Tuberculosis drug discovery: challenges and new horizons

GFS Fernandes, AM Thompson… - Journal of Medicinal …, 2022 - ACS Publications
Over the past 2000 years, tuberculosis (TB) has claimed more lives than any other infectious
disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to …

Current scenario of indole derivatives with potential anti-drug-resistant cancer activity

Y Jia, X Wen, Y Gong, X Wang - European Journal of Medicinal Chemistry, 2020 - Elsevier
Cancer chemotherapy is frequently hampered by drug resistance, so the resistance to
anticancer agents represents one of the major obstacles for the effective cancer treatment …

Recent advancements and developments in search of anti-tuberculosis agents: a quinquennial update and future directions

TM Dhameliya, KA Bhakhar, ND Gajjar, KA Patel… - Journal of Molecular …, 2022 - Elsevier
Tuberculosis (TB) has been considered as the highly chronic, contagious and infectious
disorder caused by Mycobacterium tuberculosis (Mtb). Every year more than 10 million …

Synthetic account of indoles in search of potential anti-mycobacterial agents: a review and future insights

KA Bhakhar, DK Sureja, TM Dhameliya - Journal of Molecular Structure, 2022 - Elsevier
Indole, an aza-heterocyclic scaffold, has been found one of the most privileged scaffolds in
heterocyclic chemistry and drug discovery. Efforts have been made to provide the complete …

Recent in vivo advances of spirocyclic scaffolds for drug discovery

VF Batista, DCGA Pinto, AMS Silva - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Spirocyclic scaffolds are an exceptional tool in drug design, allowing fine-tuning
of a molecule's conformational and physicochemical properties. As it expands and …

Ketones and Aldehydes as O-Nucleophiles in Iridium-Catalyzed Intramolecular Asymmetric Allylic Substitution Reaction

Y Wang, WY Zhang, SL You - Journal of the American Chemical …, 2019 - ACS Publications
Ketones and aldehydes are employed as enol O-nucleophiles in an iridium-catalyzed
asymmetric allylic substitution reaction. The reaction proceeds well in the presence of a well …

[HTML][HTML] MmpL3 inhibition: a new approach to treat nontuberculous mycobacterial infections

JP Sethiya, MA Sowards, M Jackson… - International journal of …, 2020 - mdpi.com
Outside of Mycobacterium tuberculosis and Mycobacterium leprae, nontuberculous
mycobacteria (NTM) are environmental mycobacteria (> 190 species) and are classified as …

Rhodium-catalyzed diastereoselective synthesis of highly substituted morpholines from nitrogen-tethered allenols

AZ Halimehjani, B Breit - Chemical Communications, 2023 - pubs.rsc.org
Rhodium-catalyzed intramolecular cyclization of nitrogen-tethered allenols was investigated
for the synthesis of functionalized morpholines. By using this strategy, various N-protected 2 …

Functionalized Dioxonaphthoimidazoliums: A Redox Cycling Chemotype with Potent Bactericidal Activities against Mycobacterium tuberculosis

KT Fridianto, M Li, K Hards, DA Negatu… - Journal of medicinal …, 2021 - ACS Publications
Disruption of redox homeostasis in mycobacteria causes irreversible stress induction and
cell death. Here, we report the dioxonaphthoimidazolium scaffold as a novel redox cycling …

Discovery of 1, 2, 3-triazole incorporated indole-piperazines as potent antitubercular agents: Design, synthesis, in vitro biological evaluation, molecular docking and …

R Reddyrajula, U Etikyala, V Manga… - Bioorganic & Medicinal …, 2024 - Elsevier
In this report, a library consisting of three sets of indole-piperazine derivatives was designed
through the molecular hybridization approach. In total, fifty new hybrid compounds (T1-T50) …