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 …
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
Chemistry campaigns identified amphiphilic indolyl Mannich bases as novel membrane-
permeabilizing antimycobacterials. Spiroketal analogs of this series showed increased …
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 …
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 …
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
Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here we found
that modifying the incipient scaffold by amide–amine substitution and replacing the indole …
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 …
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 …
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 …
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 …
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 …
drug-resistant (DR) forms pose this disease as a growing public health menace. Therefore, it …