Antituberculosis Drug Research: A Critical Overview

Abstract

The increasing drug resistance of Mycobacterium tuberculosis to the currently used drugs and HIV coinfection has caused alarm in the international scientific community. Subsequently, there is an urgent need for the development of new drug molecules with newer targets and with an alternative mechanism of action. Since the last 50 years, the same long-duration, multidrug treatment plan is being followed for the treatment of tuberculosis. The objective of this review article is to critically analyze the antitubercular potential of various classes of compounds (quinoline, diamine, quinolone, fluoroquinolone, quinone, nitroimidazole, terpenoid, isonicotinyl, oxazolidinone, pyrimidine, and purine), their possibility to be a future drug candidate, and latest information on the clinical status of some novel antitubercular compounds. Compounds such as moxifloxacin, PA824, and TMC207 are well tolerated and there is no adverse effect shown by them. Moxifloxacin and gatifloxacin shows cross-resistance to the currently used drugs while no cross-resistance observed in case of TMC207 and PA824. Some compounds like OPC67683 and PA824 are bactericidal in nature.

Computational and Experimental Study on Molecular Structure of Benzo[g]pyrimido[4,5-b]quinoline Derivatives: Preference of Linear over the Angular Isomer

“…Quinoline derivatives are synthetic targets because they exhibit a wide range of biological and pharmacological activities [18][19][20][21][22][23]. Compared with other derivatives that exhibit high fluorescence, quinolone derivatives are among the best candidates in the design of electroluminescent materials [24,25].…”

Isoniazid@Fe2O3‐Nanocontainer mit antibakterieller Wirkung auf Tuberkulose‐Mykobakterien

“…[1,3] Grundsätzlich stehen sehr wirksame Antibiotika wie Isoniazid (Isonikotinylhydrazin, INH), Rifampicin (RIF), Pyrazinamid (PYZ) oder Ethambutol (ETB) für die TBTherapie zur Verfügung. [2,4] Allerdings müssen diese antimykobakteriellen Wirkstoffe nicht nur Granulom-Einkapselung und die Membran der Wirtsmakrophage,s ondern auch die lipidreiche Zellwand der mykobakteriellen Zellen durchdringen. Weitere Einschränkungen betreffen die geringe Permeabilität in Biofilmen sowie den schnellen Abbau unter physiologischen Bedingungen bei geringer Dosis,a ber schweren Nebenwirkungen bei hçherer Dosis.…”

“…Weitere Einschränkungen betreffen die geringe Permeabilität in Biofilmen sowie den schnellen Abbau unter physiologischen Bedingungen bei geringer Dosis,a ber schweren Nebenwirkungen bei hçherer Dosis. [2,4] Die TBTherapie erfordert eine tägliche Dosis von bis zu 5mgkg…”

Design, synthesis of benzocoumarin-pyrimidine hybrids as novel class of antitubercular agents, their DNA cleavage and X-ray studies

“…It is known that most of the currently existing anti-tubercular drugs constitute by the group of nitrogen heterocyclic compounds such as isoniazid, clofazimine and pyrazinamide which are derived from pyridine and pyrazines [36]. Hence in search of new heterocyclic compounds containing nitrogen hetero atom, our attention curved in the direction of pyrimidine ring (N-containing heterocyclic compound) in anticipation that it may lead to more potent anti-TB agents.…”