AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
Morinidazole R enantiomer is the R-enantiomer of Morinidazole. Morinidazole is a new 5-nitroimidazole class antimicrobial agent. Morinidazole R enantiomer is the less active enantiomer.
Erythromycin lactobionate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin lactobionate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin lactobionate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Delavirdine(U 90152) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI).IC50 Value: 0.26 uM (Recombinant HIV-1 RT) [1]Target: HIV-1 reverse transcriptase; NNRTIin vitro: U-90152 [1-(5-methanesulfonamido-1H-indol-2-yl-carbonyl)-4-[3-(1-methyl eth yl-amino)pyridinyl]piperazine], which inhibited recombinant HIV-1 RT at a 50% inhibitory concentration (IC50) of 0.26 microM (compared with IC50s of > 440 microM for DNA polymerases alpha and delta). U-90152 blocked the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates, including variants that were highly resistant to 3'-azido-2',3'-dideoxythymidine (AZT) or 2',3'-dideoxyinosine, with a mean 50% effective dose of 0.066 +/- 0.137 microM. U-90152 had low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 microM. In experiments assessing inhibition of the spread of HIV-1IIIB in cell cultures, U-90152 was much more effective than AZT. When approximately 500 HIV-1IIIB-infected MT-4 cells were mixed 1:1,000 with uninfected cells, 3 microM AZT delayed the evidence of rapid viral growth for 7 days. In contrast, 3 microM U-90152 totally prevented the spread of HIV-1, and death and/or dilution of the original inoculum of infected cells prevented renewed viral growth after U-90152 was removed at day 24 [1]. Asdelavirdine concentration was increased from 0 to 100 microM, the K(M) for diclofenac metabolism rose from 4.5+/-0.5 to 21+/-6 microM, and V(max) declined from 4.2+/-0.1 to 0.54+/-0.08 nmol/min/mg of protein, characteristic of mixed-type inhibition [2].in vivo: The mean values (+/- standard deviations) for the maximum concentration in serum (C(max)) of ritonavir, the area under the concentration-time curve from 0 to 12 h (AUC(0-12)), and the minimum concentration in serum (C(min)) of ritonavir before the addition of delavirdine were 14.8 +/- 6.7 micro M, 94 +/- 36 micro M. h, and 3.6 +/- 2.1 micro M, respectively. These same parameters were increased to 24.6 +/- 13.9 micro M, 154 +/- 83 micro M. h, and 6.52 +/- 4.85 micro M, respectively, after the addition of delavirdine(P is <0.05 for all comparisons). Delavirdine pharmacokinetic parameters in the presence of ritonavir included a C(max) of 23 +/- 16 micro M, an AUC(0-8) of 114 +/- 75 micro M. h, and a C(min) of 9.1 +/- 7.5 micro M [3].Toxicity: Clinical trial: Quality of Life of HIV-infected Participants Switched to Raltegravir Versus Other Antiretroviral Regimens. Phase 4
Furaltadone-d8 (Altafur-d8) is the deuterium labeled Furaltadone. Furaltadone, a nitrofuran drug, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci [1][2].
Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL[1]. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM[2].
SARS-CoV-2-IN-21 (compound 10), a penicillin sulfone benzyl C6 derivative, is a potent SARS-CoV-2 main protease inhibitor, with an IC50 of 5.3 μM. SARS-CoV-2-IN-21 can be used for COVID-19 research[1].
Carbovir triphosphate (CBV-TP) is a phosphorylated metabolite. Carbovir triphosphate can be used for the research of human immunodeficiency virus (HIV)[1].
Arjunglucoside I, a natural compound, possesses antimicrobial activity with a MIC of 1.9 μg/mL[1].
(Z)-Mutagenic Impurity of Tenofovir Disoproxil 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.
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM[1].
6'-Sialyllactose (sodium), a predominant milk oligosaccharide, reduces the internalisation of Pseudomonas aeruginosa in human pneumocytes[1].
Cap-dependent endonuclease-IN-16 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-16 is a pyridone polycyclic derivative. Cap-dependent endonuclease-IN-16 has the potential for the research of influenza (extracted from patent CN112778330A, compound 15A)[1].
Tiamulin-d10 (Thiamutilin-d10) hydrochloride is the deuterium labeled Tiamulin. Tiamulin (Thiamutilin) is a diterpenic compound that widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia[1][2][3].
AN7973 is an benzoxaborole compound, AN7973 blocks intracellular parasite development and inhibits the two Cryptosporidium species (C.parvum and C.hominis) as an Cryptosporidium growth inhibitor[1].
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
Berkeleyacetal C, a meroterpenoid compound, shows favorable activity of inhibiting nitrogen oxide (NO) production of macrophages stimulated by lipopolysaccharide (LPS). Berkeleyacetal C exerts anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways[1].
6-Amino-5-azacytidine inhibits the growth of bacteria E. coli[1].
Nonanoic acid-d2 is the deuterium labeled Nonanoic acid[1]. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[2].
Antibiotic tan-592B is an antibiotic agent.
Filipin, produced as a mixture of related compounds known as the filipin complex (filipins I-IV) in nature[1], is a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure. Filipin III is the major component of Filipin[2].
Corianin is a sesquiterpene lactone that can be isolated from the fruits of Coriaria ruscifolia. Corianin shows antibacterial activity against S. aureus and S. epidermis[1].
MMV008138 is a species-selective antimalarial agent which targets the enzyme 2- C-methyl-d-erythritol 4-phosphate cytidylyltransferase (IspD) in the MEP pathway, with an IC50 of 250 nM for P. falciparum Dd2 strain[1][2].
(Rac)-Fosfomycin (benzylamine)-13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
Ga(III)protoporphyrin-IX is a model for the key interporphyrin interactions in malaria pigment. Ga(III)protoporphyrin-IX acts as a potent antibacterial against gram-negative, gram-positive, and acid-fast bacteria. Ga(III)protoporphyrin-IX is readily soluble in methanol (MeOH). Ga(III)protoporphyrin IX are as malarial pigment analogues for drug development and as potential antibacterial agents[1].
Oxacillin sodium monohydrate is an antibiotic similar to flucloxacillin used in resistant staphylococci infections.Target: AntibacterialOxacillin is a penicillinase-resistant β-lactam. It is similar to methicillin, and has replaced methicillin in clinical use. Another related compound is nafcillin. Since it is resistant to penicillinase enzymes, such as that produced by Staphylococcus aureus, it is widely used clinically in the US to treat penicillin-resistant Staphylococcus aureus. However, with the introduction and widespread use of both oxacillin and methicillin, antibiotic-resistant strains called oxacillin-resistant Staphylococcus aureus (MRSA/ORSA) have become increasingly prevalent worldwide. MRSA/ORSA is treated using vancomycin. From Wikipedia.
Besifovir (LB80331), a parent drug converted by LB80380, further metabolizes to its active form, LB80317. LB80380 is potent antiviral agent against hepatitis B virus (HBV) [1][2].
Tetraconazole, a chiral triazole fungicide, is widely used for the prevention of plant disease in wheat fields[1]. Tetraconazole alters the methionine and ergosterol biosynthesis pathways in Saccharomyces yeasts promoting changes on volatile derived compounds[2].
SARS-CoV-2-IN-43 (Compound 8h) is a potentSARS-CoV-2replication inhibitor with antiviral activity[1].