Synthesis, Characterization, and Biological Evaluation of New Derivatives Targeting MbtI as Antitubercular Agents [PDF]
Pharmaceuticals, 2021 Tuberculosis (TB) causes millions of deaths every year, ranking as one of the most dangerous infectious diseases worldwide. Because several pathogenic strains of Mycobacterium tuberculosis (Mtb) have developed resistance against most of the established ...
Matteo Mori +8 more
doaj +3 more sources
Exploration of Piperidinols as Potential Antitubercular Agents [PDF]
Molecules, 2014 Novel drugs to treat tuberculosis are required and the identification of potential targets is important. Piperidinols have been identified as potential antimycobacterial agents (MIC < 5 μg/mL), which also inhibit mycobacterial arylamine N ...
Areej Abuhammad +6 more
doaj +8 more sources
Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents. [PDF]
ACS Med Chem Lett, 2022 The 6-trifluoro substituted 8-nitrobenzothiazinones (BTZs) represent a novel type of antitubercular agents, and their high antimycobacterial activity is related to the inhibition of decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1), an enzyme essential ...
Shi R +9 more
europepmc +2 more sources
Exploration of 4-aminopyrrolo[2,3-d]pyrimidine as antitubercular agents. [PDF]
Mol Divers, 2023 Tuberculosis (TB) is one of the leading causes of death worldwide. Developing new anti-TB compounds using cost-effective processes is critical to reduce TB incidence and accomplish the End TB Strategy milestone.
Jesumoroti OJ +4 more
europepmc +2 more sources
New Quinoline-Urea-Benzothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling. [PDF]
Pharmaceuticals (Basel), 2022 A series of 25 new benzothiazole–urea–quinoline hybrid compounds were synthesized successfully via a three-step synthetic sequence involving an amidation coupling reaction as a critical step.
Moodley R +9 more
europepmc +2 more sources
Identification of 2-(N-aryl-1,2,3-triazol-4-yl) quinoline derivatives as antitubercular agents endowed with InhA inhibitory activity. [PDF]
Front ChemThe spread of drug-resistant tuberculosis strains has become a significant economic burden globally. To tackle this challenge, there is a need to develop new drugs that target specific mycobacterial enzymes.
Sabt A +12 more
europepmc +2 more sources
Comparison of the Efficacy of Two Novel Antitubercular Agents in Free and Liposome-Encapsulated Formulations. [PDF]
Int J Mol Sci, 2021 Tuberculosis is one of the top ten causes of death worldwide, and due to the appearance of drug-resistant strains, the development of new antituberculotic agents is a pressing challenge.
Kósa N +7 more
europepmc +2 more sources
Structure-Activity Relationships of Pyrazolo[1,5-<i>a</i>]pyrimidin-7(4<i>H</i>)-ones as Antitubercular Agents. [PDF]
ACS Infect Dis, 2021 Pyrazolo[1,5-a]pyrimidin-7(4H)-one was identified through high-throughput whole-cell screening as a potential antituberculosis lead. The core of this scaffold has been identified several times previously and has been associated with various modes of ...
Oh S +14 more
europepmc +2 more sources
Novel Pyrimidines as Antitubercular Agents. [PDF]
Antimicrob Agents Chemother, 2018 ABSTRACT Mycobacterium tuberculosis infection is responsible for a global pandemic. New drugs are needed that do not show cross-resistance with the existing front-line therapeutics. A triazine antitubercular hit led to the design of a related pyrimidine family.
Inoyama D +13 more
europepmc +4 more sources
New Application of 1,2,4-Triazole Derivatives as Antitubercular Agents. Structure, In Vitro Screening and Docking Studies. [PDF]
Molecules, 2020 A series of 1,2,4-triazole derivatives were synthesized and assigned as potential anti-tuberculosis substances. The molecular and crystal structures for the model compounds C1, C12, and C13 were determined using X-ray analysis.
Karczmarzyk Z +6 more
europepmc +2 more sources