Tectoquinone (2-Methylanthraquinone) is a SARSCoV-2 main protease inhibitor against COVID-19. Tectoquinone exhibits strong mosquito larvicidal activity with the LC50 values of 3.3 and 5.4 μg/ml against A. aegypti and A. albopictus in 24 h, respectively[1][2].
Herbicidin A is an adenosine-derived nucleoside antibiotic, but also is a herbicide against dicotyledonous plants. Herbicidin A can be isolated from Streptomyces scopuliridis M40[1][2].
T-705RTP sodium is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP sodium is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity[1][2].
Ferroquine is an ingenious antimalarial agent.
MIV-150 is a nonnucleoside reverse transcriptase (NNRT) inhibitor, blocking HIV-1 and HIV-2 infections, with an EC50<1 nM against HIV-1/HIV-2MN.
Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
Sandramycin ia a cyclic depsipeptide antibiotic isolated from cultured broth of a Nocardioides sp. Sandramycin is also a DNA intercalator that potently binds DNA and is an ADC cytotoxin. Sandramycin is active against Gram-positive bacteria and has potent antitumor activity[1][2][3].
BMAP-18 is a biological active peptide. (BMAP-18 is a truncated form of the antimicrobial peptide BMAP-27. Bovine myeloid antimicrobial peptide-27 (BMAP-27) belongs to the Cathelicidin family of peptides which displays rapid bactericidal activity against Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. BMAP-27 is cytotoxic to human erythrocytes and neutrophils, although at higher than microbicidal concentrations. BMAP-18 displays much higher cell selectivity as compared to parental BMAP-27 because of its decreased hemolytic activity and retained antimicrobial activity.)
Temporin B is an antimicrobial peptide against Legionella pneumophila[1].
Pyrimorph is a fungicide with excellent antifungal activity against oomycetes[1].
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities[1].
Azaribine (2',3',5'-Tri-O-acetyl-6-azauridine) is a potent orotidine monophosphate decarboxylase (OMPD) inhibitor. Azaribine is an antiviral inhibitor of several RNA viruses and inhibits viral genome replication and gene transcription. Azaribine shows broad-spectrum antiviral activity (EC50=3.80 nM-1.73 μM against influenza A and B viruses; EC50=1.62 μM against ZIKV Paraiba). Azaribine, a triacetate salt of Azauridine, has the potential for psoriasis research[1][2].
Caffeic acid-13C3 (3,4-Dihydroxycinnamic acid-13C3) is an 13C labeled caffeic acid. Caffeic acid is a phytonutrient belonging to the flavonoids. Caffeic acid and its derivatives, are potential antimicrobial agents, chronic infection induced by microbes such as bacteria, fungi, and viruses[1].
Dermaseptin-S3 is an antimicrobial peptide derived from frog skin against filamentous fungi[1].
TAT-HA2 Fusion Peptide is a peptide-based delivery agent that combines the pH-sensitive HA2 fusion peptide from Influenza and the cell-penetrating peptide TAT from HIV. TAT-HA2 Fusion Peptide induces the cellular uptake of macromolecules into endosomes via the TAT moiety and to respond to the acidifying lumen of endosomes to cause membrane leakage and release of macromolecules into cells via the HA2 moiety[1].
2'-Hydroxy-2-methoxychalcone (compound 3b) is a synthetic chalcone, with antimicrobial activity[1].
Aurodox is an antibiotic obtained from a streptomyces variant, Aurodox can against a number of gram-positive bacteria. Aurodox shows a very low toxicity in mice and promoted poultry growth[1].
Maraviroc is a selective CCR5 antagonist with activity against human HIV.
Enoxacin-d8 (AT 2266-d8) is the deuterium labeled Enoxacin. Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing[1][2][3][4].
BRD-K98645985 is a class of 12-membered macrolactam and a BAF (Brg/Brahma-associated factors) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, and without T cell activation or toxicity[1].
Human milk lysozyme is the lysozyme found in human milk. Human milk lysozyme is thought to be a key defense factor in protecting the gastrointestinal tract of newborns against bacterial infection[1].
Captan is a common agricultural fungicide used to control Botrytis, Fusarium, Fusicoccum, Pythium. Captan enhances denitrifying and total culturable bacteria[1].
Nifuroxime is an anti-infective agent. Nifuroxime can be used in the research of fungal infections[1].
CI-39 is an antiviral natural product. CI-39 is an NNRTI (non-nucleoside reverse transcriptase inhibit) antiviral agent with an EC50 of 3.40 µM and an CC50 of >30 µM for wild type HIV-1. CI-39 inhibits HIV-1 RT DNA polymerase and ribonuclease H activitiessup[1].
EcAMP3 is a hairpin-like peptide. EcAMP3 has antifungal and antibacterial activity. EcAMPs precursor family contains seven identical cysteine motifs: C1XXXC2(11–13)C3XXXC4[1].
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with IC50 of 2.6 uM.IC50 Value: 2.6 uM [1]Target: PLpro; SARS-CoVin vitro: PLpro inhibitor is a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have IC50 value of 2.6 ± 0.1 μM. PLpro inhibitor display significant antiviral activity with EC50 values of 13.1±0.7 uM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlates with the in vitro inhibition of PLpro, suggesting that the compounds work directly on the enzyme in cells [1,2].in vivo:
Pinellic acid is a natural product that could be isolated from a medicinal plant Pinelliae tuber. Pinellic acid is an effective oral adjuvant for nasal influenza vaccine[1].
Potassium Gluconate (Potassium D-gluconate) is an orally active carboxylic acid by the oxidation with antiseptic and chelating properties[1].
Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity[1][2].
SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomerof the octahydroisochromene scaffold, directs the P1 site imidazole[1].