engleski

Antimycobacterial activity of harminices, harmine derived triazoles

Tuberculosis (TB) remains one of the major golbal health problems with 10 million new cases (1 million children) in 2017. In 2017 TB was one of the top 10 causes of death worldwide killing 1.3 million people, ranking above HIV/AIDS as the leading cause of death from an infectious disease (1). New treatment options are urgent in order to resolve some of the major issues in current anti-TB therapy ; the emergence of multidrug-resistant (MDR-TB) and extensively drug resistant (XDR-TB) strains which require prolonged and complex treatment and toxicity. The efforts in antimycobacterial drug discovery in the last decade resulted in two new oral drugs for the treatment of TB, delamanid and bedaquiline (2). β-Carbolines such as hamine and harmole are alkaloids found in Peganim harmala and Eurycoma longifolia plants. They have been evaluated extensively for various pharmacological activities, including antimycobacterial (3). Their various synthetic analogues have been prepared and tested for antimycobacterial activity as well (4, 5). We have prepared 26 derivatives of triazole bridged harmine/harmole and cinnamyl moiety. Here we report the results of the antimycobacterial screening. Minimum inhibitory concentrations (MIC) were determined in Mycobacterium tuberculosis H37Rv, a virulent strain, by using the resazurin reduction microplate assay. Further evaluations are necessary to investigate the toxicological properties and the potential of 8g or 8h as new anti-tuberculosis drug candidate.

harmine, cinnamic acid, 1, 2, 3-triazole, synthesis

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