Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans[1].
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Chloramphenicol is a broad-spectrum antibiotic.Target: AntibacterialChloramphenicol is a bacteriostatic drug that stops bacterial growth by inhibiting protein synthesis. Chloramphenicol prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome. It specifically binds to A2451 and A2452 residues in the 23S rRNA of the 50S ribosomal subunit, preventing peptide bond formation. While chloramphenicol and the macrolide class of antibiotics both interact with ribosomes, chloramphenicol is not a macrolide. It directly interferes with substrate binding, whereas macrolides sterically block the progression of the growing peptide [1, 2].
G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity[1].
Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacterium tuberculosis.
Robenidine hydrochloride is an anticoccidial agent which is also active against MRSA and VRE with MIC50s of 8.1 and 4.7 μM, respectively.
DNA Gyrase-IN-4 (compound 8p) is a potent DNA gyrase inhibitor, with an IC50 of 0.13 μM. DNA Gyrase-IN-4 shows excellent antibacterial activity against Staphylococcus aureus, Listeria monocytogenes, Salmonella and Escherichia coli, with MIC values of 0.05, 0.05, 0.05, and 8 μg/mL, respectively[1].
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection[1].
Tilmicosin phosphate is a antibiotic, is used in veterinary medicine for the treatment of bovine respiratory disease and ovine respiratory disease associated with Mannheimia (Pasteurella) haemolytica.
Demethoxyencecalin is a chromene isolated from Helianthus annuus, has antifungal activities[1].
Alvircept sudotox is a recombinant CD4 derived from Pneumonas aeruginosa exotoxin A. Alvircept sudotox can be used in the research of HIV infections[1].
LL-25 is a fragment of LL-37 (HY-P1222) but devoid of the immunomodulatory properties of LL-37. LL-25 has antifungal and candidacidal activity[1].
Cefcapene pivoxil hydrochloride hydrate is a prodrug and an orally active 3rd-generation cephalosporin with broad-spectrum of anti-bacterial activity[1]. Cefcapene pivoxil hydrochloride hydrate is used for the study of palmoplantar pustulosis (PPP) and other infectious diseases[2].
Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.
Urease-IN-10 (Conjugate 4) is a competitive Urease inhibitor, with an IC50 of 3.59±0.07 μM and a Ki of 7.45 μM. Urease-IN-10 is a conjugate consisting of Diclofenac (HY-15036) and Sulfanilamide (HY-B0242). Diclofenac-sulfanilamide inhibits the Jack bean urease(JBU) in a competitive manner[1].
NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM)[1].
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research[1][2][3][4].
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively[1].
Cefetamet is a cephalosporin antibiotic. Cefetamet has the potential for the research of both upper and lower community-acquired respiratory tract infections[1].
BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability[1].
Olanexidine hydrochloride semihydrate is an antibacterial agent. Olanexidine hydrochloride semihydrate is active against a wide range of bacteria, imcluding both Gram-positive and Gram-negative bacteria Olanexidine hydrochloride semihydrate is also an antiseptic. Olanexidine hydrochloride semihydrate can be used in the research of infection and inflammation[1][2][3].
Penflufen is a highly efficient, broad-spectrum succinate dehydrogenase inhibitor (SDHI). Penflufen can be used as a fungicide and has broad bioactivity against many fungal diseases, including potato black scurf, wheat sharp eyespot, rice sheath blight, and root rot in peanut and other similar fungal diseases[1].
8-Abietenic acid is the secondary metabolite of mucorinic acid and is isolated from a solid culture of the fungus Mucor spp. isolated on insect Acalymma bivittula. 8-Abietenic acid exhibits antibacterial and insecticidal activities[1].
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].
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].
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].
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].
Sirpefenicol is a phenicol antibacterial agent. Sirpefenicol can be used in bacterial infections in animals (extracted from patent WO2020068607A1)[1].
Isepamicin (Sch 21420) is an aminoglycoside antibacterial. Isepamicin has better activity against strains producing type I 6'-acetyltransferase. Isepamicin’s antibacterial spectrum includes Enterobacteriaceae and staphylococci. Anaerobes, Neisseriaceae and streptococci are resistant. Isepamicin exhibits a strong concentration-dependent bactericidal effect, a long post-antibiotic effect (several hours) and induces adaptive resistance[1].