Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[1][2].
Antiviral agent 10 is an anti-viral agent that can inhibit respiratory syncytial virus (RSV)[1].
Elemicin is a alkenylbenzene widely distributed in many herbs and spices. Elemicin inhibits Stearoyl-CoA Desaturase 1 (SCD1) by metabolic activation. Elemicin is one of the main components in aromatic food and has antimicrobial, antioxidant, and antiviral activities. Elemicin possesses genotoxicity and carcinogenicity[1].
Carnidazole is an antiprotozoal agent of the nitroimidazole class. Carnidazole is used for the research of Trichomonas infection[1].
Hexapeptide-11 is a bioactive peptide with anti-aging effect. Hexapeptide-11 protects fibroblasts against oxidative stress-mediated premature cellular senescence by mediating a downregulation of cellular proteins, such as ataxia telangiectasia mutated (ATM) and p53 [1].
Florfenicol amine hydrochloride is a metabolite of Florfenicol (HY-B1374). Florfenicol inhibits bacterial protein synthesis by binding to 50S and 70S subunits in the ribosome to abolish the activity of peptidyltransferase. Florfenicol, is a veterinary antibiotic, can be used in aquaculture to control susceptible bacterial diseases[1][2].
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells[1]. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM[2].
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research[1].
Efinaconazole(KP-103) is a novel triazole antifungal drug currently under development as a topical treatment for onychomycosis.IC50 value: 0.0039 ug/ml (MIC for T. mentagrophytes SM-110) [1]Target: antifungal agentin vitro: Efinaconazole was 4-fold more active than itraconazole against T. mentagrophytes SM-110 (MICs of 0.0039 and 0.016 μg/ml, respectively). Similarly, efinaconazole was 8-fold more active than clotrimazole against C. albicans ATCC 10231 (MICs of 0.00098 and 0.0078 μg/ml, respectively) [1]. In a comprehensive survey of 1,493 isolates, efinaconazole MICs against T. rubrum and T. mentagrophytes ranged from ≤ 0.002 to 0.06 μg/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 μg/ml, respectively. Efinaconazole MICs against 105 C. albicans isolates ranged from ≤ 0.0005 to >0.25 μg/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 μg/ml at 24 and 48 h, respectively [2].in vivo: The therapeutic efficacy of KP-103, a triazole derivative, for 10 guinea pigs with interdigital tinea pedis or tinea corporis was investigated. Topical KP-103 solution (0.25 to 1%) was dose-dependently effective in treating both dermatophytoses. A 1% KP-103-treatment rendered all infected skins culture-negative on day-2 posttreatment [3].
IR415 is a novel small molecule inhibitor of HBV virus replication that blocks hepatitis B virus X protein (HBx, Kd=2 nM) mediated RNAi suppression, reverses the inhibitory effect of HBx protein on activity of the Dicer endoribonuclease; exhibits a marked depletion of HBV core protein synthesis and down-regulation of pre-genomic HBV RNA in HBV-infected HepG2 cells, selectively targets HBx in a concentration-dependent manner.
Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
Sulfamethazine sodium (Sulfadimidine sodium) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections). In China and the European Commission, the maximum residue level for Sulfamethazine sodium in animal product is set at 100 µg/kg[1][2].
Antistaphylococcal agent 1 is an antistaphylococcal therapeutic agent.
Quinoxyfen (DE-795) is a powdery mildew fungicide[1].
Antibacterial agent 54 (example 20) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
4(3H)-Quinazolinone is a building block in chemical synthesis. Biologically active nitrogen heterocyclic compounds. Possesses a wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancerous and analgesic activities[1][2].
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities[1][2][3].
N-3-Oxo-tetradecanoyl-L-homoserine lactone (oxo-C14-HSL) is a rhizobacterial inducer and can improve basic defense against nematodes[1].
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].
HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8[1].
Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases[1][2][3].
Xanthopterin, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm[2]. Xanthopterin (XPT) causes renal growth and hypertrophy in rat[1].Xanthopterin inhibits RNA synthesis[4].
AT-9010 triethylamine, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 triethylamine can inhibit SARS-CoV-2 replication[1].
16,17-Dihydroheronamide C has antifungal activity and is designed as probe for the mode-of-action analysis of heronamide C[1].
Lomtegovimab (BI 767551) is a humanized anti-SARS-COV-2 spike glycoprotein monoclonal antibody. Lomtegovimab binds and neutralizes SARS-CoV-2. Lomtegovimab shows antiviral efficacy. Lomtegovimab has the potential for the research of COVID-19[1][2].
Buparvaquone is a hydroxynaphthoquinone antiprotozoal drug related to parvaquone and atovaquone.
Phosphoglycolohydroxamic acid is a potent aldolase and triose-phosphate isomerase inhibitor. Phosphoglycolohydroxamic acid can be used in the research of antibacterial and antifungal area[1][2].