Current Pharmaceutical Design - Volume 20, Issue 27, 2014

Tuberculosis (TB) remains to be a global major public-health threat, causing millions of deaths each year. A major difficulty in dealing with TB is that the causative bacterium, Mycobacterium tuberculosis, can persist in host tissue for a long period of time even after treatment. Mycobacterial persistence has become a central research focus for developing next-generation TB drugs. Latest genomic technology has enabled a hi Read More

The rise of multi-drug resistant and extensively drug resistant M. tuberculosis around the world poses a great threat to human health, and necessitates development of new, effective and inexpensive anti-tubercular agents. The availability of knowledge on molecular biology of M. tuberculosis infection coupled with whole genome sequences, transcriptomic, proteomic and metabolomic data sets have provided insig Read More

The emergence of multi- and extensively-drug resistant strains of Mycobacterium tuberculosis makes the development of novel anti-tubercular compounds and the identification of alternative mycobacterial drugable targets urgent priorities. Recently, type VII secretion systems (T7SS) have been discovered in mycobacteria. The genome of M. tuberculosis encodes 5 of such systems (ESX-1 to - 5), three of which have been ch Read More

Mycolic acids are the major lipid components of the unique mycobacterial cell wall responsible for the protection of the tuberculosis bacilli from many outside threats. Mycolic acids are synthesized in the cytoplasm and transported to the outer membrane as trehalose- containing glycolipids before being esterified to the arabinogalactan portion of the cell wall and outer membrane glycolipids. The large size of these unique fat Read More

Several groups working in the field of the development of new antituberculosis drugs have recently reported active compounds targeting mycobacterial enzyme DprE1. Along with its counterpart, DprE2, it catalyses a unique epimerization reaction resulting in the synthesis of decaprenylphosphoryl arabinose, the single donor of arabinosyl residues for the build-up of arabinans, fundamental components of the Read More

Tuberculosis (TB) is one of the most important health concerns in the world, causing serious levels of morbidity and mortality, particularly in many developing countries. Unfortunately, the development of new anti-TB drugs with superior chemotherapeutic and prophylactic activity has been very slow. Thus, it is urgently necessary to develop novel kinds of antituberculosis drugs that exert their anti-Mycobacterium tuberculosis (MT Read More

Increasing worldwide incidence and the advent of multi drug resistant and extensively drug resistant tuberculosis raise the need of new drugs for the treatment of tuberculosis soon. To meet the required pace QSAR-based rational approaches may prove fruitful as they render rapid and cost-efficient design and optimization of new drug candidates. This review presents a comprehensive overview of QSAR studies reported for Read More

Tuberculosis (TB) is the second cause of death from a single infectious agent, the M. tuberculosis bacillus. Nearly two billion people are infected and about 8.7 million new cases and 1.4 million deaths were reported by the World Health Organization (WHO) in 2013. Despite the availability of effective treatment, the alarming emergence of multidrug resistant (MDR) strains (with 310.000 estimated cases in 2011 among notified Read More

Tuberculosis caused by Mycobacterium tuberculosis is an infectious bacterial disease which is a leading cause of mortality affecting more than 9 million people worldwide. The current standard regimens that are available for the treatment of TB are severely hampered due to the occurrence of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of Mycobacterium tuberculosis. In the past few years, a Read More

Worldwide, tuberculosis (TB) is the leading cause of death among curable infectious diseases. The emergence of multidrug resistant (MDR) and extensively drug resistant (XDR) TB is a growing global health concern and there is an urgent need for new anti-TB drugs. Enzymes involved in DNA and ATP biosynthesis are potential targets for tuberculostatic drug design, since these enzymes are essential for Mycobacterium tuberc Read More