multi-drug

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

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.

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.

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.

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Etzadroxil (Ethyl 2-Ethylbutyrate) is an orally available and volatile esterification with broad-spectrum antimicrobial activity, effective in treating urinary tract infections caused by multi-drug resistant bacteria.

Duocarmycin GA, an antibody drug conjugate (ADC) toxin and a DNA alkylating agent, effectively targets and binds in the minor groove of DNA. It is particularly potent against multi-drug resistant cell lines, offering a strategic approach in combating resistance.

Duocarmycin MA, an antibody drug conjugates (ADCs) toxin, is a DNA alkylating agent that binds in the minor groove and can be used against multi-drug resistant cell lines.

Duocarmycin MB, an antibody-drug conjugate (ADCs) toxin, is a DNA alkylating agent that binds in the minor groove and can be used against multi-drug resistant cell lines.

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor used to treat multi-drug resistant gram-negative bacterial infections.

Mtb-IN-8 (compound 5jb) serves as an orally active inhibitor specifically targeting Mycobacterium tuberculosis (Mtb). It exhibits a minimum inhibitory concentration (MIC) of 0.03 μg mL against H37Rv strains and ranges from 0.125 to 0.06 μg mL against multi-drug resistant Mtb (MDR-Mtb).

BWC0977 is an effective topoisomerase inhibitor that disrupts bacterial DNA replication by targeting both DNA gyrase and topoisomerase IV. The minimum inhibitory concentration (MIC90) of BWC0977 against MDR (multi-drug resistant) Gram-negative bacteria ranges from 0.03 to 2 µg mL.

(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium TFA (Compound 4a) functions as a Gram-negative outer membrane permeabilizer by targeting Met47 in LptA to disrupt LptA LptC interactions, exhibiting synergistic antibacterial activity. This compound, when in the form of (trifluoromethanesulfonate), enhances the efficacy of pol B against both wild-type and multi-drug resistant A. baumannii and E. coli strains. Additionally, (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) serves as an adjuvant for antibiotics combating multi-drug resistant Gram-negative bacteria.

B 746 is an antibacterial agent primarily. B 746 is used in therapy for leprosy and Mycobacterium avium infections as well as against Mycobacterium tuberculosis, including those with multi-drug resistance.

CGI-17341 is an orally active representative of the 5-nitroimidazole series of antimicrobial agents. CGI 17341 inhibits the drug-susceptible and multi-drug-resistant strains of Mycobacterium tuberculosis at concentrations ranging from 0.1 to 0.3 microgram

CP 117227 is a multi-drug resistance regulator.

Evoxanthine is an alkaloid that has been found in O. renieri and has antimalarial and anticancer activities.1,2 It is active against P. falciparum with an IC50 value of 67.6 μg ml.1 Evoxanthine decreases proliferation of nine sensitive and drug-resistant cancer cell lines (IC50s = 6.11-80.99 μM).2 |1. Khalid, S.A., Farouk, A., Geary, T.G., et al. Potential antimalarial candidates from African plants: And in vitro approach using Plasmodium falciparum. J. Ethnopharmacol. 15(2), 201-209 (1986).|2. Kuete, V., Fouotsa, H., Mbaveng, A.T., et al. Cytotoxicity of a naturally occurring furoquinoline alkaloid and four acridone alkaloids towards multi-factorial drug-resistant cancer cells. Phytomedicine 22(10), 946-951 (2015).

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg/ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of

OYYF-175 is an antimicrobial antifolate. OYYF-175 exhibits potent broad-spectrum antibacterial activities, especially against multi-drug resistant Gram-Negative-strains. OYYF-175 is an inhibitor of dihydrofolate reductase (DHFR) with an IC 50 of 2.36 nM for Escherichia coli DHFR.

Antibacterial agent 106 (compound 8) is a highly effective orally active antibacterial compound with antibiofilm activity, demonstrating potent antibacterial effects against multi-drug resistant (MDR) Gram-positive pathogens, including the eradication of 99.7% of intracellular methicillin-resistant S. aureus (MRSA) harbored within macrophages [1].