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Phenotypic screens for bactericidal compounds against drug-resistant tuberculosis are beginning to yield novel inhibitors. However, reliable target identification remains challenging. Here, we show that tetrahydropyrazo[1,5-a]pyrimidine-3-carboxamide (THPP) selectively pulls down EchA6 in a stereospecific manner, instead of the previously assigned target(More)
Tuberculosis (TB) is one of the world's oldest and deadliest diseases, killing a person every 20 s. InhA, the enoyl-ACP reductase from Mycobacterium tuberculosis, is the target of the frontline antitubercular drug isoniazid (INH). Compounds that directly target InhA and do not require activation by mycobacterial catalase peroxidase KatG are promising(More)
Mycobacterial enoyl acyl carrier protein reductase (InhA) is a clinically validated target for the treatment of tuberculosis infections, a disease that still causes the death of at least a million people annually. A known class of potent, direct, and competitive InhA inhibitors based on a tetracyclic thiadiazole structure has been shown to have in vivo(More)
Despite being one of the first antitubercular agents identified, isoniazid (INH) is still the most prescribed drug for prophylaxis and tuberculosis (TB) treatment and, together with rifampicin, the pillars of current chemotherapy. A high percentage of isoniazid resistance is linked to mutations in the pro-drug activating enzyme KatG, so the discovery of(More)
Glycosyl halides are a very valuable and versatile group of synthetic intermediates widely used in carbohydrate chemistry for the ready functionalization at the anomeric carbon. Thus, glycosyl halides can be easily converted into O-glycosides, C-glycosides, or glycals via the generation of intermediate anomeric carbocations, radicals, or cabanions. Because(More)
Tetrahydropyran derivative 1 was discovered in a high-throughput screening campaign to find new inhibitors of mycobacterial InhA. Following initial in-vitro profiling, a structure-activity relationship study was initiated and a focused library of analogs was synthesized and evaluated. This yielded compound 42 with improved antimycobacterial activity and low(More)
The increasing prevalence of multidrug-resistant strains of Mycobacterium tuberculosis is the main contributing factor in unfavorable outcomes in the treatment of tuberculosis. Studies suggest that direct inhibitors of InhA, an enoyl-ACP-reductase, might yield promising clinical candidates that can be developed into new antitubercular drugs. In this review,(More)
In the Neural Networks approach by Radial Basis Function-RBF, the property of interpolation between faces, their variation, and the diversity of faces helps to minimize the output error. However, the training set size has to be optimized because the time to train an Artificial Neural Network-ANN, is correlated with the number of samples in that training(More)
Different from traditional methods which use two-dimensional images and gray levels to recognize human faces, this article shows a known shape extraction methodology applied to the extraction of 3D human faces conjugated with a conventional and non conventional algorithms for face verification. The SORFACE project involves two main knowledge areas, 3D shape(More)
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