(-)-Ketoconazole is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Cidofovir is an anti-CMV drug which can suppress CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription.IC50 Value:Target: CMV DNA polymerasein vitro: The minimum concentrations of (S)-HPMPC required to inhibit CMV plaque formation by 50% was microgram/ml. The selectivity indices of (S)-HPMPC, as determined by the ratio of the 50% inhibitory concentration for cell growth to the 50% inhibitory concentration for plaque formation for CMV (AD-169 strain), was 1,500 [1]. The time course of uptake of HPMPC into Vero cells was linear between 10 and 75 min and proportional to the concentration in the medium from 10(-6) to 10(-2) M. HPMPC uptake was temperature sensitive and the rate of uptake was considerably lower at 27 degrees than at 37 degrees and almost totally inhibited at 4 degrees [2]. in vivo: Levels of cidofovirin serum following intravenous infusion were dose proportional over the dose range of 1.0 to 10.0 mg/kg of body weight and declined biexponentially with an overall mean +/- standard deviation terminal half-life of 2.6 +/- 1.2 h (n = 25). Approximately 90% of the intravenous dose was recovered unchanged in the urine in 24 h. The overall mean +/- standard deviation total clearance of the drug from serum (148 +/- 25 ml/h/kg; n = 25) approximated renal clearance (129 +/- 42 ml/h/kg; n = 25), which was significantly higher (P < 0.001) than the baseline creatinine clearance in the same patients (83 +/- 21 ml/h/kg; n = 12) [3]. Positive CMV urine cultures reverted to negative in 2 of 8 patients receiving doses of < or = 1.5 mg/kg twice weekly and 11 of 13 patients receiving higher doses. Cidofovir has in vivo anti-CMV activity demonstrated by prolonged clearing of CMV viruria, although this observation is tempered by the fact that clearance of viremia could not be demonstrated [4].Toxicity: Patients receiving 0.5 or 1.5 mg/kg twice weekly experienced no serious toxicity. The first two patients who received 5 mg/kg twice weekly developed glycosuria and 2+ proteinuria. Subsequent patients received concomitant probenecid to attempt to ameliorate renal toxicity [4].Clinical trial: FDA approved drug
Y18501 is a oxysterol-binding protein (OSBPI) inhibitor with a similar structure to Oxathiapiprolin. Y18501 shows strong inhibitory activities against Phytophthora spp. and Pseudoperonospora cubensis, with EC50 ranging from 0.0005 to 0.0046 μg/mL. Y18501 shows excellent protective and curative activities against P. cubensis. Y18501 in combination with Chlorothalonil (HY-N6625) can significantly promote the inhibition of P. cubensis[1].
Antitrypanosomal agent 2 is a potent and selective trypanosoma brucei inhibitor[1].
Fluconazole (hydrate) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole (hydrate) is the hydrate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.
Nequinate, a quinoline compound, is an anticoccidial agent against cecal coccidiosis (Eimeria tenella) infections[1]. Nequinate inhibits xanthine oxidoreductase (XOD) activity[2].
PTC725 is a potent, selective, and orally bioavailable inhibitor of HCV NS4B, inhibits HCV 1b (Con1) replicons with EC50 of 1.7 nM; displays a selectivity index of >5,000 with respect to cellular GAPDH, and >1,000-fold selectivity window with respect to cytotoxicity; retains fully activity against HCV replicon mutants that are resistant to inhibitors of NS3 protease and NS5B polymerase, demonstrates synergistic affect in combination with alpha interferon in vivo.
Salannin, a limonoid bitter principle of the seed oil of Azadirachta indica, shows antiulcer and spermicidal activities. Salannin displays antibacterial activity towards both Gram-positive and Gram-negative bacteria[1][2].
Enpp-1-IN-9 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-9 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51)[1].
Adenallene, a nucleoside analogue, is an anti-HIV compound. Adenallene inhibits replication and cytopathic effect of HIV-1 and HIV-2[1].
Antitubercular agent-14 (Compound 1) is an antitubercular agent with an MIC of 0.3 µg/mL against M. tuberculosis[1].
Omodenbamab is an anti-SpA (Staphylococcal protein A) humanized monoclonal antibody with a KD value of 0.0467 nM. Omodenbamab circumvents a key S. aureus evasion mechanism by targeting the cell wall moiety Protein A (SpA). Omodenbamab can be used in research of S. aureus bloodstream infection[1].
Ganoderic acid TR is a broad-spectrum inhibitor against influenza neuraminidases (NAs), particularly H5N1 and H1N1 neuraminidases. The IC50 values of 10.9 and 4.6 μM, respectively[1].
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
Secnidazole is a nitroimidazole anti-infective drug.
Antibacterial agent 55 (example 21) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system[1].
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis[1].
Pseudolaric acid A-O-β-D-glucopyranoside, isolated from Cortex Pseudolaricis, demonstrates antifungal and antifertility activities[1].
Urease-IN-3 (Compound L12) is a potent inhibitor of Urease with an IC50 of 1.449 μM. Urease-IN-3 is a flavonoid analogue compound[1].
QPX7728 is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. QPX7728 inhibits key serine and metallo beta-lactamases at a nano molar range[1].
Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM. IC50 Value: 15 nMTarget: HIV IntegraseBMS-707035 was scheduled to be evaluated in a Phase II study to assess the antiretroviral activity, safety, pharmacodynamics, and pharmacokinetics in 50 HIV-infected subjects using a 10-day randomized, double-blind, placebo-controlled, ascending multiple-dose study design.
Cefcapene pivoxil is an orally active cephalosporin antibiotic. It is a precursor agent that dissociates into free acid and then exerts antibacterial effect[1].
Canadensolide is an antifungal metabolite of Penicillium canadense.
Antistaphylococcal agent 2 is an antistaphylococcal therapeutic agent.
SARS-CoV-2-IN-17 (Compound 16) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-17 exhibits potent anti-viral activity with the EC50 of 2.18 μM. SARS-CoV-2-IN-17 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-17 is a potent NPro ligand[1].
Fiztasovimab (NPC-21; EV2038) is a fully human IgG1λ mAb against human cytomegalovirus (hCMV). Fiztasovimab acts neutralizing activity by binding to the antigenic domain 1 of glycoprotein B on hCMV envelope. Fiztasovimab inhibits cell-to-cell transmission of hCMV[1].
Yhhu6669 is an anti-HBV agent. Yhhu6669 inhibits HBV DNA. Yhhu6669 inhibits HBV replication by inducing the formation of DNA-free capsids. Yhhu6669 decreases HBV DNA and HBcAg in AAV/HBV-infected mice. Yhhu6669 has favorable PK properties[1].
Loracarbef-d5 is the deuterium labeled Loracarbef. Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].