Indolyl azaspiroketal Mannich bases are potent antimycobacterial agents with selective membrane permeabilizing effects and in vivo activity

SA Nyantakyi, M Li, P Gopal… - Journal of medicinal …, 2018 - ACS Publications
The inclusion of an azaspiroketal Mannich base in the membrane targeting antitubercular 6-
methoxy-1-n-octyl-1 H-indole scaffold resulted in analogs with improved selectivity and …

Potency increase of spiroketal analogs of membrane inserting indolyl mannich base antimycobacterials is due to acquisition of MmpL3 inhibition

M Li, ZY Phua, Y Xi, Z Xu, SA Nyantakyi… - ACS infectious …, 2020 - ACS Publications
Chemistry campaigns identified amphiphilic indolyl Mannich bases as novel membrane-
permeabilizing antimycobacterials. Spiroketal analogs of this series showed increased …

Amphiphilic indole derivatives as antimycobacterial agents: structure–activity relationships and membrane targeting properties

T Yang, W Moreira, SA Nyantakyi, H Chen… - Journal of medicinal …, 2017 - ACS Publications
Antibacterials that disrupt cell membrane function have the potential to eradicate “persister”
organisms and delay the emergence of resistance. Here we report the antimycobacterial …

2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis

M Naik, S Ghorpade, LK Jena, G Gorai… - ACS Medicinal …, 2014 - ACS Publications
A cellular activity-based screen on Mycobacterium tuberculosis (Mtb) H37Rv using a
focused library from the AstraZeneca corporate collection led to the identification of 2 …

Amide–amine replacement in indole-2-carboxamides yields potent mycobactericidal agents with improved water solubility

YJ Tan, M Li, GA Gunawan, SA Nyantakyi… - ACS Medicinal …, 2020 - ACS Publications
Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here we found
that modifying the incipient scaffold by amide–amine substitution and replacing the indole …

Design, synthesis and biological evaluation of alkynyl-containing maleimide derivatives for the treatment of drug-resistant tuberculosis

P Li, B Wang, X Chen, Z Lin, G Li, Y Lu, H Huang - Bioorganic Chemistry, 2023 - Elsevier
A series of alkynyl-containing maleimides with potent anti-tuberculosis (TB) activity was
developed through a rigid group substitution strategy based on our previous study …

Synthesis of Bisindole Alkaloids and Their Mode of Action against Methicillin-Resistant Staphylococcus Aureus

ET Adeniyi, M Kruppa, S De Benedetti… - ACS Infectious …, 2024 - ACS Publications
About 100,000 deaths are attributed annually to infections with methicillin-resistant
Staphylococcus aureus (MRSA) despite concerted efforts toward vaccine development and …

Identification of Novel Chemical Scaffolds that Inhibit the Growth of Mycobacterium tuberculosis in Macrophages

S Ahmed, A Manning, L Flint, D Awasthi… - Frontiers in …, 2022 - frontiersin.org
Mycobacterium tuberculosis is an important global pathogen for which new drugs are
urgently required. The ability of the organism to survive and multiply within macrophages …

Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines

CRM Asquith, N Fleck, CD Torrice, DJ Crona… - Bioorganic & medicinal …, 2019 - Elsevier
We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel
inhibitors of Mycobacterium tuberculosis (Mtb). The focused 4-anilinoquinoline/quinazoline …

Design, synthesis and antimycobacterial evaluation of novel adamantane and adamantanol analogues effective against drug-resistant tuberculosis

SSR Alsayed, S Lun, A Payne, WR Bishai… - Bioorganic …, 2021 - Elsevier
The treacherous nature of tuberculosis (TB) combined with the ubiquitous presence of the
drug-resistant (DR) forms pose this disease as a growing public health menace. Therefore, it …