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].
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.
ACSS2-IN-1 is a potent ACSS2 inhibitor for the treatment of cancer.ACSS2-IN-1 (Cpmpound 1) is a potent ACSS2 inhibitor. ACSS2-IN-1 inhibits ACSS2 with the IC50 of 0.01 nM to <1 nM. ACSS2-IN-1 can be used for the research of cancer[1].
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].
Aegeline, a main alkaloid, mimics the yeast SNARE protein Sec22p in suppressing α-synuclein and Bax toxicity in yeast. Aegeline restores growth of yeast cells suppressed by either αsyn or Bax. Antioxidant activity[1].
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].
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.
S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively[1].
Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[1][2][3].
PPm, a derivative of penthiopyrad and hapten, is a representative member of the succinate dehydrogenase inhibitors group of fungicides[1].
Pseudouridimycin (PUM), an antibiotic, is a selective bacterial RNA polymerase (RNAP) inhibitor. Pseudouridimycin is a C-nucleoside analogue that is effective against both Gram-negative and Gram-positive bacteria[1].
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].
Cosalane (NSC 658586) is a potent inhibitor of HIV replication. Cosalane has an intrinsic ability to block human and murine CCR7 function in vitro in response to both of its natural ligands, CCL19 and CCL21, with the IC50 of 0.207/2.66 μM in human for CCL19/CCL21 and 0.193/1.98 μM in murine, respectively[1][2].
Antistaphylococcal agent 1 is an antistaphylococcal therapeutic agent.
BO3482 has Antimicrobial activity and can inhibit the growth of methicillin-resistant Staphylococci (MRS) with an MIC90 of 6.25 mg/mL.
Fmoc-Glu-OMe a glutamic acid derivative, shows antibacterial activity and gelation property in AgNO3 solution. Fmoc-Glu-OMe is a mouldable wound healing biomaterial[1].
Doripenem monohydrate is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.Target: AntibacterialDoripenem is an ultra-broad-spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It was launched by Shionogi Co. of Japan under the brand name Finibax in 2005 and is being marketed outside Japan by Johnson & Johnson. It is particularly active against Pseudomonas aeruginosa. It is recommended that those allergic to doripenem or to any type of beta-lactam antibiotics such as cephalosporin or other Carbapenems not receive doripenem.Doripenem appears as crystalline powder anywhere from a white to somewhat yellowish colour.Doripenem is moderately soluble in water, slightly soluble in methanol, and virtually insoluble in ethanol. Doripenem is also solution in N,N-dimethylformamide. Doripenem's chemical configuration has 6 asymmetrical carbon atoms (6 stereocentres) and is most commonly supplied as one pure isomer. In terms of doripenem for injection, the crystallized powered drug can form a monohydrate when mixed with water. However, Doripenem has not been proven to possess polymorphism.
Quinoxyfen (DE-795) is a powdery mildew fungicide[1].
HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
Vidarabine monohydrate is an adenine arabinoside. Vidarabine monohydrate an antiviral drug which is active against herpes simplex viruses (HSV) and varicella zoster viruses[1].
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%)[1].
Metallo-beta-lactamase ligand 1 is a class B β-lactamase inhibitor with antibacterial activity extracted from patent WO2019221122A1, compound A[1].
Quellenin is an anti-saprolegnia compound. Quellenin can be isolated from deep-sea fungus Aspergillus sp. YK-76[1]
Pazufloxacin (T-3761) mesylate 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].