Tuberculosis remains a growing threat of infectious diseases of twenty-first century. An attempt to find new antituberculosis agents was made especially to treat multidrug-resistant and extensively drug-resistant tuberculosis. One of the most promising drugs is bedaquiline - a new drug approved by Food and Drug Administration (FDA) and by the European Union countries. This compound is intended to treat multidrug-resistant pulmonary tuberculosis in adult patients in combination regimens in case of impossibility of using other drugs. This paper is also focused on some interesting molecules in treating multidrug-resistant tuberculosis which are currently tested in clinical studies: delamanid (dihydro-nitroimidazooxazole derivative, phase III), AZD5847 (oxazolidinone derivative, phase II), pretomanid (nitroimidazole derivative, phase III), sutezolid (oxazolidinone derivative, phase II) and SQ109 (ethambutol analogue, phase II) and some prospective molecules at the level of preclinical studies e.g., CPZEN-45, SQ609 and SQ641.

2015-10-01·Future Medicinal Chemistry4区 · 医学

The Anti-Tuberculosis Agents Under Development and the Challenges Ahead

4区 · 医学

Review

作者: Negi, Beena ; Rawat, Diwan S ; Kumar, Deepak

Tuberculosis (TB) is a serious health problem causing 1.5 million deaths worldwide. After the discovery of first-line anti-TB drugs, the mortality rate declined sharply, however, the emergence of drug-resistant strains and HIV co-infection have led to increased incidence of this disease. A number of new potential antitubercular drug candidates with novel modes of action have entered clinical trials in recent years. Compounds such as gatifloxacin, moxifloxacin and linezolid, the already known antibiotics are currently being evaluated for their anti-TB activity. OPC-67683 and TMC207 have been approved for the treatment of MDR-TB patients recently, while PA-824, SQ109, PNU-100480, AZD5847, LL3858, SQ609, SQ641, BTZ043, DC-159a, CPZEN-45, Q-203, DNB1, TBA-354 are in various phases of clinical and preclinical developments. This review evaluates the current status of TB drug development and future aspects.

2012-05-01·European Journal of Medicinal Chemistry1区 · 医学

Tuberculosis: The drug development pipeline at a glance

1区 · 医学

Review

作者: Marion Flipo ; Nicolas Willand ; Baptiste Villemagne ; Alain R. Baulard ; Benoit Déprez ; Céline Crauste

Tuberculosis is a major disease causing every year 1.8 million deaths worldwide and represents the leading cause of mortality resulting from a bacterial infection. Introduction in the 60's of first-line drug regimen resulted in the control of the disease and TB was perceived as defeating. However, since the progression of HIV leading to co-infection with AIDS and the emergence of drug resistant strains, the need of new anti-tuberculosis drugs was not overstated. However in the past 40 years any new molecule did succeed in reaching the market. Today, the pipeline of potential new treatments has been fulfilled with several compounds in clinical trials or preclinical development with promising activities against sensitive and resistant Mycobacterium tuberculosis strains. Compounds as gatifloxacin, moxifloxacin, metronidazole or linezolid already used against other bacterial infections are currently evaluated in clinical phases 2 or 3 for treating tuberculosis. In addition, analogues of known TB drugs (PA-824, OPC-67683, PNU-100480, AZD5847, SQ609, SQ109, DC-159a) and new chemical entities (TMC207, BTZ043, DNB1, BDM31343) are under development. In this review, we report the chemical synthesis, mode of action when known, in vitro and in vivo activities and clinical data of all current small molecules targeting tuberculosis.

100 项与 SQ-609 相关的药物交易

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