drug-resistant

iKIX1 is an Pdr1-dependent gene activation. It re-sensitizes drug-resistant C. glabrata to azole antifungals in vitro and in animal models for disseminated and urinary tract C. glabrata infection.

DCZ0415 induces antimyeloma activity in vitro, in vivo and in primary cells of drug-resistant myeloma patients. DCZ0415 is a potent TRIP13 inhibitor that can impair the repair of non-homologous end junctions and inhibit NF-κB activity.

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

Tectol has anti-plasmodial activity, it as a moderately active growth inhibitor with an IC50 3.44±0.20μM. It exhibited significant activity against human leukemia cell lines HL60 and CEM. Tectol may cause itchy dermatitis, the dermatitis appeared on the n

D-Cycloserine (RO-1-9213) is a broad spectrum antibiotic used as a second line agent for treatment of drug resistant tuberculosis, always in combination with other antituberculosis agents.

Fosfomycin calcium (Phosphomycin calcium salt) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis.

An antibiotic produced by Streptomyces fradiae.

Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis.

Fenamic acid (N-Phenylanthranilic acid) is a chloride channel blocker that causes renal papillary necrosis in rats. Fenamic acid serves as a parent structure for several nonsteroidal anti-inflammatory drugs (NSAIDs), including flufenamic acid, tolfenamic acid, mefenamic acid, and meclofenamic acid.

Sulbactam sodium (CP-45899-2) (Unasyn) is an irreversible β-lactamase inhibitor.

Batabulin (T138067) is an antitumor compound that binds covalently and selectively to a subset of the β-tubulin isotypes, disrupting microtubule polymerization. This disruption affects cell morphology, induces cell-cycle arrest, and ultimately leads to apoptotic cell death.

LtaS-IN-1 is an effective inhibitor of Lipoteichoic acid synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 is against Enterococcus spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 inhibits strain E1630 and E1590 with MIC values of 0.5 μg/mL.

Sulbactam (CP45899) is a semi-synthetic beta-lactamase inhibitor. The beta-lactam ring of sulbactam irreversibly binds to beta-lactamase at or near its active site, thereby blocking enzyme activity and preventing metabolism of other beta-lactam antibiotics by the enzyme. Combining this agent with a beta-lactamase susceptible antibiotic, such as penicillins or a cephalosporin, to treat infections caused by beta-lactamase producing organisms, results in a decreased turnover rate of the beta-lactamase sensitive antibiotic and enhances its antibacterial activity.

Artelinic acid is a water-soluble artemisinin analog with antimalarial activity and is used for the treatment of multi-drug resistant strains of Plasmodium falciparum.

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.

Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci, enterococci and streptococci, as well as anaerobic bacteria.

Benzquinamide (P2647), an antiemetic agent with anticancer activity, inhibits p-glycoprotein-mediated drug efflux and potentiates the cytotoxicity of anticancer drugs in multidrug-resistant cells.The Ki values of Benzquinamide for α2A, α2B, and α2C adrenergic receptor (α2-AR) were 1,365, 691, and 545 nM, respectively. 545 nM, respectively.

Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) is a cell-permeable microtubule destabilizer that induces cell cycle arrest and apoptosis in G2/M phase. Suprafenacine binds to microtubules and inhibits aggregation at the colchicine junction. Suprafenacine is selective for cancer cells, including drug-resistant cancer cells.

Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR/ABL and BCR/ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.

Anticonvulsant agent 2 is a potent, orally active anticonvulsant demonstrating antiepileptic activity in a drug-resistant epilepsy model.

GSK2556286 (GSK286) is an orally active inhibitor of Mycobacterium tuberculosis (M. tuberculosis), effective against multidrug-resistant (MDR), extensively drug-resistant (XDR), and drug-sensitive (DS) strains. It inhibits the growth of human macrophages with an IC50 value of 0.07 μM.

Moxifloxacin (Avelox) is a fourth-generation fluoroquinolone that has been shown to be effective against Gram-positive, Gram-negative, and atypical strains, as well as multi-drug resistant Streptococcus pneumoniae.

Linezolid (PNU-100766), the first of the oxazolidinone class, is a synthetic antibiotic used for the therapy of infections resulted from multi-resistant bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and streptococcus. The drug takes effect as the inhibitor of the initiation of bacterial protein synthesis.

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.