MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.IC50 Value: 2.6 nM for HIV IntegraseTarget: HIV IntegraseMK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection. MK-2048 inhibits subtype B and subtype C integrase activities. MK-2048 inhibits R263K mutants slightly more effectively than G118R mutants. MK-2048 inhibits S217H intasome and, by contrast, MK-2048 remains fully active against the N224H intasome. MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. MK-2048 is active against viruses resistant to RAL and EVG. MK-2048 exposure leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. MK-2048, with continued pressure, subsequently leads to an additional substitution, at position E138K, after 29 weeks, within the IN gene. Although the G118R mutation alone confers only slight resistance to MK-2048 but not to RAL or EVG, its presence arouses a dramatic reduction in viral replication capacity compared to wild-type NL4-3. E138K both partially restores viral replication capacity and also contributes to increased levels of resistance against MK-2048.
Ertapenem sodium is a new long-acting 1-β-methyl carbapenem antibiotic with a broad antibacterial spectrum including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases.
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties[1][2].
Oseltamivir (GS 4104) is an orally active influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC50s of 0.67, 0.9, 1.34 and 13 nM, respectively[1].
DDX3-IN-2 is an active DEADbox polypeptide 3 (DDX3) inhibitor with an IC50 value of 0.3 μM. DDX3-IN-2 shows a broad spectrum of antiviral activity. DDX3-IN-2 has the potential to overcome HIV resistance[1].
HIV-1 inhibitor-39 (compound 3c) is a potent HIV-1 inhibitor with an EC50 of >112.88 µM. HIV-1 inhibitor-39 shows anti-RT (HIV-1 reverse transcriptase) activities with an IC50 of 15.75 µM. HIV-1 inhibitor-39 shows cytotoxicity for MT-4 cells with an CC50 of 112.9 µM[1].
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination[1][2].
Antifungal agent 14 exhibits broad-spectrum activity against the fungal strains with excellent minimum inhibitory concentration values.
5,6-Dihydroxyindole, a melanin precursor, has a broad-spectrum antibacterial, antifungal, antiviral, antiparasitic activity. 5,6-Dihydroxyindole has cytotoxic effects and is strongly toxic against various pathogens[1].
Metham sodium (Carbathion) is a broad-spectrum soil microbial suppressant. Metham sodium controls soil-borne pests and weeds. Metham sodium inhibits weed seeds, plant-parasitic nematodes, plant pathogenic fungi and soil insects[1].
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM.GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools[1].
13,21-Dihydroeurycomanone, a natural compound isolated from Eurycoma longifolia root, possesses anti-parasite activity for Plasmodium falciparum and Toxoplasma gondii[1][2].
Antibacterial agent 60, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity[1].
Penicillin V (Phenoxymethylpenicillin) is a potent and orally active antibiotic. Penicillin V shows antibacterial activity for Streptococci, Clostridium difficile and staphylococcus aureus. Penicillin V has the potential for the research of otitis, sinusitis, pharyngitis and tonsillitis[1][2][3][4].
Chrysomycin A (Chr-A), an antibiotic, can be obtained from Streptomyces. Chrysomycin A exhibits antitumor and anti-tuberculous and MRSA activities. As for glioblastoma, Chrysomycin A inhibits the proliferation, migration, and invasion of cancer cells through the Akt/GSK-3β/β-catenin signaling pathway[1].
Sutidiazine (ZY-19489) is an orally active and antimalarial agent. Sutidiazine inhibits parasitemia-induced infection. Sutidiazine shows short half-lives (approximately 7 h) and an exposure effect[1].
A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice. Diabetes Phase 2 Clinical
8-Hydroxy-9,10-diisobutyryloxythymol is a natural monoterpenoid with antibacterial properties. 8-Hydroxy-9,10-diisobutyryloxythymol against S. aureus, S. flexneri, and S. paratyphi-B with MIC values of 6.25 μg/mL[1].
Purfalcamine is a potent, specific inhibitor of Plaasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) with IC50 of 17 nM; inhibits proliferation of P falciparum strains (Dd2, FCB, HB3 and W2) with nanomolar EC50s of (171–259 nM); blocks microneme discharge and erythrocyte invasion by P. falciparum merozoites; an anti-malaria parasite agent.
Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively)[1][2][3].
KKL-35 is a trans-translation tagging reaction inhibitor with an IC50 of 0.9 µM.
Cefathiamidine is a first-generation cephalosporin antibacterial agent and is used to treat infections caused by susceptible bacteria. Cefathiamidine exhibits a wide spectrum of antimicrobial activity against bacteria. Cefathiamidine is used for the treatment of respiratory, liver, five senses, urinary tract infections, endocarditis and sepsis[1][2].
Stearyl gallate is an alkyl gallate with a long alkyl chain (carbon number of 18). Stearyl gallate has an antioxidant activity, and a weak antiviral activity against HSV-1[1][2].
FR179642 is a key intermediate in the synthesis of the echinocandin antifungal Micafungin[1]. FR179642 is the cyclic peptide nucleus of the echinocandin-like antifungal lipopeptide FR901379[2].
Dodicin hydrochloride is an effective disinfectant with broad antimicrobial activity[1].
Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity.
Desmethyl Levofloxacin is a metabolite of Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication[1].
Ampicillin sodium is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.