Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
Macrocarpal B is an antibacterial compounds. Macrocarpal B can be isolated from the branch of Eucalyptus globulus. Macrocarpal B can be used for the research of periodontal disease[1].
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe2+ and Zn2+ ions from the biofilm matrix.
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2].
5-Fluorouracil-13C4,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Arbemnifosbuvir is a nidovirus DdRp-associated nucleotidyltransferase (NiRAN) domain of non-structural protein 12 (nsp12)-interfering drugs. Arbemnifosbuvir can be used for SARS-CoVs infection research[1].
Aromadendrene can be isolated from Eucalyptus globulus. Aromadendrene has antimicrobial activity[1].
Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.Target: AntibacterialOlsalazine is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Olsalazine is potent inhibitors of human intestinal macrophages chemotaxis to LTB4 with IC50 of 0.39 mM. Olsalazine (0.4 mM) inhibits the superoxide radical production generated by phorbol myristate acetate (PMA)-activated neutrophils or by xanthine-xanthine oxidase reaction by reduction of 31% and 73%, respectively. Olsalazine inhibits tumor growth in a rodent model of colorectal cancer. In 1,2-dimethylhydrazine-treated rats, Olsalazine (25 mg/kg/day) decreases number and volume of tumors by 58.17% and 62.67%, respectively. Administration of Olsalazine induces a 1.7-fold times increase in the number of apoptotic cells, companied with a reduction of 42.4% in cell proliferation rate.
Crotalicidin is an antimicrobial peptide and anti-tumor peptide that can effectively inhibit the activity of Gram-negative bacteria and tumor cells. Crotalicidin can be obtained from rattlesnake venom. Crotalicidin can be used in the study of microbial infections and cancer[1].
RPW-24 protects C. elegans from bacterial infection by stimulating the host immune response of the nematode. RPW-24 has antibacterial activity[1].
Coronatine is a plant growth regulator produced by Pseudomonas syringae. Coronatine simulates bioactive jasmonic acid (HY-122464A) conjugates or octadecanoid signal molecules of higher plants to make plants appear pathogenic symptoms. Coronatine promotes the virulence of Pseudomonas syringae in plants by activating the signal cascade that inhibits the accumulation of Salicylic acid (HY-B0167)[1][2][3][4].
Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells[1][2].
Sulfadiazine is a sulfonamide antibiotic.Target: AntibacterialSulfadiazine eliminates bacteria that cause infections by stopping the production of folate inside the bacterial cell, and is commonly used to treat urinary tract infections (UTIs). In combination, sulfadiazine and pyrimethamine, can be used to treat toxoplasmosis, a disease caused by Toxoplasma gondii. From Wikipedia.The ulcers who treated with silver sulfadiazine cream responded rapidly, with one-third showing bacterial levels of less than 10(5) within three days, and half within a week [1].
Ertapenem (MK-0826) is a broad spectrum and long acting β-lactam antibiotic. Ertapenem has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract[1][2].
Buclosamide is a topical antimycotic agent[1].
Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains[1].
Cap-dependent endonuclease-IN-23 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-23 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-23 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8A or 8B)[1].
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml[1].
MtbHU-IN-1 is an inhibitor of Mycobacterium tuberculosis nucleoid-associated protein HU (MtbHU), with a Kd of 98 nM for binding to WT MtbHU.
Licoflavanone (compopund 2) is a flavanone. Licoflavanone can be isolated from the MeOH extract of Air-dried leaves of G. glabra var. typica. Licoflavanone has antibacterial activity[1].
(±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.IC50 value: 2.4–2.9 μM(HIV-Luc infection of WT and Hdgfrp2 KO cells) [1]Target: integrase inhibitorin vitro: Approximately 2.4–2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160–200 nM, in Psip1 and double-KO cells [1].
Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
RPR103611, the betulinic acid derivative, is a potent HIV-1 entry inhibitor with IC50s of 80, 0.27, and 0.17 for CCR5-tropic virus YU2, CXCR4-tropic virus NL4-3 and dual tropic virus 89.6, respectively[1].
Perillic acid is the metabolite of Perillyl alcohol (HY-N7000). Perillic acid induces lung cancer cell cycle arrest and apoptosis. Perillic acid shows anti-HSV-1 and immunomodulatory activities[1][2][3].
ZINC04177596 is a potent HIV-negative factor (HIV-Nef) protein inhibitor. Nef is an accessory gene product of HIV and has an imperative role in viral replication and AIDS pathogenesis[1].
Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections[1][2].
Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2].
Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].
Rimantadine (Flumadine) is an anti-influenza virus drug.Target: Influenza Virusrimantadine are oral antiviral drugs useful in the prophylaxis and treatment of influenza A virus infections. rimantadine has prophylactic efficacy comparable to amantadine but lower potential for causing adverse effects [1]. double-blind study of children with influenza-like illness. 37 received rimantadine for five days. Of the total 37 children in the rimantadine group, 27% were found to have resistant isolated compared with 6% in the total group receiving acetaminophen (P < .04). Furthermore, the mean inhibitory concentration of rimantadine increased with time in the rimantadine group (r = .4, P = .002) [2].