Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs
Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs
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DOI：
10.1016/j.bmc.2008.02.011
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发表时间：
2008-04-01
影响因子：
3.5
通讯作者：
Charris, Jaime
中科院分区：
文献类型：
--
作者：
Barazarte, Arthur;Camacho, Jose;Charris, Jaime
本文报道了3-氨基-9-芳基取代噻吩并[3，2-B]苯并噻嗪S，S-二氧化物2-脱羧合成方法的改进。研究了噻吩并-[3，2-B]苯并噻嗪S，S-二氧化物衍生物抑制b-正铁血红素形成、血红蛋白水解的能力以及它们在啮齿动物伯氏疟原虫中的体内功效。化合物5 j-o作为血红蛋白水解的抑制剂是最有前途的，然而，这些化合物不如氯喹有效。在这一系列的构效关系（SAR）进行了研究。我们的研究结果使我们能够确定产生生物反应的最低结构要求。(C)2008爱思唯尔有限公司保留所有权利。
An improved procedure for the synthesis of 3-amino-9-arylsubstituted-thieno[3,2-b] benzothiazine S,S-dioxide 2-decarboxylated is reported. Thieno-[3,2-b] benzothiazine S,S-dioxide derivatives were investigated for their abilities to inhibit b-hematin formation, hemoglobin hydrolysis and in vivo for their efficacy in rodent Plasmodium berghei. Compounds 5j-o were the most promising as inhibitors of hemoglobin hydrolysis, however, the compounds are not as efficient as chloroquine. A structure-activity relationship (SAR) study was carried out in this series. Our results allow us to determine the minimal structural requirements to produce the biological response. (C) 2008 Elsevier Ltd. All rights reserved.