Novel Indolyl Aryl Sulfones Active Against HIV-1 Carrying NNRTI Resistance Mutations: Synthesis and SAR Studies

Romano Silvestri; Gabriella De Martino; Giuseppe La Regina; Marino Artico; Silvio Massa; Laura Vargiu; Massimo Mura; Anna Giulia Loi; Tiziana Marceddu; Paolo La Colla

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Novel Indolyl Aryl Sulfones Active Against HIV-1 Carrying NNRTI Resistance Mutations: Synthesis and SAR Studies

机译：新型抗HIV-1携带NNRTI抗性突变的吲哚芳基砜：合成和SAR研究

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The potent anti-HIV-1 activities of L-737,126 (2) and PAS sulfones prompted us to design and test against HIV-1 in acutely infected MT-4 cells a number of novel 1- and 3-benzenesulfonylindoles. Indoles belonging to the 1-benzenesulfonyl series were found poorly or totally inactive. On the contrary, some of the 3-benzenesulfonyl derivatives turned out to be as potent as 2, being endowed with potencies in the low nanomolar concentration range. In particular, (2-methylphenyl)sulfonyl (72) and (3-methylphenyl)sulfonyl (73) derivatives showed EC_(50) values of 1 nM. Introduction of two methyl groups at positions 3 and 5 of the phenyl ring of 2 furnished derivatives (80 and 83) which showed very potent and selective anti-HIV-1 activity not only against the wt strain, but also against mutants carrying NNRTI-resistant mutations at positions 103 and 181 of the reverse transcriptase gene.

机译：L-737,126（2）和PAS砜具有很强的抗HIV-1活性，促使我们设计和测试了急性感染的MT-4细胞中许多新型的1-和3-苯磺酰吲哚的HIV-1。发现属于1-苯磺酰基系列的吲哚几乎没有或完全没有活性。相反，某些3-苯磺酰基衍生物具有与2相同的效力，被赋予低纳摩尔浓度范围内的效力。特别地，（2-甲基苯基）磺酰基（72）和（3-甲基苯基）磺酰基（73）衍生物的EC_（50）值为1nM。在2个提供的衍生物（80和83）的苯环的3和5位上引入两个甲基，这些衍生物不仅对wt菌株而且对带有NNRTI抗性的突变体均显示出非常有效的选择性HIV-1活性逆转录酶基因的103和181位突变。

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《Journal of Medicinal Chemistry》 |2003年第12期|共12页
作者
Romano Silvestri; Gabriella De Martino; Giuseppe La Regina; Marino Artico; Silvio Massa; Laura Vargiu; Massimo Mura; Anna Giulia Loi; Tiziana Marceddu; Paolo La Colla;
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1. Novel Indolyl Aryl Sulfones Active Against HIV-1 Carrying NNRTI Resistance Mutations: Synthesis and SAR Studies [J] . Romano Silvestri, Gabriella De Martino, Giuseppe La Regina, Journal of Medicinal Chemistry . 2003,第12期

机译：新型抗HIV-1携带NNRTI抗性突变的吲哚芳基砜：合成和SAR研究
2. Indolyl Aryl Sulfones (IASs): Development of Highly Potent NNRTIs Active Against wt-HIV-1 and Clinically Relevant Drug Resistant Mutants [J] . R. Silvestri M. Artico Current Pharmaceutical Design . 2005,第29期

机译：吲哚基芳基砜（IASs）：高活性NNRTIs对wt-HIV-1和临床相关的耐药突变体的活性开发
3. Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives [J] . Ragno R, Artico M, De Martino G, Journal of Medicinal Chemistry . 2005,第1期

机译：吲哚基芳基砜的对接和3-D QSAR研究。 HIV-1逆转录酶非核苷结合位点的结合模式探索及高活性N-（2-羟乙基）羧酰胺和N-（2-羟乙基）碳酰肼衍生物的设计
4. Synthesis of poly(aryl sulfone benzimidazole) sulfone [C] . Guanjun Chang, Lin Zhang, Runxiong Lin International Conference on Advanced Engineering Materials and Technology . 2011

机译：聚（芳基砜苯并咪唑）砜的合成
5. Synthesis and characterization of poly(aryl ether)sulfone-vinyl block copolymers: Model studies. [D] . Phulpagar, Stanley Samuel. 1992

机译：聚（芳基醚）砜-乙烯基嵌段共聚物的合成与表征：模型研究。
6. Discovery synthesis and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root [O] . Chengbo Xu, Yijing Xin, Minghua Chen, -1

机译：发现合成和优化针对板蓝根中带有NNRTI耐药突变的HIV-1的N-烷氧基吲哚基乙酰胺
7. Discovery, synthesis, and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root [O] . Chengbo Xu, Yijing Xin, Minghua Chen, 2020

机译：从Isatis Indigotica根系中抵抗HIV-1的N-烷氧基InvolylaCainide的发现，合成和优化。
8. Chemical Modification of Matrix Resin Networks with Engineering Thermoplastics. III. Synthesis and Properties of Epoxy Networks Modified with Amine Terminated Poly(Aryl Ether Sulfone) Oligomers [R] . Hedrick, J. L., Jurek, M. J., Yilgor, I., 1985

机译：工程热塑性塑料对基质树脂网络的化学改性。 III。胺封端聚（芳醚砜）低聚物改性环氧网络的合成与性能

Novel Indolyl Aryl Sulfones Active Against HIV-1 Carrying NNRTI Resistance Mutations: Synthesis and SAR Studies

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