7-Acetoxybonducellpin C, a diterpenoid, is a nature product that could be isolated from the seed kernels of Caesalpinia crista. 7-Acetoxybonducellpin C has antimalarial activity[1].
Carnidazole is an antiprotozoal agent of the nitroimidazole class. Carnidazole is used for the research of Trichomonas infection[1].
Sulfadiazine sodium belongs to the class of sulfonamide antibiotics that are used for veterinary purposes worldwide, mainly in pig production. Sulfadiazine sodium is also used for toxoplasmosis[1][2].
Robinetin (3,3',4',5',7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation[1][2][3][4][5].
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].
(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
(-)-Corypalmine (Discretinine), an alkaloid that could be isolated from the stem of Guatteriopsis friesiana, possesses antimicrobial activity[1].
BiCAPPA is the first bivalent antiprion ligand. BiCAPPA can decrease infectious conformational form of prion protein (PrPSc) from scrapie-infected cells, with an EC50 of 0.32 μM[1][2].
Glurate (4-Acetylbutyric acid; 5-Oxohexanoic acid) can be used to construct antiviral agents (acyclic nucleoside esters) (extracted from patent WO1997030052A1)[1].
Antifungal agent 30 (compound A18) is a potent antifungal agent. Antifungal agent 30 shows excellent antifungal activity against Candida albicans (CPCC400616) and Aspergillus fumigatus, with MIC of 0.03 and 0.5 μg/mL, respectively. Antifungal agent 30 also shows excellent antifungal activity against fluconazole-resistant strains. The potent antifungal activity of Antifungal agent 30 mainly causes by hydrogen and coordination bond interaction with the CYP51[1].
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].
Stilbamidine dihydrochloride is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.
1-Acetyl-β-carboline is metabolite of streptomyces kasugaensis[1].
2-Amino-2'-deoxyadenosine is a deoxyribonucleoside used for the oligonucleotide synthesis.
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].
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[1].
DENV-IN-7, a flavone analog, is a dengue virus (DENV) inhibitor with an EC50 value of 70 nM. DENV-IN-7 has low toxicity against normal cell and anti-dengue activity[1].
Cochliodone A is an active compound extracted from cultures of the deep-sea derived fungus Chaetomium sp. and has antibacterial and anticancer activity. Cochliodone A is toxic to a variety of bacteria, with MICs of 15.3 μg/mL (V. vulnificus), 32.7 μg/mL (V. rotiferianus), 15.9 μg/mL (S. aureus ATCC 43300), and 16.3 μg/mL (S . aureus CGMCC 1.12409). Cochliodone A also inhibits a variety of cancer cell lines, with IC50s of 28.1 μM (A549), 20.7 μM (HeLa), and 23.2 μM (Hep G2)[1].
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.
HAA-09 is an orally active and potent anti-influenza agent, targeting the influenza PB2_cap binding domain. HAA-09 displays potent anti-influenza A virus activity, with an EC50 of 0.03 μM. HAA-09 shows polymerase inhibition, with an IC50 of 0.06±0.004 μM. HAA-09 blocks virus replication without causing obvious cytotoxicity[1].
3,4-Dichlorocatechol is a substrate of the broad-spectrum chlorocatechol 1,2-dioxygenase of pseudomonas chlororaphis RW71[1].
Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Tobramycin sulfate (Nebramycin Factor 6 sulfate) is a parenterally administered, broad spectrum aminoglycoside antibiotic that is widely used in the treatment of moderate to severe bacterial infections due to sensitive organisms[1].
Acetylazide is a synthetic broad-spectrum bacteriostatic antibiotic.
Saccharothrixin K, a glycosylated saccharothrixin, shows moderate inhibition against Helicobacter pylori G27, H. pylori 159, and Staphylococcus aureus ATCC25923 with MIC values of 16 μg/mL[1].
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
Pazufloxacin (T-3761) is a fluoroquinolone antibiotic.Target: AntibacterialPazufloxacin (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus [1]. T-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria. The MICs of T-3761 against 90% of the methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp. tested were 0.39 to 6.25 micrograms/ml. The MBCs of T-3761 were either equal to or twofold greater than the MICs. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively [2].