Antibacterial agent 35, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Valganciclovir-d5 (TFA) is the deuterium labeled Valganciclovir TFA[1]. Valganciclovir, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir. Valganciclovir is an antiviral medication used to treat cytomegalovirus infections[2][3][4].
Multifungin (Bromochlorosalicylanilide) is an antifungal that treats oral candidiasis[1]. Multifungin prevents the formation and accumulation of Zearalenone and reduces the fungal population in stored-crushed corn[2].
Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection[1][2].
JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.
Protein kinase G inhibitor-1 (Compound 270) is a mycobacterial protein kinase G inhibitor, with an IC50 of 0.9 μM. Protein kinase G inhibitor-1 can be used for mycobacterial infection research[1].
Afabicin is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.
Propylparaben sodium is an antimicrobial agent, preservative, flavouring agent[1].
Meropenem is a carbapenem antibiotic, which displaying a broad spectrum of antibacterial activity.Target: AntibacterialMeropenem, a new parenteral carbapenem demonstrated increased activity as compared to imipenem against 336 strains of Neisseria gonorrhoeae, 119 strains of Haemophilus influenzae, and 110 strains of H. Ceftriaxone and ciprofloxacin demonstrated activity superior to that of both carbapenems while the activity of ceftazidime was similar to that of meropenem [1]. Meropenem, like imipenem and various experimental penems, may overcome the resistance problems presented by Class I beta-lactamases [2]. MEROPENEM was rapidly penetrated to the pleural effusion and was retained for a more prolonged time in the pleural effusion than in the blood of patients with accumulated pleural effusion, and it suggested the usefulness of MEROPENEM in antibacterial therapy for patients with pleurisy causing accumulation of pleural effusion [3].Clinical indications: Appendicitis; Bacterial infection; Bacterial meningitis; Bacterial pneumonia; Bacterial respiratory tract infection; Bacterial skin infection; Bacterial urinary tract infection; Bacteroides fragilis infection; Bacteroides infection; Bacteroides thetaiotaomicron infection; Complicated skin and skin structure infectionFDA Approved Date: July 1996Toxicity: In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Variotin is an Anti-Fungal Agent. Variotin has a strong antibiotic activity on dermatophytes such as Trichophyton, Microsporum, and Epidermophyton, and also pathogenic fungi in internal mycosis such as Blastomyces and Cryptococcus[1].
5-Nitrobarbituric acid is a herpes simplex virus type-1 (HSV-1) inhibitor (IC50=1.7 μM)[1].
Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.1 μM (VIM-1), 1.3 μM (NDM-1), and 5.0 μM (IMP-7), respectively[1].
Antifungal agent 15 has the most potent activity with EC50 values of 0.52 and 0.50 μg/mL against S. sclerotiorum and B. cinerea, respectively.
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 Mpro with an IC50 value of 72.07 nM. The main protease (Mpro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in drug discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19[1].
Cetalkonium chloride is an ammonium antiseptic agent used in many topical drugs for infections of mouth, throat and eye. Cetalkonium chloride acts as anti-inflammatory amphiphilic agent[1].
Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.
Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
FtsZ-IN-2 (Compound 19) is an inhibitor of the bacterial cell division protein FtsZ with GTPase inhibitory activity. FtsZ-IN-2 exhibits anti-staphylococcal activity with MIC values of 2 µg/ml for MSSA and MRSA[1].
Cefiderocol is a novel siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less.
Xanthyletin is a coumarin isolated from Citrus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants[1].
Fidaxomicin(OPT-80; PAR-101) is a new class of narrow spectrum macrocyclic antibiotic drug; selective eradication of pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora.
Acetyl-CoA Carboxylase-IN-1 is a potent acetyl-CoA carboxylase (ACC) inhibitor with an IC50 value of ＜5 nM. Acetyl-CoA Carboxylase-IN-1 has antibacterial activity[1].
SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research[1].
Crexavibart (BMS-986413; C-144-LS) is an IgG1λ2 antibody that targets the SARS-CoV2 spike (S) glycoprotein receptor-binding domain[1].
Cefixime trihydrate (FR-17027 trihydrate) is an antibiotic and a third generation cephalosporin antibiotic, useful for the treatment of a number of bacterial infections[1][2].
Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Dehydropipernonaline (Compound 24) is an amide compound. Dehydropipernonaline shows considerable cytotoxicity to L5178Y mouse lymphoma cells (IC508.9μM). Dehydropipernonaline can be used for screening antifungal and cytotoxicity [1].
DSM265 is a PfDHODH inhibitor with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of P. falciparum 3D7 parasites with an EC50 of 4.3 nM.
Ganciclovir (INN) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. Ganciclovir is a synthetic analogue of 2′-deoxy-guanosine. It is first phosphorylated to ganciclovir monophosphate by a viral kinase encoded by the cytomegalovirus (CMV) gene UL97 during infection. Subsequently, cellular kinases catalyze the formation of ganciclovir diphosphate and ganciclovir triphosphate, which is present in 10-fold greater concentrations in CMV or herpes simplex virus (HSV)-infected cells than uninfected cells. A prodrug form with improved oral bioavailability (valganciclovir) has also been developed.