[HTML][HTML] Development of phenothiazine hybrids with potential medicinal interest: A review

MC Posso, FC Domingues, S Ferreira, S Silvestre - Molecules, 2022 - mdpi.com
The molecular hybridization approach has been used to develop compounds with improved
efficacy by combining two or more pharmacophores of bioactive scaffolds. In this context …

Efflux pumps in Mycobacterium tuberculosis and their inhibition to tackle antimicrobial resistance

M Laws, P **, KM Rahman - Trends in microbiology, 2022 - cell.com
Tuberculosis (TB), an infectious disease caused by the bacterium Mycobacterium
tuberculosis, was the leading cause of mortality worldwide in 2019 due to a single infectious …

Verapamil targets membrane energetics in Mycobacterium tuberculosis

C Chen, S Gardete, RS Jansen, A Shetty… - Antimicrobial agents …, 2018 - journals.asm.org
Mycobacterium tuberculosis kills more people than any other bacterial pathogen and is
becoming increasingly untreatable due to the emergence of resistance. Verapamil, an FDA …

Interplay between Mutations and Efflux in Drug Resistant Clinical Isolates of Mycobacterium tuberculosis

D Machado, TS Coelho, J Perdigão, C Pereira… - Frontiers in …, 2017 - frontiersin.org
Numerous studies show efflux as a universal bacterial mechanism contributing to antibiotic
resistance and also that the activity of the antibiotics subject to efflux can be enhanced by …

Diversity and evolution of drug resistance mechanisms in Mycobacterium tuberculosis

M Al-Saeedi, S Al-Hajoj - Infection and drug resistance, 2017 - Taylor & Francis
Despite the efficacy of antibiotics to protect humankind against many deadly pathogens,
such as Mycobacterium tuberculosis, nothing can prevent the emergence of drug-resistant …

Multimetallic Microparticles Increase the Potency of Rifampicin against Intracellular Mycobacterium tuberculosis

T Ellis, M Chiappi, A Garcia-Trenco, M Al-Ejji… - ACS …, 2018 - ACS Publications
Mycobacterium tuberculosis (M. tb) has the extraordinary ability to adapt to the
administration of antibiotics through the development of resistance mechanisms. By rapidly …

Approaches for targeting the mycobactin biosynthesis pathway for novel anti-tubercular drug discovery: Where we stand

M Shyam, D Shilkar, G Rakshit… - Expert opinion on drug …, 2022 - Taylor & Francis
Introduction Several decades of antitubercular drug discovery efforts have focused on novel
antitubercular chemotherapies. However, recent efforts have greatly shifted toward …

Mycobactin analogues with excellent pharmacokinetic profile demonstrate potent antitubercular specific activity and exceptional efflux pump inhibition

M Shyam, H Verma, G Bhattacharje… - Journal of Medicinal …, 2022 - ACS Publications
In this study, we have designed and synthesized pyrazoline analogues that partially mimic
the structure of mycobactin, to address the requirement of novel therapeutics to tackle the …

Antituberculosis drugs: reducing efflux= increasing activity

L Rodrigues, T Parish, M Balganesh, JA Ainsa - Drug Discovery Today, 2017 - Elsevier
Highlights•Efflux pumps are membrane proteins involved in the transport of antimicrobial
drugs.•Inhibition of efflux systems can prevent drug resistance.•Strategies to avoid …

Genetics and roadblocks of drug resistant tuberculosis

J Perdigão, I Portugal - Infection, Genetics and Evolution, 2019 - Elsevier
Considering the extensive evolutionary history of Mycobacterium tuberculosis, anti-
Tuberculosis (TB) drug therapy exerts a recent selective pressure. However, in a …