Cyclo(Phe-Gly) is a cyclodipeptides with antimicrobial and anticancer activities, isolated from broth culture of endophytic Streptomyces YIM 64018 associated with Paraboea sinensis[1].
Tet-20 is a biological active peptide. (Tet-20, is a synthetic cathelicidin-derived peptide. It was tested as infection-resistant coating for medical devices. When tethered on an implant surface Tet-20 exhibited broad antimicrobial activities both in vivo and in vitro. It can stop biofilm formation and appears to be non-toxic to eukaryotic cells)
Effusanin A is a natural product that can be found in Isodon rugosus. Effusanin A exhibits DNA-damaging and antibacterial activities[1].
Nifursol is a nitrofuran antibiotic which inhibits the growth of Histomonas meleagridis but is not lethal to the flagellated protozoan. Target: AntibacterialNifursol can be analyzed and detected in tissues using intact 3,5-dinitrosalicylic acid hydrazide side chains along with electron-capture GC, spectrophotometric detection, and HPLC with ultraviolet light detection. In tissues, it has been observed that Nifursol is tightly bound to proteins and requires basic solutions such as ammonia to break the bonds between the two.
Ansuvimab (Ansuvimab-zyk) is a recombinant human monoclonal IgG1 antibody that exhibits antiviral activity against Zaire ebolavirus. Ansuvimab binds to the glycoprotein on Zaire ebolavirus to block its entry into host cells[1].
CRAMP-18 (mouse) is an antibiotic peptide without hemolytic activity. CRAMP-18 (mouse) has good inhibitory activity against Gram-negative bacteria, such as S. typhimurium and P. aeruginosa. CRAMP-18 (mouse) has the potential to study antifungal, antibacterial and antitumor[1][2].
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].
Galactofucan (Fucogalactan) is a sulfated polysaccharide. Galactofucan can be extracted from brown seaweed Saccharina longicruris with anticoagulant, anti-tumor, anti-thrombosis, anti-inflammatory and antiviral properties. Galactofucan shows antiviral activities to HSV-1 and HSV-2 with IC50s of 0.76 and 1.34 µg/mL, respectively. Galactofucan can be used for the research of cancer and inflammation[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].
N-Acetylneuraminic acid-13C-2 is the 13C labeled N-Acetylneuraminic acid.
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].
Aminoacyl tRNA synthetase-IN-1 is a bacterial aminoacyl tRNA synthetase (aaRS) inhibitor.
Fusafungine (Bioparox; Fusaloyos; Locabiotal) is a potent and orally active antibiotic and anti-inflammatory agent. Fusafungine has the potential for the research of upper respiratory airways disease (URAD)[1][2].
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].
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities[1]. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE[2]. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters[3].
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].
BPH-1086 (compound 10) is an IspH inhibitor, IspH domain fused with ribosomal protein S1 (RPS1) can bind to mRNA or form part of the bacterial ribosome[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].