With the advent of multidrug-resistant Mycobacterium tuberculosis strains, new and effective therapies are rapidly needed to combat infections caused by these strains. Some new 2-quinoxalinecarbonitrile 1,4-di-N-oxides have been synthesized and tested as antituberculosis agents and interesting results have been obtained from the first screening.

The in vitro activities of cloxyquin (5-chloroquinolin-8-ol) against 9 standard strains and 150 clinical isolates of Mycobacterium tuberculosis were studied. The MICs ranged from 0.062 to 0.25 microg/ml. The MIC(50) and MIC(90) were 0.125 and 0.25 microg/ml, respectively. These indicate that cloxyquin exhibited good antituberculosis activity, even for multidrug-resistant isolates.

New drugs active against drug-resistant tuberculosis are urgently needed to extend the range of TB treatment options to cover drug resistant infections. Quinoxaline derivatives show very interesting biological properties (antibacterial, antiviral, anticancer, antifungal, antihelmintic, insecticidal) and evaluation of their medicinal chemistry is still in progress. In this review we report the p...

Six new antituberculosis compounds in 4 classes are presently in clinical trials. Although these show substantial promise for drug-resistant (DR) tuberculosis, the presently planned studies of these compounds will not inform their optimal use, as each will be tested singly vs placebo with existing drugs, rather than in new regimens. Each successive regulatory approval will increase the size, co...

An n-pentenyl furanosyl-1,2-orthoester can function as a donor or be rearranged leading to an n-pentenyl furanoside acceptor which is glycosylated by its progenitor, regioselectively or doubly, thereby enabling rapid fabrication of a multibranched dodecasaccharide, known to possess a wide variety of biological interactions.

In search of new active molecules, a small focused library 1,2,3-triazoles derived from naphthols were efficiently prepared via the click chemistry approach. The synthesized triazole derivatives evaluated for their antifungal, antioxidant and antitubercular activities. Furthermore, to rationalize observed biological activity data, molecular docking study has also been carried out against site c...

Lack of awareness about isolated tubercular osteomyelitis of the sternum resulted in a delay in diagnosing the condition in an eleven-year-old girl who presented with a gradually increasing swelling over the sternum. Radiological, histological, and microbiological investigations helped diagnose the condition and the child responded well to antitubercular therapy (ATT) and surgical debridement. ...

Although awareness of tuberculosis among captive elephants is increasing, antituberculosis therapy for these animals is not standardized. We describe Mycobacterium tuberculosis transmission between captive elephants based on whole genome analysis and report a successful combination treatment. Infection control protocols and careful monitoring of treatment of captive elephants with tuberculosis ...

A series of heteronemin-related antitubercular scalaranes, both from natural products and from chemical derivatization, were subjected to structure–activity investigations. Based on the activity profile, three main regions; i.e., the substituted groups hovering over C-19/C-18 and furan moiety, the functionalities in the vicinity of C-16 and the right-hand side of ring D, and the substituted gro...

The nontuberculosis mycobacteria are often naturally resistant to the conventional antibiotics and to antituberculosis drugs (1–3). In addition, providing advice for the treatment of nontuberculosis is complicated by the variable and changing designations of these organisms, the heterogeneity of the clinical syndromes and patients, and the relative lack of controlled clinical trials (1,2). This...