Infection

Dihydrodaunomycin has antibacterial and antitumor activities.

YKAs3003 is a potent inhibitor of Escherichia coli KAS III (ecKAS III) with antibacterial activity. The minimum inhibitory concentrations (MICs) of YKAs3003 against a variety of bacteria ranged from 128 to 256 μg/mL.

SARS-CoV-2-IN-102 (example 58) is a SARS-CoV papain-like protease (PLpro) inhibitor with an IC₅₀ <100 nM.

Torvoside C (Torvoside K) is a compound found in Solanum torvum with antifungal activity. The ZOIs and MIC values of Torvoside C against the tested fungi (Alternaria brassicicola, Alternaria geophila, Aspergillus flavus, etc.) range from 33.4% to 87.4% and 31.25 to 250 μg/mL, respectively. Additionally, it exhibits a dose-dependent inhibitory effect on the production of mycotoxins aflatoxin B1 and fumonisin B1, which are produced by A. flavus and F. verticillioides, respectively. Torvoside C can be used for research in the field of antifungal infection.

NA808 is an Serine Palmitoyltransferase (SPT) inhibitor. NA808 reduces sphingomyelin synthesis, inhibits its activation in hepatic stellate cells, and decreases the expression of α-SMA protein and mRNA, as well as collagen 1A1 mRNA (IC₅₀ 0.16, 0.12, and 0.11 μM, respectively). NA808 inhibits HCV replication and reduces NS3 and RdRp protein expression in HCV replicon cells without significant cytotoxicity and exhibits almost no immunosuppressive effect at effective concentrations. NA808 demonstrates broad-spectrum antiviral activity in humanized chimeric liver mice infected with various HCV genotypes, and dose-dependently reduces serum and hepatic HCV RNA levels. NA808 can be used for research on non-alcoholic steatohepatitis and hepatitis C virus infection.

Ochracenomicin C is found in the strain of Amicolatopsis sp. MJ 950-891. Ochracenomicin C has a weak antibacterial effect.

GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC₅₀=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND).

Argimicin C is an antibiotic that can be isolated from Sphingomonas sp.. Argimicin C exhibits algicidal activity against a variety of toxic cyanobacteria with MIC of low micromolar levels.

31-Homorifamycin W is an antibiotic found in Amycolatopsis mediterranei.

Dapsone-¹⁵N₂ (4,4′-Diaminodiphenyl sulfone-¹⁵N₂) is ¹⁵N labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al.

Gluconasturtiin is an orally active glucosinolate found in the roots of Brassica juncea and Brassica hirta. Gluconasturtiin acts as a feeding activator for P. maculipennis larvae at low concentrations, while it exhibits toxicity to the larvae at high concentrations.

Galacardin A has anti-Gram-positive bacterial activity.

Sch 29482 is an orally active penem antibiotic with broad-spectrum antibacterial activity.

Monamycin D1 is an ester peptide antibiotic. Monamycin D1 has activity against Gram-positive bacteria.

Antibiotic adjuvant 4 (Compound 13) is an Antibiotic adjuvant and efflux pump inhibitor. Antibiotic adjuvant 4 exhibits potent efflux pump inhibitory activity. Antibiotic adjuvant 4 significantly downregulates virulence-related genes of Staphylococcus aureus when used alone or in combination with antibiotics. Antibiotic adjuvant 4 enhances the efficacy of Ciprofloxacin (HY-B0356) against multiagent-resistant Staphylococcus aureus strains.

GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains.

Antibacterial agent 306 (Compound 8c), a lactate dehydrogenase inhibitor, is a highly effective antibacterial agent, especially effective against Gram-positive bacteria. Antibacterial agent 306 exhibits MIC against Staphylococcus aureus of as low as 1 μg/mL. Antibacterial agent 306 can not only damage membrane integrity and block the replication of DNA by intercalation, but also make reactive oxygen species (ROS) burst. Antibacterial agent 306 can be used for research on anti-multi-drug resistant bacteria.

Thiofanox sulfone is an oxidative metabolite of the insecticide/nematicide Thiofanox.

Mycoplanecin C is a cyclic peptide compound .

TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC₅₀ of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC₅₀ as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC₅₀ of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection.