinoline alkaloids are achieved, the anti-
tubercle bacillus activity and the anti-
drug resistance of the compound are improved, the
toxicity to normal cells is reduced, and the compound can be further developed as an anti-
tubercle medicine with a brand new structure.