Infection

N-Phenylacetyl-L-homoserine lactone is a small diffusible signaling molecule that strongly antagonizes or super-activates the quorum sensing of Vibrio fischeri.

SSF-109 is a broad-spectrum fungicide which has protective activity against plant disease. SSF-109 inhibits the biosynthesis of ergosterol at the 14α-demethylation step in Botrytis cinerea.

Bisdemethoxycurcumin is an orally effective curcuminoid. Bisdemethoxycurcumin downregulates pro-inflammatory cytokines in macrophages by inhibiting the phosphorylation of PI3K/Akt and p38 MAPK. Bisdemethoxycurcumin relieves autophagy inhibition and promotes lipophagy to clear vascular smooth muscle foam cells by inhibiting the PDK1/Akt/mTOR pathway. Bisdemethoxycurcumin activates the cAMP/Epac/AMPKα axis and the NRF2/HO-1 antioxidant axis, thereby indirectly inhibiting the phosphorylation of NF-κB p65 and pro-inflammatory outputs such as IL-1β/IL-6/TNF-α, so as to alleviate pulmonary oxidative stress, inflammatory infiltration and pulmonary edema. Bisdemethoxycurcumin blocks NLRP3-mediated pyroptosis and protects cartilage extracellular matrix degradation by activating NRF2/HO-1. Bisdemethoxycurcumin also exerts a synergistic effect with potassium iodide against Candida.

Ditiocarb-d₁₀ sodium (Sodium diethyldithiocarbamate-d₁₀) is the deuterium labeled Ditiocarb sodium (HY-B1637). Ditiocarb sodium (Sodium diethyldithiocarbamate) is an orally active copper reagent. Ditiocarb sodium exhibits activities such as antioxidation, chelation, anti-tumor effects, immunomodulation, and anti-HIV properties. Ditiocarb sodium can be used in the research of tumors, inflammatory, and immune-related diseases.

Antitrypanosomal agent 12 is a C20-phenylthiourea with trypanocidal and cytotoxic activities. Antitrypanosomal agent 12 shows antitrypanosomal activity with 50% growth inhibition (GI₅₀) values of 0.22 μM. Antitrypanosomal agent 12 induces faster cell swelling in bloodstream-form trypanosomes than Salinomycin (HY-15597).

DENV-IN-4 is a potent DENV inhibitor (DENV EC₅₀=4.79 μM, Vero CC₅₀>100 μM, SI>20.9). DENV-IN-4 can inhibit the expression level of DENV2 with concentration-dependence and reduce RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 has antiviral effect.

Trypanothione synthetase-IN-4 is a L. infantum trypanothione synthetase (TryS) inhibitor, and the activity is dependent on the concentration of the polyamine substrate. Trypanothione synthetase-IN-4 has potent antileishmanicidal activity with an EC₅₀ value of 0.6 μM and a selectivity index of 35. Trypanothione synthetase-IN-4 can be used for the research of leishmaniasis.

Antiviral agent 18 (Compound 5) is an anti-infection agent. Antiviral agent 18 results in good antiviral activity against murine norovirus. Antiviral agent 18 has the potential for the research of infectious and malignant diseases.

FAM labled Ozisiran sodiumis a FAM labled Ozisiran sodium.

Antifungal agent 75 (compound 6r) is a potent antifungal agent against Candida albicans. Antifungal agent 75 significantly inhibits the formation of C. albicans biofilm, increases the permeability of the cell membrane, reduces the ergosterol level of the cell membrane, damages the membrane structure, and destroys the integrity of the cell structure to exert excellent antifungal activity.

DS-22-inf-021 is a neuraminidase (NA) inhibitor. DS-22-inf-021 has antiviral activity against influenza viruses.

Wychimicin C is a spirotetronate polyketide, can be isolated from the rare actinomycete Actinocrispum wychmicini strain MI503-AF4. Wychimicin C shows strong antibacterial activity against methicillin-resistant Staphylococcus. aureus (IC₅₀=0.125-0.5 μg/mL) and Enterococcus. faecalis/faecium (IC₅₀=0.125-0.25 μg/mL).

6"'-Deamino-6"'-hydroxyparomomycin I is an amino glycosyl antibiotic that can be produced by Streptomyces rimosus forma paromomycinus A67 15. It is active against both Gram-positive and Gram-negative bacteria. 6"'-Deamino-6"'-hydroxyparomomycin I can be used as an intermediate in the biosynthesis of paromomycin.

Nanangenine F is a drimane sesquiterpenoid with weak antibacterial and anticancer activities. Nanangenine F inhibits Bacillus subtilis (ATCC 6633) with an IC₅₀ of 78 µg/mL. Nanangenine F inhibits NS-1, DU-145, MCF-7 and human fibroblast NFF cells with IC₅₀s of 49 µg/mL, 95 µg/mL, 49 µg/mL, and 84 µg/mL, respectively.

Acopafant (Dacopafant; RP 55778) is a potent platelet-activating factor antagonist. Acopafant inhibits the induction of human immunodeficiency virus (HIV) expression in chronically infected cells. Acopafant has the potential for the research of HIV infection.

Cap-dependent endonuclease-IN-27 (Compound 8) is an orally active potent cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-27, an antiviral agent, shows activity against influenza B virus. Cap-dependent endonuclease-IN-27 has inhibitory activity against IFV A/WSN/33 (H1N1) polymerase (EC₅₀ = 12.26 nM).

3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC₅₀ and K_i of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19.