Three novel amido-alcohols were synthesized on the base of the camphane scaffold. Natural amino acids were transformed into their -hydroxy analogues with retention of configuration, and attached to bornylamine. The compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv. The activity shifts from micromolar to nanomolar inhibitory concentrations depending o...

Artificial, therapeutic pneumothorax was commonly used to treat tuberculosis (TB) prior to the development of antimycobacterial agents. Recent reports1-2 suggested that therapeutic pneumothorax is efficacious. In 1820, James Carson suggested therapeutic pneumothorax for TB,3 and Carlo Forlanini began to apply it in clinical practice in 1888.4 Therapeutic pneumothorax evolved from the idea that ...

Buruli ulcer (BU), caused by Mycobacterium ulcerans, was recently recognized by the World Health Organization as an important emerging disease. While antimycobacterial therapy is often effective for the earliest nodular or ulcerative lesions, medical management of BU lesions in patients presenting for treatment is usually disappointing, leaving wide surgical excision the only alternative. Advan...

We demonstrated previously that susceptibility testing of Mycobacterium tuberculosis could be accomplished within 24 h after the organisms were incubated with antituberculosis agents by using fluorescein diacetate (FDA) staining and flow cytometry. Continued studies have now shown that assay suspensions containing M. avium, M. fortuitum, M. gordonae, or M. marinum incubated with various concent...

A series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. The 4-amino-1,2,4-triazole-5-thione analogues (Ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. Reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivat...

A series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. The 4-amino-1,2,4-triazole-5-thione analogues (Ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. Reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivat...

BACKGROUND Tuberculosis (TB) is a serious public health problem worldwide. Mycobacterium tuberculosis (M. tuberculosis) grows as drug tolerant pellicles. Agents that inhibit biofilm formation in M. tuberculosis have the potential to reduce the disease treatment period and improve the quality of tuberculosis chemotherapy. Parinari curatellifolia (P. curatellifolia) leaf extracts are claimed to t...

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...