[HTML][HTML] Bottlenecks and opportunities in antibiotic discovery against Mycobacterium tuberculosis

PD Craggs, LPS de Carvalho - Current Opinion in Microbiology, 2022 - Elsevier
Highlights•“Old” molecules and targets represent attractive start points.•Modern medicinal
chemistry is essential to convert a compound hit into a drug.•Nutritional flexibility makes …

Natural products and their analogues acting against Mycobacterium tuberculosis: A recent update

G Kumar - Drug Development Research, 2023 - Wiley Online Library
Tuberculosis (TB) remains one of the deadliest infectious diseases caused by
Mycobacterium tuberculosis (M. tb). It is responsible for significant causes of mortality and …

Development of 2nd generation aminomethyl spectinomycins that overcome native efflux in Mycobacterium abscessus

GA Phelps, MN Cheramie… - Proceedings of the …, 2024 - National Acad Sciences
Mycobacterium abscessus (Mab), a nontuberculous mycobacterial (NTM) species, is an
emerging pathogen with high intrinsic drug resistance. Current standard-of-care therapy …

A modified BPaL regimen for tuberculosis treatment replaces linezolid with inhaled spectinamides

MZ Ali, TS Dutt, A MacNeill, A Walz, C Pearce, H Lam… - Elife, 2024 - elifesciences.org
The Nix-TB clinical trial evaluated a new 6 month regimen containing three oral drugs;
bedaquiline (B), pretomanid (Pa), and linezolid (L)(BPaL regimen) for the treatment of …

Spectinamide MBX-4888A exhibits favorable lesion and tissue distribution and promotes treatment shortening in advanced murine models of tuberculosis

AA Bauman, JP Sarathy, F Kaya… - Antimicrobial Agents …, 2024 - journals.asm.org
The spectinamides are novel, narrow-spectrum semisynthetic analogs of spectinomycin,
modified to avoid intrinsic efflux by Mycobacterium tuberculosis. Spectinamides, including …

Investigation of the antimycobacterial activity of African medicinal plants combined with chemometric analysis to identify potential leads

P Moyo, M Ofori, OS Bodede, M Wooding… - Scientific Reports, 2024 - nature.com
The emergence of drug-resistant Mycobacterium tuberculosis strains is a threat to global
health necessitating the discovery of novel chemotherapeutic agents. Natural products drug …

“Upcycling” known molecules and targets for drug-resistant TB

C Roubert, E Fontaine, AM Upton - Frontiers in Cellular and Infection …, 2022 - frontiersin.org
Despite reinvigorated efforts in Tuberculosis (TB) drug discovery over the past 20 years,
relatively few new drugs and candidates have emerged with clear utility against drug …

Development of a Minimalistic Physiologically Based Pharmacokinetic (mPBPK) Model for the Preclinical Development of Spectinamide Antibiotics

KR Parmar, PB Lukka, S Wagh, ZH Temrikar, J Liu… - Pharmaceutics, 2023 - mdpi.com
Spectinamides 1599 and 1810 are lead spectinamide compounds currently under
preclinical development to treat multidrug-resistant (MDR) and extensively drug-resistant …

Characterization of spectinamide 1599 efficacy against different mycobacterial phenotypes

ZH Temrikar, S Kodidela, S Kumar, J Liu, GT Robertson… - Tuberculosis, 2023 - Elsevier
Spectinamides are a novel series of spectinomycin analogs being developed for the
treatment of tuberculosis. The preclinical lead spectinamide 1599 is an antituberculosis drug …

The rabbit model for spinal tuberculosis: An overview

J Jia, M Zhang, Z Cao, X Hu, S Lei… - Journal of …, 2024 - journals.sagepub.com
Mycobacterium tuberculosis infection has emerged as a global public health issue,
predominantly manifesting as pulmonary tuberculosis. Bone and joint tuberculosis, with …