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In this work the aim of study was the synthesis and evaluation of in vitro anti-Mycobacterium tuberculosis activity as well as the cytotoxicity in VERO cells of a series of 17 novel thiosemicarbazones derived from the natural monoterpene (-)-camphene by REMA and MTT methods. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of M. tuberculosis HRv, especially the derivatives 3, 4a-c, 4f, 4i, 4k, 5 and 6a-b. MIC values of 20 tested compounds ranged from 3.9 to > 250 μg/mL. It was found that when inserting new nitrogenous groups to the (-)-camphene increased the anti-M. tuberculosis activity of some compounds. The SI was calculated for all compounds that showed highly potent anti-M. tuberculosis activity and the best SI values were 21.36, 26.92 and 31.62 (4b, 6a and 6b), and may be considered potential candidates for future antituberculosis drugs.

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Aim: To evaluate the potential of three benzohydrazones (1–3), four acylhydrazones derived from isoniazid (INH-acylhydrazones) (4–7) and one hydrazone (8) as antituberculosis agents. Materials & methods: Inhibitory and bactericidal activities were determined for the reference Mycobacterium tuberculosis ( Mtb) strain and clinical isolates. Cytotoxicity, drug combinations and ethidium bromide accumulation assays were also performed. Results: The tested compounds (1–8) presented excellent antituberculosis activity with surprisingly inhibitory (0.12–250 μg/ml) and bactericidal values, even against multidrug-resistant Mtb clinical isolates. Compounds showed high selectivity index, with values reaching 1833.33, and a limited spectrum of activity. Some of the compounds (2 & 8) are also great inhibitors of bacillus efflux pumps. Conclusion: Benzohydrazones and INH-acylhydrazones may be considered scaffolds for the development of new anti- Mtb drugs.

Natural products are great prototypes for the development of new compounds with pharmacologic properties. In this work, the monoterpene R-(+)-limonene was used to obtain a series of 1,3,4-thiadiazoles and their antitumor and antileishmania activities against Leishmania amazonenses were investigated. The analogous 4-methyl (4b) was potentially active against melanoma tumor cells (UACC-62), while the derivative 4-methoxy (4c) and 4-dimethylamino (4d) were the most active against L. amazonensis.

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