On the basis of our previous results 22 salicylanilides were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. The Free-Wilson method was used to evaluate structure-antimycobacterial activity relationships. 4-Chloro-N-(4-propylphenyl)salicylamide and 5-chloro-N-(4-propylphenyl)salic...

Background. Tuberculosis (TB) is a chronic bacterial disease. Mycobacterium tuberculosis, being the leading member of the MTB complex, is the main cause of tuberculosis worldwide. Tuberculosis is managed with combination of drugs: streptomycin, isoniazid, rifampicin, ethambutol, and pyrazinamide. Over the recent past years resistance against first line antituberculous drugs has emerged rapidly ...

The development of new drugs and vaccines directed against Mycobacterium tuberculosis is severely impeded by the slow growth of this organism and the need to work under stringent biosafety conditions. These difficulties pose considerable obstacles when animal studies with M. tuberculosis are performed. We investigated whether a novel approach termed luciferase in vivo expression, using an enhan...

A series of new 2-(phenylthio) benzoylaryl hydrazones were synthesized by acid-catalyzed condensation of hydrazide 3 with corresponding aldehydes. The chemical structures of the compounds were elucidated by FT-IR, 1H-NMR and Mass spectra. All newly synthesized compounds were evaluated for their antimycobacterial activities against Mycobacterium tuberculosis H37Rv using the microplate alamar blu...

To develop novel antimycobacterial agents, a new series of thiazolidinone-azole hybrids 4a-b, 5a-b and 6-13 were designed and synthesized. Thiazolidin-4-ones (4a-b and 5a-b) were obtained by the reaction of Schiff bases and hydrazones (2a-b and 3a-b) with mercaptoacetic acid. 5-Benzylidene derivatives (6-13) were gained by treatment of 5a-b with appropriate benzaldehydes according to Knoevenage...

In the present work the pharmacological activities of SFE extracts from T. catharinensis were evaluated. The SFE extracts were obtained using supercritical CO2 plus ethanol as cosolvent (4.6 and 9.2% m/m) at pressures of 250 and 300 bar and temperatures of 35, 45, and 55oC. The crude extracts were solvent-fractionated (hexanic fraction, alkaloid, and aqueous fractions) and analyzed by Thin-laye...

A new series of antimycobacterial agents 2a–j, 3a–d, 6b–f,j, and 7b,f was designed, synthesized and evaluated for antimycobacterial activity against different mycobacterium species i.e. M. tuberculosis, M. avium, and M. intracellulare in an agar dilution method. Some of these compounds (2e, 3a–d) were highly potent with in vitro activity against M. tuberculosis H37Rv and clinical isolates (sens...

To show, as a model system, that mycobacteria can express heterologous luciferase genes and that bioluminescence can be a rapid method of measuring antimycobacterial activity, a bioluminescent form of Mycobacterium smegmatis was made by transformation with a Mycobacterium-Escherichia coli shuttle vector containing the luxAB genes from Vibrio harveyi. The antimycobacterial effects of antibiotics...

A series of new 2-(phenylthio) benzoylarylhydrazones were synthesized by acid-catalyzed condensation of hydrazide 3 with corresponding aldehydes. The chemical structures of the compounds were elucidated by FT-IR, (1)H-NMR and Mass spectra. All newly synthesized compounds were evaluated for their antimycobacterial activities against Mycobacterium tuberculosis H37Rv using the microplatealamar blu...