Antitubercular agent-41 (Compound 106) is an antitubercular agent that can be used in the study of Mycobacterium tuberculosis infection[1].
Kanosamine hydrochloride is an antibiotic which inhibits the growth of plant-pathogenic oomycetes, certain fungi and a few bacterial species. Kanosamine inhibits Phytophthora medicaginis M2913 and Aphanomyces euteiches WI-98 with MICs of 25 and 60 µg/mL, respectively.
YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity. IC50 value: 8.4 μM Target: HIVIC50 (=8.4 μM) value of YYA-021 is determined by a single round assay using cYTA48P virus and TZM-bl cells. YYA-021 is broadly distributed in tissues, probably as a result of its hydrophobicity. The plasma concentrations of YYA-021 in both species remained at micromolar levels for several hours post-injection. [1] YYA-021 also enhances the neutralizing activity of KD-247 against simian-human immunodeficiency virus (SHIV)-KS661 strain via highly synergistic interactions. YYA-021 might have promise as a lead compound for the intravenous administration in a cocktail therapy with anti-gp120 monoclonal antibodies such as KD-247 and with co-receptor antagonists such as T140. [2]
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CLpro. 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases[1].
Guanosine-8-d is a deuterium labeled Guanosine. Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity[1].
Filicenol B can be isolated from the whole plant of Adiantum lunulatum. Filicenol B has antibacterial activity[1].
Tirfipiravir is a nucleoside compound and antiviral agent, against the novel coronavirus or influenza virus[1].
RSV-IN-3 (Compound 1) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza virus A (IAV). RSV-IN-3 shows anti-RSV activity (EC50 = 32.70 μM)[1].
QST4 has antitubercular activity, with the MIC value of 6.25 μM in Mycobacterium tuberculosis H37Rv[1].
Efavirenz is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1[1]. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects[2].
Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2].
Carumonam (AMA-1080; Ro 17-2301) is a sulfonated monocyclic β-Lactam Antibiotic, targeting to penicillin-binding protein (PBP). Carumonam exerts highly activity against Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae, while it weakly and even inactively inhibits Streptococcus pneumoniae and Staphylococcus aureus. Carumonam is resistant to beta-lactamase-mediated hydrolysis[1].
PGLa is an antimicrobial peptide. PGLa is known to be bacteriostatic against both Gram-positive and Gram-negative bacteria.
UCM53, a FtsZ inhibitor, is an antibacterial agent. UCM53 can inhibit the growth of clinical isolates of antibiotic-resistant Staphylococcus aureus and Enterococcus faecalis[1]
Anti-infective agent 3 (compound 3l) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.47 and 0.13 μM, respectively. Anti-infective agent 3 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 4 μg/mL[1].
Oxacillin sodium salt is a narrow-spectrum β-lactam antibiotic of the penicillin class.
Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV.
Antifungal agent 70 (compound 13) is a dihydroeugenol-imidazole against multi-resistant Candida auris (MIC: 36.4 μM). Antifungal agent 70 shows antifungal activity[1].
Dryocrassin ABBA (Dryocrassin) is a flavonoid natural product derived from Dryopteris crassirhizoma, with antiviral and antibacterial activities[1][2]. Dryocrassin ABBA exhibits antiviral activity against H5N1 avian influenza virus[1]. Dryocrassin ABBA inhibits the coagulase activity of Staphylococcus aureus vWbp[3]. Dryocrassin ABBA suppresses immunostimulatory function of dendritic cells and prolongs skin allograft survival[4].
HBV-IN-11 is a potent HBsAg secretion inhibitor with an EC50 of 0.46 µM (From patent WO2018085619A1, example 28)[1].
Cymoxanil is a fungicidal against plant diseases caused by fungi belonging to the Perenosporales[1].
Tubercidin (7-Deazaadenosine) is an adenosine analog, is an antibiotic obtained from Streptomyces tubercidicus.Target: AntibacterialTubercidin inhibits the growth of Streptococcus faecalis by 50 % at a concentration of 20 nM. Tubercidin is not subject to cleavage by adenosine phosphorylase or to deamination by adenosine deaminase. The antibiotic served as a substrate for numerous enzymes involved in the anabolism of adenosine, as demonstrated by its incorporation into RNA and DNA, and by the formation of nicotinamide-deaza-adenine dinucleotide. Tubercidin proves to be a weak inhibitor of adenosine phosphorylase, and interfered with the phosphorylation of adenosine and AMP. The inhibition of the growth of S. faecalis by Tubercidin is prevented by purine and pyrimidine nucleosides, ribose 5-phosphate, pyruvate, and certain amino acids. In the presence of Tubercidin, growing cultures of the test organism used pyruvate instead of glucose, whereas in the absence of the antibiotic glucose served as the main source of energy. It is suggested, therefore, that the impairment of growth is due primarily to the interference of Tubercidin with the utilization of glucose.
Nonacosane, isolated from Baphia massaiensis, exhibits weak activities against E. coli, B. subtilis, P. aeruginosa and S. aureus[1].
Erythromycin aspartate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin aspartate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin aspartate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties[1].
L685818 is a specific immunophilin ligand. L685818 was neuroregenerative and non-neuroprotective in primary brain cultures. L685818 protects dopaminergic neurons from toxic inhibition of MPP+ and 6-OHDA, reduces tyrosine hydroxylase (TH) loss, and promotes neuronal process regeneration. L685818 is also an antifungal reagent for Cryptococcus neoformans[1][2].
Bithionol is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.IC50 value:Target: anticaner agentBithionol caused dose dependent cytotoxicity against all ovarian cancer cell lines tested with IC50 values ranging from 19 μM - 60 μM. BT treatment resulted in cell cycle arrest at G1/M phase and increased ROS generation [1]. Both bithionol and bithionol sulphoxide demonstrated in vitro toxicity to Neoparamoeba spp. at all concentrations examined (0.1 to 10 mg l(-1) over 72 h), with a comparable toxicity to freshwater observed for both chemicals at concentrations > 5 mg l(-1) following a 72 h treatment [2].
Propamocarb is a systemic fungicide. Propamocarb is widely used to protect cucumbers, tomatoes and other plants from pathogens[1].
Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research[1][2][3][4].