Comparative analysis of pharmacodynamics in the C3HeB/FeJ mouse tuberculosis model for DprE1 inhibitors TBA-7371, PBTZ169, and OPC-167832

…, V Gruppo, C Hastings, LK Woolhiser… - Antimicrobial agents …, 2021 - Am Soc Microbiol
Multiple drug discovery initiatives for tuberculosis are currently ongoing to identify and
develop new potent drugs with novel targets in order to shorten treatment duration. One of the …

[PDF][PDF] Bayesian models leveraging bioactivity and cytotoxicity information for drug discovery

…, M Ekonomidis, M Talaue, SD Paget, LK Woolhiser… - Chemistry & biology, 2013 - cell.com
Identification of unique leads represents a significant challenge in drug discovery. This hurdle
is magnified in neglected diseases such as tuberculosis. We have leveraged public high-…

Comparative Studies Evaluating Mouse Models Used for Efficacy Testing of Experimental Drugs against Mycobacterium tuberculosis

…, CL Wells, EJ Brooks, LK Woolhiser… - Antimicrobial agents …, 2011 - Am Soc Microbiol
Methodologies for preclinical animal model testing of drugs against Mycobacterium tuberculosis
vary from laboratory to laboratory; however, it is unknown if these variations result in …

[HTML][HTML] Effects of P-MAPA immunomodulator on toll-like receptors and p53: potential therapeutic strategies for infectious diseases and cancer

…, OS Nunes, FRF Seiva, IS Nunes, LK Woolhiser… - Infectious agents and …, 2012 - Springer
Background Compounds that can act as agonists for toll-like receptors (TLRs) may be
promising candidates for the development of drugs against infectious diseases and cancer. The …

Novel pyridopyrazine and pyrimidothiazine derivatives as FtsZ inhibitors

…, LJ Ross, WJ Suling, EL White, LK Woolhiser… - Bioorganic & medicinal …, 2011 - Elsevier
A series of pyridopyrazine and pyrimidothiazine derivatives have been synthesized and their
activity against FtsZ from Mycobacterium tuberculosis (Mtb) and in vitro antibacterial activity …

Discovery of a cofactor-independent inhibitor of Mycobacterium tuberculosis InhA

…, B Sunde, L Flint, LK Woolhiser… - Life Science …, 2018 - life-science-alliance.org
New antitubercular agents are needed to combat the spread of multidrug- and extensively
drug-resistant strains of Mycobacterium tuberculosis. The frontline antitubercular drug …

A Novel Metabolite of Antituberculosis Therapy Demonstrates Host Activation of Isoniazid and Formation of the Isoniazid-NAD+ Adduct

S Mahapatra, LK Woolhiser, AJ Lenaerts… - Antimicrobial agents …, 2012 - Am Soc Microbiol
One of the most effective and widely used antituberculosis (anti-TB) drugs is isoniazid (INH),
a prodrug activated via oxidation that forms an adduct with NAD + to inhibit NADH-…

[HTML][HTML] Pentacyclic Nitrofurans with In Vivo Efficacy and Activity against Nonreplicating Mycobacterium tuberculosis

Rakesh, DF Bruhn, MS Scherman, LK Woolhiser… - PLoS …, 2014 - journals.plos.org
The reductively activated nitroaromatic class of antimicrobials, which include nitroimidazole
and the more metabolically labile nitrofuran antitubercular agents, have demonstrated some …

Importance of Confirming Data on the In Vivo Efficacy of Novel Antibacterial Drug Regimens against Various Strains of Mycobacterium tuberculosis

MA De Groote, V Gruppo, LK Woolhiser… - Antimicrobial agents …, 2012 - Am Soc Microbiol
In preclinical testing of antituberculosis drugs, laboratory-adapted strains of Mycobacterium
tuberculosis are usually used both for in vitro and in vivo studies. However, it is unknown …

Mouse model for efficacy testing of antituberculosis agents via intrapulmonary delivery

M Gonzalez-Juarrero, LK Woolhiser… - Antimicrobial agents …, 2012 - Am Soc Microbiol
Here we describe an experimental murine model that allows for aerosolized antituberculosis
drug efficacy testing. Intrapulmonary aerosol delivery of isoniazid, capreomycin, and …