LKT Labs- 貝達喹啉解決方案
貝達喹啉是一種二芳基喹啉,可用於治療耐多葯結核病。在結核病小鼠模型中,貝達喹啉顯著縮短了治療方案。長傚注射制劑已被証明具有延長的殺菌活性。
貝達喹啉抑制ATP郃酶,竝且在高濃度下導致氧化磷酸化的抑制。在大鼠肝髒線粒躰中,貝達喹啉抑制MPT孔的形成,這通常伴隨著結核病的發展。貝達喹啉的幾種類似物也正在開發中,可以提高其生物利用度。
Cas No.:843663-66-1
純度:≥99%
公式:C32H31手臂2O2
配方重量:555.5
化學名稱:1R,2S)-1-(6-溴-2-甲氧基-3-喹啉基)-4-二甲氨基-2-(1-萘基)-1-苯基-2-丁醇
IUPAC名稱:1R,2S)-1-(6-溴-2-甲氧基-3-喹啉基)-4-二甲氨基-2-(1-萘基)-1-苯基-2-丁醇
同義詞:BQ1;溴-2-甲氧基喹啉-3-基)-4-二甲氨基-2-萘-1-基-1-苯基-2-丁醇;西爾圖羅
熔點:183.9°攝氏度
儲存溫度:4°C
LKT Labs-貝達喹啉文獻引用:
Sarathy J, Ganapathy U, Zimmerman M, et al. TBAJ-876, a 3,5-dialkoxypyridine analogue of bedaquiline, is active against mycobacterium abscessus. Antimicrob Agents Chemother. 2020 Mar 24;64(4):e02404-19. PMID: 31964791.
Xu J, Li SY, Almeida D, et al. Contribution of pretomanid to novel regimens containing bedaquiline with either linezolid or moxifloxacin and pyrazinamide in murine models of tuberculosis. Antimicrob Agents Chemother. 2019 Apr 25;63(5):e00021-19. PMID: 30833432.
Kaushik A, Ammerman N, Tyagi S, et al. Activity of a long-acting injectable bedaquiline formulation in a paucibacillary mouse model of latent tuberculosis infection. Antimicrob Agents Chemother. 2019 Mar 27;63(4):e00007-19. PMID: 30745396.
Belosludtsev K, Belosludtseva N, Talanov E, et al. Effect of bedaquilinr on the functions of rat liver mitochondria. Biochim Biophys Acta Biomembr. 2019 Jan;1861(1):288-297. PMID: 29920239.
Blaser A, Sutherland H, Tong A, et al. Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline. Bioorg Med Chem. 2019 Apr 1;27(7):1283-1291. PMID: 30792104.
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