resistant strain

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.

N-acetyltyramine is a metabolite of the biogenic amine tyramine . It enhances cytotoxicity of doxorubicin in resistant P388 murine leukemia cells with an IC50 value of 0.13 μg ml compared with an IC50 value of 0.48 μg ml for doxorubicin alone.

Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.

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.

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.

HDAC-IN-76 (compound 6i), a histone deacetylase (HDAC) inhibitor, demonstrates robust antimalarial activity, particularly against the asexual blood stages of Plasmodium. The compound exhibits potent efficacy with IC 50 values of 30 nM and 98 nM against Pf3D7 (chloroquine drug-susceptible strain) and PfDd2 (chloroquine drug-resistant strain), respectively. Moreover, HDAC-IN-76 shows selective inhibition towards parasites, displaying IC 50 values of 7 nM and 9 nM against human HDAC1 and HDAC6, respectively, and effectively inhibits PfHDAC1.

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.

Antimicrobial agent-38 (compound 10) effectively inhibits methicillin-resistant Staphylococcus aureus (S. aureus) strain ATCC 700699 and non-resistant strain ATCC 29213, with minimum inhibitory concentrations (MIC) of 32 mg L and 64 mg L, respectively.

6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 |1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).

Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]

Milbemycin A4 oxime, a derivative of milbemycin A4 and a component of milbemycin oxime, exhibits insecticidal and nematocidal activity. At 0.05 mg kg, it reduces microfilariae of the heartworm D. immitis in naturally infested dogs and inhibits the growth of C. glabrata clinical isolates with MIC80 values of 16 to >32 μg ml. At 2.5 μg ml, it blocks fluconazole efflux from C. glabrata clinical isolates (but not from strains lacking CgCDR1 and PDH1 efflux pumps) and reduces MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. Furthermore, it enhances adriamycin-induced inhibition of cell growth, increases intracellular accumulation of adriamycin and the P-glycoprotein substrate rhodamine 123 in adriamycin-resistant, but not adriamycin-sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.

Neospiramycin I is a macrolide antibiotic and derivative of spiramycin I.1It is active against the macrolide-sensitive KB210, but not the macrolide-resistant KB224, strain ofS. aureus(MICs = 3.12 and >100 μg/ml, respectively), as well asB. cereus,B. subtilis,M. luteus,E. coli, andK. pneumoniae(MICs = 1.56, 3.12, 3.12, 0.2, 50, and 12.5 μg/ml, respectively). Neospiramycin I binds toE. coliribosomes with an IC50value of 1.2 μM. It protects against mortality in a mouse model ofS. pneumoniaetype III infection (ED50= 399.8 mg/kg).2

Licoricone exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains.

4,4'-Dicyanostilbene (compound 43) demonstrates potent antimalarial activity against the Dd2 strain with an EC50 value of 27 nM and shows in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA) [1].

RYL-552S is a drug-resistant strain of Plasmodium falciparum that effectively kills the asexual blood stage of the parasite in vitro.

Antimycobacterial agent-3 is an antimycobacterial agent with low cytotoxicity. antimycobacterial agent-3 is effective against sensitive MTB strain H37Rv and resistant clinical isolates (MIC < 0.029-0.110 μ M).

Anti-IAV Agent 1-1a is an orally administered compound effective against the Influenza A virus (IAV), demonstrating inhibitory concentration 50 (IC50) values of 0.03 μM and 0.06 μM for the H1N1 strain and the Oseltamivir-resistant H1N1 strain of IAV, respectively.

Wychimicin C, a spirotetronate polyketide isolated from the rare actinomycete, Actinocrispum wychmicini strain MI503-AF4, demonstrates potent antibacterial efficacy. Specifically, it exhibits significant activity against methicillin-resistant Staphylococcus aureus (IC 50 =0.125-0.5 μg mL) and Enterococcus faecalis faecium (IC 50 =0.125-0.25 μg mL) [1] [2].

Wychimicin A, a spirotetronate polyketide isolated from the rare actinomycete Actinocrispum wychmicini strain MI503-AF4, exhibits potent antibacterial activity. Specifically, it demonstrates efficacy against methicillin-resistant Staphylococcus aureus (IC 50 = 0.125-0.5 μg mL) and Enterococcus faecalis faecium (IC 50 = 0.125-0.25 μg mL) [1] [2].

HIV-1 Inhibitor-58 (Compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain IIIB and NNRTI-resistant strains like K103N and E138K in MT-4 cells at an EC50 of less than 50 nM. Additionally, it inhibits CYP2C9 and CYP2C19 with IC50 values of 2.06 μM and 1.91 μM, respectively. This compound is utilized in HIV infection research [1].

Antimycobacterial agent-6 (compound 25) effectively inhibits Mycobacterium tuberculosis, including wild-type and fluoroquinolone-resistant strains, by targeting the Mtb DprE1-C387S mutant, with minimal inhibitory concentrations (MIC90) of 0.9 μM for H37Rv and MoxR strains, and 0.5 μM for the DprE1-P116S strain [1].

Antitubercular agent-39 (Compound P1) is a potent agent effective against both drug-resistant and drug-susceptible clinical isolates of tuberculosis, inhibiting the Mtb strain H37Rv with a minimum inhibitory concentration (MIC) of less than 1 μM [1].

DprE1-IN-5 (Compound 10), a potent DprE1 inhibitor, exhibits anti-TB activity with an MIC of 4 μM against the Mtb H37Rv strain and demonstrates antimycobacterial efficacy against drug-resistant strains. Additionally, it possesses high microsomal stability [1].

DprE1-IN-6 (Compound 56) is a DprE1 inhibitor with anti-TB activity, showing a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain and efficacy against drug-resistant mycobacterial strains. Additionally, it has high microsomal stability and medium clearance [1].