Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.
Butoconazole nitrate is an anti-fungal agent.Target: Antifungalbutoconazole 1-BSR is an effective and safe alternative to longer-term therapy with miconazole nitrate (seven days) for vulvovaginal candidiasis [1]. A sustained-release (SR) bioadhesive vaginal cream (2% butoconazole nitrate) has incorporated VagiSite technology, a topical drug delivery system that allows SR of the drug [2].
Monobehenin has a strong inhibitory activity toward bacterial biofilm formation.
Sulfamethomidine is an antibacterial agent[1].
Silver sulfadiazine (AgSD), a sulfonamide antibiotic, effects a dual inhibitory action on bacterial growth by its sulfa moiety (SD-SDZ) that prevents bacterial folate absorption and subsequent DNA synthesis. The silver that is released from Silver sulfadiazine binds and disrupts the DNA structure, precluding bacterial DNA replication[1].
Fmoc-Pro-OH-1-13C is a 13C-labeled Sulfabenzamide. Sulfabenzamide (N-Sulfanilylbenzamide) is an antimicrobial agent and usually consumed in combination with Sulfathiazole and Sulfacetamide. Sulfabenzamide is effective against Gram-positive and negative ba
Fosfomycin sodium (MK-0955 sodium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[1].
SPR720 (pVXc-486) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). SPR720 has potent bactericidal activities in vivo[1].
3,5-Di-tert-butylphenol is an volatile organic compound with anti-biofilm and antifungal activities. 3,5-Di-tert-butylphenol induces accumulation of reactive oxygen species (ROS).
Valacyclovir-d4 hydrochloride is the deuterium labeled Valacyclovir hydrochloride. Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir hydrochloride inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir hydrochloride is a prodrug of Aciclovir (HY-17422)[1][2][3][4][5].
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent[1][2].
HBV Seq2 aa:28-39 is a HBsAg peptide, which binds to major histocompatibility complex (MHC) class I molecules[1][2].
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].
Lansoprazole D4 (AG-1749 D4) is a deuterium labeled Lansoprazole. Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid[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.
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.
Allyl methyl sulfide is a bioactive organosulfur compound found in garlic. Allyl methyl sulfide exhibits antibacterial, antioxidant and anticancer properties[1].
Trofosfamide-d4 is the deuterium labeled Trofosfamide. Trofosfamide is an orally bioavailable oxazaphosphorine derivative with antineoplastic activity[1][2].
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].
Junceellolide C is a transcription inhibitor of cccDNA. Junceellolide C inhibits HBV DNA replication and significantly decreases the level of supernatant HBV RNA with EC50 values of 5.19, 3.52 μM respectively in HepAD38 cells. Junceellolide C is a potent anti-HBV agent[1].
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].
N-octanoyl-L-Homoserine lactone is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism. N-octanoyl-L-Homoserine lactone can be used for the infection prevention and regulation of virulence in general and in cystic fibro.
Sulfachloropyridazine (sodium) is a sulfonamide antibiotic that inhibits bacterial growth[1].
Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].