multidrug-resistant

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.

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.

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.

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

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.

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.

Valspodar (PSC 833) is a small-molecule inhibitor and a P-glycoprotein (P-gp) inhibitor with high selectivity and chemosensitizing properties. This compound can effectively reverse P-gp-mediated multidrug resistance (MDR) and is used in experimental research on drug-resistant tumors such as advanced epithelial ovarian cancer.

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.

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

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.

Benzyldodecyldimethylammonium chloride dihydrate can be used as an insecticide reagent. It can target drug-resistant bacteria, such as methicillin-resistant Staphylococcus aureus, multidrug-resistant Pseudomonas aeruginosa, etc., in a concentration-dependent manner.

GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral bioavailability.

Kokusaginine is a furoquinoline alkaloid that inhibits acetylcholinesterase (AChE) with an IC50 of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptosis-inducing effects in MCF-7/ADR cells and is utilized in biochemical research focused on cholinesterase inhibition, apoptosis regulation, and multidrug-resistant cancer cell signaling pathways.

Polymyxin B1, a potent antimicrobial lipopeptide derived from Bacillus polymyxa, has potential for treating multidrug-resistant Gram-negative bacterial infections.

SPR206 is a polymyxin analogue and an important class of antibiotic for the treatment of bacterial infections due to multidrug resistant Gram-negative pathogen.

BRD9185 is an inhibitor of Dihydroorotate dehydrogenase (DHODH) with an EC50 of 16 nM against multidrug-resistant blood-stage parasites in vitro.

GNF179, an optimized 8,8-dimethyl IP analog, exhibits potency (4.8 nM against the multidrug-resistant strain W2), in vitro metabolic stability, and in vivo oral bioavailability.

CN-CC-861 is a broad-spectrum antibiotic that exhibits antimicrobial activity against both sensitive and multidrug-resistant bacteria. It demonstrates potent bactericidal activity in vivo.

Bcl-2-IN-22 (compound 1), a gold (I) NHC complex, exhibits anticancer activity. It induces cell death (apoptosis) via the mitochondrial pathway with an IC50 value of 0.014 μM. Additionally, Bcl-2-IN-22 targets members of the BCL-2 family, promoting apoptosis and sensitization in multidrug-resistant leukemia cells overexpressing BCL-2.

BWC0977 is an effective topoisomerase inhibitor that disrupts bacterial DNA replication by targeting both DNA gyrase and topoisomerase IV. BWC0977 exhibits a minimum inhibitory concentration (MIC90) against multidrug-resistant Gram-negative bacteria ranging from 0.03 to 2 µg/mL. BWC0977 is therefore applied in antibacterial pharmacology research to investigate dual topoisomerase inhibition mechanisms and resistance profiles in Gram-negative bacterial model systems.

Villalstonine, a bisindole alkaloid, exhibits a broad spectrum of bioactivities, including anticancer, antimalarial, and anti-amoebic properties. It demonstrates potent antimalarial activity against the multidrug-resistant Plasmodium falciparum K1 strain, with an IC50 value of 0.27 μM.