Microbiology

Maribavir is an UL97 kinase inhibitor potentially for the treatment of cytomegalovirus (CMV) infection. The mechanism by which maribavir inhibits HCMV replication is by inhibition of an HCMV encoded protein kinase enzyme called UL97 or pUL97.

RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ??0.12 μg/ml.

Ridinilazole is a novel antibacterial with MICs range of 0.06-0.25??g/mL (MIC90=8??g/mL) against C.?difficile.

Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.

Penthiopyrad(MTF-753) is a carboxamide fungicide used to control a broad spectrum of diseases on large variety of corps; inhibits fungal respiration by binding to mitochondrial respiratory complex II.

Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; fungicide.

Sarolaner (PF-6450567) is an orally active, broad-spectrum ectoparasiticide, has efficacy against fleas and ticks on dogs, with LC80 of 0.3 μg/mL against C. felis and an LC100 of 0.003 μg/mL against O. turicata.

Tolfenpyrad is a pesticide that was first approved in 2002 in Japan.

Merimepodib is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.

Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum.

ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.

Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2'-oxidase) inhibitor.

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.

(Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.

Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.

RSV604 racemate is a racemic mixture, shows less potency against strains of respiratory syncytial virus (RSV) than the S-isomer.

Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM.

Cenobamate (YKP-3089) is a novel antiepileptic drug candidate with broad-spectrum anticonvulsant activity.

FOY 251, an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor. FOY 251 inhibits SARS-CoV-2 infection in cells assay.

Sisunatovir, also known as RV521, is a highly potent fusion inhibitor with efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses.

Merafloxacin, also known as CI 934, is a fluoroquinolone antibacterial, which was also identified as a -1 PRF inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on -1 PRF of other beta coronaviruses. Importantly, frameshift inhibition by merafloxacin substantially impedes SARS-CoV-2 replication in Vero E6 cells, thereby providing the proof of principle of targeting -1 PRF as an effective antiviral strategy for SARS-CoV-2.

Elsulfavirine is a new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) being developed by Viriom for the treatment and prevention of human immunodeficiency virus (HIV) infections. It is the prodrug of the active compound VM-1500A, a small molecule selective NNRTI, which prevents HIV replication.

Riamilovir, also known as Triazavirin, is a nucleoside analogue of nucleic acid and an antiviral agent, works by inhibiting the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is shown active in inhibition of the tick-borne encephalitis virus reproduction (strain Sofiin) by accumulation in the SKEV cell culture.

AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.

SMAP-29, a promising antiinfective agent, is a broad spectrum antibacterial and antifungal α-helical cathelicidin-derived peptide. SMAP-29 acts by permeabilizing bacterial membranes and inducing remarkable changes in the surface morphology of susceptible microorganism.

Dermaseptin, a peptide isolated from frog skin, exhibits potent antimicrobial activity against, bacteria, fungi, and protozoa at micromolar concentration.