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].
(E)-Coniferin is the isomer of Coniferin. Coniferin is a glucoside of coniferyl alcohol. Coniferin inhibits fungal growth and melanization[1].
Carbendazim is a broad-spectrum benzimidazole fungicide which can be used to control a broad range of diseases on arable crops, fruits, vegetables, ornamentals and medicinal herbs.
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV[1][2][3].
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes[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.
Antibacterial agent 35, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Methyl anthranilate, a plant spice extract, is a quorum sensing inhibitor and anti-biofilm agent against Aeromonas sobria. Methyl anthranilate has been widely employed for the preparation of edible flavor and food additives in food processing industries[1].
Mafenide is a sulfonamide-type medication.Target: AntibacterialMafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
(+)-Carbovir triphosphate is an enantiomer of Carbovir triphosphate (HY-131607). (+)-Carbovir triphosphate is an inhibitor and substrate of HIV reverse transcriptase[1].
Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Diethyl butylmalonate-d9 is the deuterium labeled Diethyl butylmalonate[1]. Diethyl butylmalonate exhibits toxicity to T. pyriformis, with a log(IGC50-1) of 0.557[2].
Nitrofural is a bactericidal compound used as an antibiotic most commonly in the form of ointments.Target: AntibacterialNitrofurazone, a nitroaromatic drug, is a broad spectrum antibiotic which has until now been considered as activated in bacteria by nitroreductases. Its use in medicine has become less frequent as safer and more effective products have become available, and it has been discontinued in the US.Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. In vitro cruzain inhibition tests were performed for both compounds, and the 50% inhibitory concentration (IC50) for NF and NFOH presented values of 22.83 ± 1.2 μM and 10.55 ± 0.81 μM, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.
(R)-Eucomol, a flavonoid derivative, displays marginal antibacterial activity. (R)-Eucomol shows cytotoxic activity against KB and P-388 cells[1].
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].
Omiganan is a cationic antimicrobial peptide. Omiganan as an analogue of indolicidin shows activity against gram-positive and gram-negative bacteria but also Candida spp. isolates. Omiganan can be used for the research of alcohol nose and acne[1][2].
GS-6207 is a HIV-1 capsid inhibitor. GS-6207 shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. GS-6207 displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs)[1].
Helvolic acid (Fumigacin) is an antibiotic isolated from Xylaria sp, active against the Gram-positive bacteria[1].
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
Antimycobacterial agent-4 is a 2-amino-4-(2-pyridyl) thiazole derivative, with antimycobacterial activity, antiplasmodial activity, and cytotoxicity on a mammalian cell line[1][2].
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].
Benzoic Acid is an aromatic alcohol existing naturally in many plants and is a common additive to food, drinks, cosmetics and other products. It acts as preservatives through inhibiting both bacteria and fungi.
Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 15 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 2.3 and 7.8 μM, respectively. Anti-inflammatory agent 15 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 15 can be used for tuberculosis (TB) research[1].
Clindamycin-13C,d3 is the 13C- and deuterium labeled. Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Sulfanitran is a sulfonamide antiinfective drug.
Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant[1].
3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 µM, an Ki value of 0.58 µM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies[1].