6-取代的2-(3',4'-二氯苯氧基)-2H-吡喃并[2,3-b]吡啶MDL 20,610、MDL 20,646和MDL 20,957的体外抗病毒活性
In vitro antiviral activity of the 6-substituted 2-(3',4'-dichlorophenoxy)-2H-pyrano[2,3-b]pyridines MDL 20,610, MDL 20,646, and MDL 20,957.
作者信息
Kenny M T, Dulworth J K, Bargar T M, Torney H L, Graham M C, Manelli A M
出版信息
Antimicrob Agents Chemother. 1986 Sep;30(3):516-8. doi: 10.1128/AAC.30.3.516.
Abstract
The 6-substituted 2-(3',4'-dichlorophenoxy)-2H-pyrano[2,3-b]pyridines MDL 20,610 (6-SO2CH3), MDL 20,646 (6-Br), and MDL 20,957 (6-Cl) are potent antirhinovirus compounds with median plaque 50% inhibitory concentrations (IC1/2s) of 0.03, 0.006, and 0.006 micrograms/ml, respectively, against the 32 serotypes evaluated. The 6-halogenated analogs produced 99% reductions in progeny virion yields at concentrations as low as 0.004 micrograms/ml. However, these analogs perturbated HeLa cell metabolism at lower concentrations (at or above 5 micrograms/ml) than did the 6-methylsulfonyl analog (at or above 20 micrograms/ml). Compound MDL 20,610 was also active against human, simian, and bovine rotaviruses (cytopathic effect IC1/2s of 0.8 to 1.5 micrograms/ml) and possessed variable enterovirus and paramyxovirus activity.
摘要
6-取代的2-(3',4'-二氯苯氧基)-2H-吡喃并[2,3-b]吡啶类化合物MDL 20,610（6-SO2CH3）、MDL 20,646（6-Br）和MDL 20,957（6-Cl）是强效抗鼻病毒化合物，针对所评估的32种血清型，其半数噬斑50%抑制浓度（IC1/2s）分别为0.03、0.006和0.006微克/毫升。6-卤代类似物在低至0.004微克/毫升的浓度下可使子代病毒粒子产量降低99%。然而，与6-甲基磺酰类似物（在20微克/毫升及以上）相比，这些类似物在更低浓度（在5微克/毫升及以上）时会干扰HeLa细胞代谢。化合物MDL 20,610对人、猴和牛轮状病毒也有活性（细胞病变效应IC1/2s为0.8至1.5微克/毫升），并具有可变的肠道病毒和副粘病毒活性。
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