A series of highly potent, structurally novel, non-nucleoside RT inhibitors has been described. Low nanomolar concentrations of 5-chloro-3-(phenylsulfonyl)-indole-2-carboxamide (1) inhibit the HIV-1 RT enzyme in vitro and HTLVIIIb viral spread in MT-4 human T-lymphoid cells. Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel. When compared to other non-nucleoside inhibitors (e.g. 15-18), 1 possesses improved inhibitory potency with respect to the wild-type RT, as well as the K103N and Y181C mutant enzymes. Additional studies within this class of inhibitors are in progress.

中文翻译：

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5-氯-3-（苯磺酰基）吲哚-2-羧酰胺：一种新型的HIV-1逆转录酶的非核苷抑制剂。

已经描述了一系列高效，结构新颖的非核苷RT抑制剂。低纳摩尔浓度的5-氯-3-（苯磺酰基）-吲哚-2-羧酰胺（1）在体外抑制HIV-1 RT酶，并且HTLVIIIb病毒在MT-4人T淋巴细胞中传播。口服给予1的Methocel悬浮液后，在恒河猴中观察到良好的口服生物利用度。与其他非核苷抑制剂（例如15-18）相比，1具有相对于野生型RT以及K103N和Y181C突变酶的改善的抑制能力。这类抑制剂的其他研究正在进行中。