Quinones as antimycobacterial agents

In vitro synergic effect of ²-lapachone and isoniazid on the growth of Mycobacterium fortuitum and Mycobacterium smegmatis

“…However, the MIC values obtained in this work for β-lapachone are in agreement with those obtained by D'albuquerque et al (1972) against M. smegmatis (MIC values ranging from 40-60 μg/mL). Tran et al (2004) reported the in vitro antimycobacterial of quinone derivatives against M. fortuitum and M. smegmatis. Plumbagin was the most potent synthesised quinone against M. smegmatis and M. avium, exhibiting a MIC value of 12.5 μg/mL.…”

“…Some published articles have demonstrated that quinones are active against Mycobacterium tuberculosis, Mycobacterium smegmatis and Mycobacterium avium. The mechanism of these compounds is still being investigated, although some reports have suggested that quinones stimulate oxidative stress in biological systems (Tran et al 2004, Akhtar et al 2006, Silva et al 2008.…”

“…β-lapachone is known to have a variety of pharmacological effects, including trypanocidal, moluscicidal, antifungal, antibacterial, antiviral and anticancer actions. Quinones have been reported to stimulate isoniazid activity, most likely by increasing intracellular superoxide production (Tran et al 2004, Silva et al 2008). …”

2-Arylnaphthoquinone analogues: potential anti-TB and pro-apoptotic agents

“…4 Subsequent studies, which included the synthesis and evaluation of related analogues of diospyrin 1 demonstrated the potential of this basic scaffold to be considered as an integral aspect for good antimycrobacterial activity. [5][6][7] In order to gain a better understanding of the structural features and functional parameters that are necessary for such systems to demonstrate activity, we synthesized a number of biquinone molecules in which the two quinone moieties were directly linked viz., 2 and evaluated their pro-apoptotic activities against three human cancer cells lines. In addition the demethylated analogues viz., 3 were also evaluated and demonstrated that the molecules were specific for the available cancer cell lines evaluated.…”

Synthesis of novel 2-substituted 1,4-naphthoquinones using Heck reaction in ‘green’ reaction media

“…These are associated with antidiabetic, anticancer, antimalarial, antibacterial, antiinflammatory and antifungal activities [1][2][3][4] . Various 2-substituted 1,4-naphthoquinone derivatives can be prepared with ease starting from 2-bromonaphthalene using the Heck coupling reaction 5 , followed by oxidation 6 .…”