DMT-dC(ac) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
Baquiloprim-d6 is deuterium labeled Baquiloprim. Baquiloprim, an antibiotic, is a selective inhibitor of bacterial dihydrofolate reductases. Baquiloprim possesses in vitro bacteriostatic activity against both Gram-negative and Gram-positive bacteria[1][2].
SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19[1].
Chamaejasmenin C, a biflavanone, shows nematicidal activity against second-stage juveniles (J2s) of B. xylophilus and B. mucronatus[1][2].
Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively[1].
Cephaloridine is a broad-spectrum antibacterial antibiotic. Cephaloridine has certain dose-related nephrotoxicity[1][2].
Antifungal agent 33 (compound 4e) is a potent antifungal agent. Antifungal agent 33 exhibits remarkable antifungal activity against C. albicans, with a MIC of 16 μg/mL. Antifungal agent 33 shows potent inhibitory activity against Lanosterol 14α-demethylase (CYP51), with an IC50 of 0.19 μg/mL[1].
GW433908 is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.IC50 Value:Target: HIV Proteasein vitro: There were no significant changes in buprenorphine or PI plasma levels and no significant changes in medication adverse effects or opioid withdrawal. Increased concentrations of the inactive metabolite buprenorphine-3-glucuronide suggested that darunavir-ritonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine[1].in vivo: Fosamprenavir-ritonavir administered with methadone did not alter plasma amprenavir pharmacokinetics compared with historical control data; nor did it alter the unbound R-methadone at 2 and 6 hours after methadone dosing. Pharmacodynamic indexes remained essentially unchanged after adding fosamprenavir-ritonavir to methadone [2]. After a high-fat meal compared with fasting, (1) the bioavailability of GW433908G suspension was decreased by 20% and Cmax by 41%, and (2) for GW433908G tablets, there was no influence on AUC(12% lower Cmax). After a low-fat meal compared with fasting, (1) there was bioequivalence for GW433908G tablets, but (2) bioavailability was decreased by 23% for amprenavir capsules (Cmax was also lower, by 46%) [3].Clinical trial: Study of an Investigational Regimen Including FDA Approved HIV Drugs In HIV-Infected Pediatric Subjects. Phase 2
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research[1][2].
Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA[1].
Cuspidiol (compound 3) is a CH2Cl2 extract of Fagara zanthoxyloides Lam. Cuspidiol has antifungal and antioxidative activity[1].
Mtb-cyt-bd oxidase-IN-2 is an inhibitor of Mycobacterium tuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) with an IC50 value of 0.67 μM. Mtb-cyt-bd oxidase-IN-2 inhibits the growth of Mycobacterium tuberculosis with a MIC value of 256 μM. Mtb-cyt-bd oxidase-IN-2 can be used for the research of infection[1].
Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody drug conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation[1].
Aminoacyl tRNA synthetase-IN-1 is a bacterial aminoacyl tRNA synthetase (aaRS) inhibitor.
Antitubercular agent-21 (Compound 15) is an antitubercular agent with an MIC of o.4 µg/mL against M. tuberculosis H37Rv. Antitubercular agent-21 exhibits lower activity against other microorganism such as bacteria gram-positive, gram-negative or fungi. Antitubercular agent-21 shows low cytotoxicity[1].
Antifungal agent 69 (compound 13) is a eugenol-imidazole against Candida albicans (MIC: 4.6 μM) with no relevant cytotoxicity. Antifungal agent 69 alters the fungal ergosterol biosynthesis and shows antifungal activity[1].
Trypanothione synthetase-IN-3 is a noncompetitive mixed hyperbolic Trypanothione synthetase (TryS) inhibitor (Ki: 0.8 μM). Trypanothione synthetase-IN-3 can be used in the study of parasites, such as L. infantum[1].
Phenothiazine is an antibiotic which has insecticidal, fungicidal, antibacterial and anthelmintic activities. Phenothiazine also can be used for the research of neurological diseases[1][2].
Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.IC50 Value: Target: HCV
A potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 89 nM; shows anti-RSV activity with IC50 of 57.6 nM and 47.8 nM for RSV A2 and RSV B-EST, respectively; shows weak cytotoxicity (CC50=600 nM).
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria[1][2].
Arterolane is an antimalarial agent, with IC50 of both 1.1 nM against P. falciparum Ro73 and W2, respectively.
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS[1].
Miconazole-d2 is the deuterium labeled Miconazole[1]. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects[2][3].
Surfactin is a potent cyclic lipopeptide biosurfactants that mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes. Surfactin can act as an antimicrobial adjuvant with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects[1][2]. Surfactin also has antiviral activity against a variety of enveloped viruses[3].
Bronopol is an antimicrobial, with low mammalian toxicity (at in-use levels) and high activity against bacteria (especially the troublesome Gram-negative species).
1,4, 6-trihydroxy-5-methoxy-7-prenylxanthone is an antimicrobial agent that can be isolated from the genus garcinia. 1,4, 6-trihydroxy-5-methoxy-7-prenylxanthone inhibits S. aureus and B. cereus with MIC values of 128 μg/mL and 200 μg/mL, respectively[1].
Destomycin B (A-16316-C) is an antibiotic, and is active against fungi. Destomycin B also has anthelmintic activity[1].
Ceftriaxone is an antibiotic useful for the treatment of a number of bacterial infections.Target: AntibacterialCeftriaxone inhibits bacterial cell wall synthesis by means of binding to the penicillin-binding proteins (PBPs). Inhibition of PBPs would in turn inhibit the transpeptidation step in peptidoglycan synthesis which is required for bacterial cell walls. Like other cephalosporins, ceftriaxone is bacteriocidal and exhibits time-dependent killing. Ceftriaxone, one of the beta-lactam antibiotics, is a stimulator of EAAT2 expression with neuroprotective effects in both in vitro and in vivo models based in part on its ability to inhibit neuronal cell death by glutamate excitotoxicity. Based on this consideration and its lack of toxicity, ceftriaxone has potential to manipulate glutamate transmission and ameliorate neurotoxicity [1].