Design, Synthesis, and Cytoprotective Effect of 2-Aminothiazole Analogues as Potent Poly(ADP-Ribose) Polymerase-1 Inhibitors

机译：2-氨基噻唑类似物作为强力聚（ADP-核糖）聚合酶-1抑制剂的设计，合成和细胞保护作用

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A series of novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors were designed within 2aminothiazole analogues (4-10) based on a constructed three-dimensional pharmacophore model. After synthesis, the inhibitory effect on PARP-1 activity and the cytoprotective action of these compounds were tested and evaluated. Among them, compounds 4-6 and 10 appeared to be potent PARP-1 inhibitors with IC50 values less than 1 μM, which had been perfectly predicted by pharmacophore model. These compounds proved to be highly potent against cell injury induced by H2O2 and oxygen-glucose deprivation (OGD) in PC12 cells. These novel 2-aminothiazole analogues are potentially applicable as neuroprotective agents for the treatment of neurological diseases.

机译：基于构建的三维药效团模型，在2aminothiazole类似物（4-10）中设计了一系列新型的poly（ADP-核糖）聚合酶-1（PARP-1）抑制剂。合成后，测试和评估了对PARP-1活性的抑制作用和这些化合物的细胞保护作用。其中，化合物4-6和10似乎是有效的PARP-1抑制剂，IC50值小于1μM，这已通过药效基团模型完美预测。这些化合物被证明对PC12细胞中H2O2和氧葡萄糖剥夺（OGD）诱导的细胞损伤具有很强的抵抗力。这些新颖的2-氨基噻唑类似物潜在地可用作神经保护剂，用于治疗神经系统疾病。

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《ICMSI;International conference of molecular simulations and applied informatics technologies》|2010年|p.806-813|共8页
会议地点 Wuhan(CN);Wuhan(CN)
作者
Wen-Ting Zhang; Gang-Ying Chen; Yi-Jing Zhu; Jun Gu; Jian-Guo Chen; Jin-Lan Ruan; Peng-Fei Wu; Feng-Chao Jiang; Li-Na Zhang; Wei Fang; Xiang-Long Chen; Yue Wang; Bao-Shuai Cao;
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Department of Medicinal Chemistry Tongji Medical College Huazhong University of Science and Technology;

Department of Pharmacology Tongji Medical College Huazhong University of Science and Technology;

Department of Pharmacology Tongji Medical College Huazhong University of Science and Technology The Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation of Hubei Province;

Department of Pharmacology Tongji Medical College Huazhong University of Science and Techn;

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1. Design, Synthesis, and Cytoprotective Effect of 2-Aminothiazole Analogues as Potent Poly(ADP-Ribose) Polymerase-1 Inhibitors [J] . Zhang WT, Ruan JL, Wu PF, Journal of Medicinal Chemistry . 2009,第3期

机译：2-氨基噻唑类似物作为有效的聚（ADP-核糖）聚合酶-1抑制剂的设计，合成和细胞保护作用
2. Design and synthesis of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. Part 4: biological evaluation of imidazobenzodiazepines as potent PARP-1 inhibitors for treatment of ischemic injuries. [J] . Ferraris D, Ficco RP, Dain D, Bioorganic and medicinal chemistry . 2003,第17期

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3. Design and Synthesis of Benzimidazole-4-carboxamides as Potent Poly(ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors [J] . Kalam B. Reddy, Gangula M. Rao, Baru V. Kumar, Current bioactive compounds . 2018,第2期

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4. Design, Synthesis, and Cytoprotective Effect of 2-Aminothiazole Analogues as Potent Poly(ADP-Ribose) Polymerase-1 Inhibitors [C] . Wen-Ting Zhang, Gang-Ying Chen, Yi-Jing Zhu, International conference of molecular simulations and applied informatics technologies . 2010

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5. Design and Synthesis of Poly(ADP-ribose) Polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity [D] . Velagapudi, Uday Kiran. 2019

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Design, Synthesis, and Cytoprotective Effect of 2-Aminothiazole Analogues as Potent Poly(ADP-Ribose) Polymerase-1 Inhibitors

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