DNA Gyrase-IN-7 (compound 6d) is a novel Microbial DNA-Gyrase inhibitor[1].
Callophycin A, red seaweed derived metabolite, is potently against C. albicans. Callophycin A exhibits potent activity against drug resistance vaginal candidiasis[1].
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
N7-Methyl-guanosine-5'-triphosphate-5'-adenosine (m7GpppA) is a dinucleotide cap analog that can be used for in vitro RNA transcription[1].
Aricine ((-)-Aricine), an indole alkaloid, displays larvicidal activity[1].
HBV-IN-9 is a potent HBsAg (HBV Surface antigen) inhibitor (IC50=10 nM) and HBV DNA production inhibitor (IC50=0.15 nM in HepG2.2.15 cells)[1]. From patent WO2018001952A1, example 20.
3-Oxo-hop-22(29)-ene is a yeast α-glucosidase inhibitor. 3-Oxo-hop-22(29)-ene shows a moderate effect on the viability of T. cruzi and L. mexicana. 3-Oxo-hop-22(29)-ene shows marginal activity of anti-inflammatory[1].
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod[1][2].
Clindamycin phosphate is an antibiotic, which blocks the ribosomes of microorganisms. It is usually used to treat infections with anaerobic bacteria, can also be used to treat protozoal diseases, such as malaria.
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.
3-Acetonyl-3-hydroxyoxindole (AHO) is a potent systemic acquired resistance (SAR) inducer in plants. 3-Acetonyl-3-hydroxyoxindole induces resistance in tobacco plants against infection with tobacco mosaic virus (TMV) and the fungal pathogen Erysiphe cichoracearum. 3-Acetonyl-3-hydroxyoxindole increases the level of pathogenesis-related gene 1 (PR-1) expression, salicylic acid (SA) accumulation and phenylalanine ammonia-lyase activity[1].
Allyl methyl sulfide is a bioactive organosulfur compound found in garlic. Allyl methyl sulfide exhibits antibacterial, antioxidant and anticancer properties[1].
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter[1][2][3].
Myricetin 3-O-glucoside (Myricetin 3-β-D-glucopyranoside) is a flavonol from Tibouchina paratropica. Myricetin 3-O-glucoside exhibits anti-Leishmanial, anti-inflammatory and antimicrobial activities[1].
Fenpropimorph is a fungicide that inhibits the sterol pathway. Fenpropimorph inhibits δ8-δ7-sterol isomerase in yeast at low concentrations, with δ14-sterol reductase being blocked at higher levels, preventing the biosynthesis of ergosterol. Fenpropimorph also inhibits sterol synthesis in certain plants and mammalian cells[1][2][3].
Lateritin is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), isolated from the mycelial cake of Gibberella lateritium IFO 7188[1]. Lateritin also inhibits the growth of a mini-panel of human cancer cell lines, gram-positive bacteria, and Candida albicans[2].
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively[1][2][3].
Finafloxacin is a fluoroquinolone antimicrobial agent that exhibits optimum efficacy in slightly acidic environments. Target: AntibacterialFinafloxacin is a pH-activated fluoroquinolone (belonging to a new 8-cyano subclass) to treat serious bacterial infections associated with an acidic environment, including urinary tract infections (UTIs) and Helicobacter pylori infections. Finafloxacin exhibits optimal efficacy in slightly acidic environments (pH 5.0-6.0), under which other fluoroquinolones lose activity. Finafloxacin is highly selective for bacterial type II topoisomerases, including DNA gyrase and DNA topoisomerase IV. [1]
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].
Sulfachloropyridazine (sodium) is a sulfonamide antibiotic that inhibits bacterial growth[1].
(Rac)-Lonafarnib (Sch66336 racemate) is the racemate of Lonafarnib. Lonafarnib is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities[1].
Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3].
Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane[1].
Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.
Influenza A virus-IN-4 (compound 23b), an Oseltamivir derivative, is a potent inhibitor of neuraminidase. Influenza A virus-IN-4 exerts powerful inhibitions on influenza viruses[1].
Cerebroside C, a sphingolipid, is a fungal metabolite. Cerebroside C licits defense responses in rice[1].
Ganciclovir mono-O-acetate is a derivative of Ganciclovir. Ganciclovir, a nucleoside analogue, is an orally active antiviral agent with activity against CMV[1].
Pleconaril-d4 is deuterium labeled Pleconaril.
Abacavir sulfate (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. Target: NRTIAbacavir is a nucleoside reverse transcriptase inhibitor marketed since 1999 for the treatment of infection with the human immunodeficiency virus type 1 (HIV). Despite its clinical efficacy, abacavir administration has been associated with serious and sometimes fatal toxic events. Abacavir has been reported to undergo bioactivation in vitro, yielding reactive species that bind covalently to human serum albumin, but the haptenation mechanism and its significance to the toxic events induced by this anti-HIV drug have yet to be elucidated. The mechanism underlying abacavir hypersensitivity syndrome is related to the change in the HLA-B*5701 protein product. Abacavir binds with high specificity to the HLA-B*5701 protein, changing the shape and chemistry of the antigen-binding cleft. This results in a change in immunological tolerance and the subsequent activation of abacavir-specific cytotoxic T cells, which produce a systemic reaction known as abacavir hypersensitivity syndrome.