Strategies to combat multi-drug resistance in tuberculosis

V Singh, K Chibale - Accounts of chemical research, 2021 - ACS Publications
Conspectus “Drug resistance is an unavoidable consequence of the use of drugs; however,
the emergence of multi-drug resistance can be managed by accurate diagnosis and tailor …

Bioactivities and structure–activity relationships of fusidic acid derivatives: a review

J Long, W Ji, D Zhang, Y Zhu, Y Bi - Frontiers in Pharmacology, 2021 - frontiersin.org
Fusidic acid (FA) is a natural tetracyclic triterpene isolated from fungi, which is clinically used
for systemic and local staphylococcal infections, including methicillin-resistant …

Semisynthetic antimycobacterial C-3 silicate and C-3/C-21 ester derivatives of fusidic acid: pharmacological evaluation and stability studies in liver microsomes, rat …

M Njoroge, G Kaur, M Espinoza-Moraga… - ACS Infectious …, 2019 - ACS Publications
Fusidic acid (FA), a natural product fusidane triterpene-based antibiotic with unique
structural features, is active in vitro against Mycobacterium tuberculosis, the causative agent …

Old fusidane-type antibiotics for new challenges: Chemistry and biology

T Chuan, W Ke, X Zhang, LI Gang… - Chinese Journal of …, 2022 - Elsevier
The spread of antibiotic-resistant bacteria and exhausted drug leads render some infections
untreatable now and in the future. To deal with these “new challenges”, scientists tend to re …

Novel antimycobacterial C-21 amide derivatives of the antibiotic fusidic acid: synthesis, pharmacological evaluation and rationalization of media-dependent activity …

GA Dziwornu, S Kamunya, T Ntsabo, K Chibale - MedChemComm, 2019 - pubs.rsc.org
Fusidic acid is a natural product antibiotic used clinically, primarily against staphylococcal
infections. It has also exhibited antimycobacterial activity against Mycobacterium species …

High rates of treatment success in pulmonary multidrug-resistant tuberculosis by individually tailored treatment regimens

ID Olaru, C Lange, A Indra, L Meidlinger… - Annals of the …, 2016 - atsjournals.org
Rationale: We evaluated whether treatment outcomes for patients with multidrug-resistant
and extensively drug-resistant tuberculosis can be substantially improved when sufficient …

Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre

V Singh, D Mambwe, CM Korkor… - ACS Medicinal Chemistry …, 2022 - ACS Publications
As the so-called “next frontier” in global economic terms, Africa's disease burden continues
to choke and cripple economic growth across the continent. The highest burden is …

Pharmacokinetics and organ distribution of C-3 alkyl esters as potential antimycobacterial prodrugs of fusidic acid

N Strydom, G Kaur, GA Dziwornu, J Okombo… - ACS infectious …, 2020 - ACS Publications
Fusidic acid (FA) has previously been shown to be rapidly metabolized in rodents to its C-3
epimer, which has significantly lower antimycobacterial activity relative to FA. This was in …

Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity

K Singh, G Kaur, PS Shanika, GA Dziwornu… - Bioorganic & Medicinal …, 2020 - Elsevier
Fusidic acid (FA) is a potent congener of the fusidane triterpenoid class of antibiotics.
Structure-activity relationship (SAR) studies suggest the chemical structure of FA is optimal …

Unlocking translational machinery for antitubercular drug development

N Kumar, MA Wani, CI Raje, P Garg - Trends in Biochemical Sciences, 2024 - cell.com
Targeting translational factor proteins (TFPs) presents significant promise for the
development of innovative antitubercular drugs. Previous insights from antibiotic binding …