| Identification | Back Directory | [Name]
Thieno[3,2-b]pyridine-6-carboxamide, N-butyl-4,5-dihydro-7-hydroxy-5-oxo-4-(phenylmethyl)- | [CAS]
1574576-45-6 | [Synonyms]
P163-0892
Thieno[3,2-b]pyridine-6-carboxamide, N-butyl-4,5-dihydro-7-hydroxy-5-oxo-4-(phenylmethyl)- | [Molecular Formula]
C19H20N2O3S | [MOL File]
1574576-45-6.mol | [Molecular Weight]
356.44 |
| Hazard Information | Back Directory | [Uses]
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration[1]. | [in vivo]
P163-0892 (10 mg/kg; 5 days) significantly extends the survival of larvae infected with either C. neoformans or C. gattii[1]. | Animal Model: | Wax moth larva infected with C. neoformans H99 or C. gattii WM178[1] | | Dosage: | 10 mg/kg | | Administration: | 5 days | | Result: | Increased the survival rate of larvae. |
| Animal Model: | Male Sprague–Dawley rats weighing 200–250 g[1] | | Dosage: | 2 mg/kg or 5 mg/kg | | Administration: | Intravenous or oral administration (Pharmacokinetic Analysis) | | Result: | Pharmacokinetic Parameters of P163-0892a[1]
| route | dose (mg/kg) | T1/2 (h) | Tmax (h) | AUC0-inf (h?ng/mL) | Cl (mL/h/kg) | MRT0-t (h) | Vdss (L/kg) | BA (%) | | iv | 2 mg/kg | 7.61 | | 749 | 172 | 2.63 | 7.12 | | | po | 5 mg/kg | 15.3 | 3.17 | NR | | 3.83 | NR | 0.8 |
aAbbreviations: iv, intravenous; po, per os; T1/2, half-life elimination in hours; Tmax, time of maximal concentration in hours; AUC, area under the curve; Cl, clearance; MRT, mean residence time; Vdss, volume of distribution at the steady state; BA, bioavailability; NR, not reportable; n = 3.
|
| [References]
[1] Li L, et al. Discovery of Novel 7-Hydroxy-5-oxo-4,5-dihydrothieno[3,2-b]pyridine-6-carboxamide Derivatives with Potent and Selective Antifungal Activity against Cryptococcus Species. J Med Chem. 2022 Aug 3. DOI:10.1021/acs.jmedchem.2c00794 |
|
|