4.4 Article

Synthesis of novel (-)-Camphene-based thiosemicarbazones and evaluation of anti-Mycobacterium tuberculosis activity

Journal

NATURAL PRODUCT RESEARCH
Volume 33, Issue 23, Pages 3372-3377

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2018.1478829

Keywords

(-)-camphene; thiosemicarbazones; Mycobacterium tuberculosis; cytotoxicity

Funding

  1. CNPq [311615/2012-0, 508857/2010]
  2. Fundacao Araucaria [15787/2008]
  3. Capes

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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 H(37)Rv, 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??g/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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