Published: 2016-02-17

Current directions in searching for tuberculostatic substances

Department of Organic Chemistry, Poznan University of Medical Sciences, Poland
Department of Organic Chemistry, Poznan University of Medical Sciences, Poland
tuberculosis tuberculostatic agents clinical trials

Abstract

Yearly, 8 milion people advance to active tuberculosis (TB) and nearly 2 milion victims die of their infection. Long drug regimen is blamed for the emergence of drug resistant TB. Moreover, 20% of TB isolates are already resistant to the first line antituberculosis drugs. This situation has required to develop new, more active anti-TB substances. Several novel drug candidates from different groups of chemical compounds undergo clinical trials. Others, also promising agents, have been obtained recently. They are the basis for further modifications heading for improvement of their physicochemical, biological and toxicological parameters.

Downloads

Download data is not yet available.

References

  1. Protopopova M, Bogatcheva E, Nikonenko B, Hundert S, Einck L, Nacy CA. In search of new cures for tuberculosis. Med Chem. 2007;3:301–16.
  2. Laughon BE. New tuberculosis drugs in development. Curr Topics Med Chem. 2007;7(5):463–73.
  3. Showalter HDH, Denny WA. A roadmap for drug discovery and its translation to small molecule agents in clinical development for tuberculosis treatment. Tuberculosis. 2008;88(Suppl. 1):3–17.
  4. Żwawiak J, Zaprutko L. Pochodne imidazolu jako leki przeciwgruźlicze. Farm Współcz. 2012;5(4):192–9.
  5. Andries K, Verhasselt P, Guillemont J, Gohlmann HW, Neefs JM, Winkler H, et al. A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science. 2005;307:223–7.
  6. Matteelli A, Carvalho AC, Dooley KE, Kritski A. TMC207: the first compound of a new class of potent anti-tuberculosis drugs. Future Microbiol. 2010;5(6):849–58.
  7. De Souza MVN, Pais KC, Kaiser CR, Peralta MA, Ferreira ML, Lourenco MCS. Synthesis and in vitro antitubercular activity of a series of quinoline derivatives. Bioorg Med Chem. 2009;17:1474–80.
  8. Bogatcheva E, Hanrahan C, Nikonenko B, Samala R, Chen P, Gearhart J, et al. Identification of new diamine scaffolds with activity against Mycobacterium tuberculosis. J Med Chem. 2006;49(11):3045–8.
  9. Chen P, Gearhart J, Protopopova M, Einck L, Nacy CA. Synergic interaction of SQ109, a new ethylene diamine, with front-line antitubercular drugs in vitro. J Antimicrob Chemother. 2006;58:332–7.
  10. Nikonenko BV, Protopopova M, Samala R, Einck L, Nacy CA. Drug Therapy of Experimental Tuberculosis (TB): Improved Outcome by Combining SQ109, a New Diamine Antibiotic, with Existing TB Drugs. Antimicrob Agents Chemother. 2007;51(4):1563–5.
  11. SQ-109. Tuberculosis. 2008;88(2):159–61.
  12. Makobongo MO, Einck L, Peek RM, Merrel DS. In Vitro Characterization of the Anti-Bacterial Activity of SQ 109 Against Helicobacter Pylori. PLoS One. 2013;8(7): e68917.
  13. Jones PB, Parrish NM, Houston TA, Stapon A, Bansal NP, Dick JD, et al. A new class of anti-tuberculosis agents. J Med Chem. 2000;43:3304–14.
  14. Parrish NM, Houston TA, Jones PB, Townsend C, Dick JD. In Vitro Activity of a Novel Antimycobacterial Compound, N-Octanesulfonylacetamide, and Its Effects on Lipid and Mycolic Acid Synthesis. Antimicrob Agents Chemother. 2001;45:1143–50.
  15. Shinabarger D. Mechanism of action of the oxazolidinone antibacterial agents. Exp Opin Invest Drugs. 1999;8(8): 1195–202.
  16. Alffenaar JWC, van der Laan T, Simons S, van der Werf TS, van de Kasteele PJ, de Neeling H, et al. Susceptibility of Clinical Mycobacterium tuberculosis Isolates to a Potentially Less Toxic Derivate of Linezolid, PNU-100480. Antimicrob Agents Chemother. 2011;55(3):1287–9.
  17. Schlunzen F, Pyetan E, Fucini P, Yonath A, Harms JM. Inhibition of peptide bond formation by pleuromutilins: the structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin. Mol Microbiol. 2004;54:1287–94.
  18. Hu Y, Coates AR, Mitchison DA. Sterilizing activities of fluoroquinolones against rifampin-tolerant populations of Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2003;47:653–7.
  19. Nuermberger E, Tyagi S, Tasneen R, Williams KN. Almeida D, Rosenthal I, Grosset JH. Powerful Bactericidal and Sterilizing Activity of a Regimen Containing PA-824, Moxifloxacin, and Pyrazinamide in a Murine Model of Tuberculosis. Antimicrob Agents Chemother. 2008; 52(4):1522–4.
  20. Paramasivan CN, Sulochana S, Kubendiran G, Venkatesan P, Mitchison DA. Bactericidal Action of Gatifloxacin, Rifampin, and Isoniazid on Logarithmic- and Stationary-Phase Cultures of Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2005;49:627–31.
  21. Sriram D, Yogeeswari P, Dhakla P, Senthilkumar P, Banerjee D, Manjashetty TH. 5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species. Bioorg Med Chem Lett. 2009;19:1152–4.
  22. Onayole OK, Pieroni M, Tipparaju SK, Lun S, Stec J, Chen G, et al. Preliminary Structure – Activity Relationships and Biological Evaluation of Novel Antitubercular Indolecarboxamide Derivatives Against Drug – Susceptible and Drug – Resistant Mycobacterium tuberculosis Strains. J Med Chem. 2013;56:4093–103.
  23. Moraski GC, Markley LD, Cramer J, Hipskind PA, Boshoff H, Bailey MA, et al. Advancement of Imidazo[1,2-a]pyridines with Improved Pharmacokinetics and nM Activity vs. Mycobacterium tuberculosis. ACS Med Chem Lett. 2013;4:675–9.
  24. Yokokawa F, Wang G, Chan WL, Ang SH, Wong J, Ma I, et al. Discovery of Tetrahydropyrazolopyrimidine Carboxamide Derivatives As Potent and Orally Active Antitubercular Agents. ACS Med Chem Lett. 2013;4(5):451–5.
  25. McCulloch MWB, Haltli B, Marchbank DH, Kerr RG. Evaluation of Pseudopteroxazole and Pseudopterosin Derivatives against Mycobacterium tuberculosis and Other Pathogens. Mar Drugs. 2012;10(8):1711–28.
  26. Liu B, Liu K, Lu Y, Zhang D, Yang T, Li X, et al. Systematic Evaluation of Structure – Activity Relationships of the Riminophenazine Class and Discovery of a C2 Pyridylamino Series for the Treatment of Multidrug – Resistant Tuberculosis. Molecules. 2012;17:4545–59.
  27. WHO Report 2011. Global Tuberculosis Control. World Health Organization. ISBN 978 92 4 1564 38 0.
  28. Yew WW. Managment of Multidrug-Resistant Tuberculosis and Extensively Drug-Resistant Tuberculosis: Current Status and Future Prospects. Kekkaku. 2011;86(1):9–16.

How to Cite

1.
Żwawiak J, Zaprutko L. Current directions in searching for tuberculostatic substances. JMS [Internet]. 2016Feb.17 [cited 2020Aug.10];83(2):138-44. Available from: https://jms.ump.edu.pl/index.php/JMS/article/view/58