Chemical classes presenting novel antituberculosis agents currently in different phases of drug development: A 2010–2020 review

KT Angula, LJ Legoabe, RM Beteck - Pharmaceuticals, 2021 - mdpi.com
Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), is a curable airborne
disease currently treated using a drug regimen consisting of four drugs. Global TB control …

Synthetic molecules as DprE1 inhibitors: A patent review

M Imran, A AS, HK Thabet, Abida… - Expert Opinion on …, 2021 - Taylor & Francis
Introduction In recent years, the advent of multidrug-resistant tuberculosis (MDR-TB), the
extensively-resistant TB (XDR-TB), and the total drug-resistant-TB (TDR-TB) have led the …

Development of macozinone for TB treatment: an update

V Makarov, K Mikušová - Applied Sciences, 2020 - mdpi.com
Macozinone, a piperazine-benzothiazinone PBTZ169, is currently undergoing Phase 1/2
clinical studies for the treatment of tuberculosis (TB). In this review we summarize the key …

[HTML][HTML] Quinolone analogues of benzothiazinone: synthesis, antitubercular structure-activity relationship and ADME profiling

PS Dube, LJ Legoabe, A Jordaan, L Sigauke… - European Journal of …, 2023 - Elsevier
Mycobacterium tuberculosis (Mtb) has an impermeable cell wall which gives it an inherent
ability to resist many antibiotics. DprE1, an essential enzyme in Mtb cell wall synthesis, has …

Recent progress in the development of novel mycobacterium cell wall inhibitor to combat drug-resistant tuberculosis

TM Belete - Microbiology Insights, 2022 - journals.sagepub.com
Despite decades of research in drug development against TB, it is still the leading cause of
death due to infectious diseases. The long treatment duration, patient noncompliance …

[HTML][HTML] Optimized LC-MS/MS quantification of tuberculosis drug candidate macozinone (PBTZ169), its dearomatized Meisenheimer Complex and other metabolites …

V Desfontaine, S Guinchard, S Marques, A Vocat… - … of Chromatography B, 2023 - Elsevier
Tuberculosis, and especially multidrug-resistant tuberculosis (MDR-TB), is a major global
health threat which emphasizes the need to develop new agents to improve and shorten …

DprE1 and Ddn as promising therapeutic targets in the development of novel anti-tuberculosis nitroaromatic drugs

R Paoli-Lombardo, N Primas, P Vanelle - European Journal of Medicinal …, 2024 - Elsevier
Tuberculosis remains the second deadliest infectious disease in humans and a public
health threat due to the emergence of multidrug-resistant (MDR-TB) and extensively drug …

Advances in spray drying technology for anti-tubercular formulation development: A comprehensive review

E Kole, K Jadhav, Y Sonar, M Kapse, SA Patil… - Drying …, 2024 - Taylor & Francis
Global health is still seriously threatened by tuberculosis (TB), especially considering the
increasing incidence of strains of the disease that are extensively drug-resistant (XDR) and …

Identifying Novel Therapeutics for the Resistant Mutant “F533L” in PBP3 of Pseudomonas aeruginosa Using ML Techniques

T Joshi, S Vijayakumar, S Ghosh, S Mathpal… - ACS …, 2024 - ACS Publications
Pseudomonas aeruginosa (P. aeruginosa) is a highly infectious and antibiotic-resistant
bacterium, which causes acute and chronic nosocomial infections. P. aeruginosa exhibits …

Synthesis, structures, reactivity and medicinal chemistry of antitubercular benzothiazinones

RW Seidel, A Richter, R Goddard… - Chemical …, 2023 - pubs.rsc.org
Tuberculosis is the leading bacterial killer worldwide. 8-Nitro-4H-benzo [e][1, 3] thiazin-4-
ones are a potent class of antitubercular agents with a new mechanism of action. BTZ043 …