Provider: Ingenta Connect Database: Ingenta Connect Content: application/x-research-info-systems TY - ABST AU - Rivers, Emma C. AU - Mancera, Ricardo L. TI - New Anti-Tuberculosis Drugs with Novel Mechanisms of Action JO - Current Medicinal Chemistry PY - 2008-08-01T00:00:00/// VL - 15 IS - 19 SP - 1956 EP - 1967 KW - OPC-67683 KW - Mycobacterium tuberculosis KW - TMC207/R207910 KW - SQ109 KW - PA-824 KW - drug action N2 - It is estimated that a third of the world's population is currently infected with tuberculosis, leading to 1.6 million deaths annually. The current drug regimen is 40 years old and takes 6-9 months to administer. In addition, the emergence of drug resistant strains and HIV co-infection mean that there is an urgent need for new anti-tuberculosis drugs. The twenty-first century has seen a revival in research and development activity in this area, with several new drug candidates entering clinical trials. This review considers new potential firstline anti-tuberculosis drug candidates, in particular those with novel mechanisms of action, as these are most likely to prove effective against resistant strains. A brief overview of current first-line and recent drugs (such as fluoroquinolones, rifampicin and isoniazid analogues) is initially presented. This is followed by a description of structure-activity relationships, in vitro and in vivo activity, pharmacokinetics, mechanism of action, combination regimens and clinical trials of the new drug candidates SQ109, PA-824, OPC-67683, TMC207 and others. UR - https://www.ingentaconnect.com/content/ben/cmc/2008/00000015/00000019/art00008 M3 - doi:10.2174/092986708785132906 UR - https://doi.org/10.2174/092986708785132906 ER -