Novel Tricyclic(新型三环)研究综述
Novel Tricyclic 新型三环 - The protocol proceeds under operationally simple conditions and provides novel tricyclic and tetracyclic scaffolds such as 3,4-dihydroindolo[1,2-c]quinazoline-1,6(2H,5H)-dione and 1H-[1,3]oxazino[3,4-a]indol-1-one derivatives with a broad range of functional group tolerance and moderate to excellent yields. [1] The synthetic route toward novel tricyclic, nitrogen-containing system is disclosed. [2] A new domino mode of assembly was discovered from the one-pot three-component reactions of pyrrole derivatives, active methylene compounds (malononitrile, methyl cyanoacetate, or ethyl cyanoacetate), and sodium cyanide in the presence of piperidinium acetate in EtOH at room temperature, leading to a novel tricyclic skeleton in excellent yield under mild and eco-friendly conditions. [3] To develop a selective TRPM2 inhibitor, three-dimensional similarity-based screening strategy was employed using the energy-minimized conformation of non-selective TRPM2 inhibitor 2-APB as the query structure, which resulted in the discovery of a novel tricyclic TRPM2 inhibitor Z-4 with benzo[d]imidazo[1,2-a]imidazole skeleton. [4] An efficient two-steps strategy for the regioselective synthesis of the benzo[f]pyrimido[4,5-b][1,5]oxazocine as a novel tricyclic system has been developed via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 2-aminobenzylalcohol in room temperature and short reaction times under mild conditions, followed amination with some secondary amines. [5] Purpose To evaluate efficacy and safety of novel tricyclic corneal stroma injection (TCSI) voriconazole for the treatment of fungal keratitis. [6] ABSTRACT Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions. [7] Here we show that WEHI-9625, a novel tricyclic sulfone small molecule, binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. [8] Cyclobutene alcohols undergo Prins cyclisations to generate single diastereomers of novel tricyclic heterocycles with five contiguous stereocentres. [9] A series of novel tricyclic quinazolinone-iminosugars 1 (a-c) were synthesized from the benzyl protected sugars through three steps. [10] All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1. [11] – The synthesis of novel tricyclic fused furo[2,3-b]pyridine derivatives is described. [12] Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats with experimental myocardial infarction. [13] Interestingly, the latter was seen to undergo facile reductive elimination, affording a novel tricyclic monodentate NHC ligand. [14] Medicinal chemistry design efforts yielded two novel tricyclic cores that enhanced M4 PAM potency, regained CNS penetration, displayed favorable DMPK properties and afforded robust in vivo efficacy in reversing amphetamine-induced hyperlocomotion in rats. [15] A novel tricyclic nested electromagnetic bandgap (TN-EBG) structure has been proposed to restrain the simultaneous switching noise (SSN) in high-speed digital systems. [16] This Letter describes the chemical optimization of a new series of muscarinic acetylcholine receptor subtype 1 (M1) positive allosteric modulators (PAMs) based on novel tricyclic triazolo- and imidazopyridine lactam cores, devoid of M1 agonism, e. [17] A novel tricyclic heterocyclic compound, 5,5’-(furan-2,5-diyl)bis (1,3,4- thiadiazol-2-amine) (3), was easily synthesized, which has an excellent fluorescence performance and could be a chemical sensor of Pd2+ at a very broad pH range. [18] A series of novel tricyclic matrinic derivatives with 11-adamantyl substitution were designed, synthesized, and evaluated for their activities against Influenza A H3N2 virus, based on the privileged structure strategy. [19] F-GE180 is a novel tricyclic indole compound that binds to TSPO with high affinity [3], and has been used with satisfactory results in a variety of preclinical models [4–6]. [20] Upon the prenylation, side reactions were observed, resulting in the formation of nucleolipids with a novel tricyclic nucleobase (→4a, 4b). [21]该协议在操作简单的条件下进行，并提供了新的三环和四环支架，例如 3,4-二氢吲哚[1,2-c]喹唑啉-1,6(2H,5H)-二酮和 1H-[1,3]恶嗪[ 3,4-a]indol-1-one 衍生物具有广泛的官能团耐受性和中等至优异的产率。 [1] 新型三环含氮系统的合成路线是 披露。 [2] 在室温下，在醋酸哌啶鎓的存在下，吡咯衍生物、活性亚甲基化合物（丙二腈、氰基乙酸甲酯或氰基乙酸乙酯）和氰化钠的一锅三组分反应发现了一种新的多米诺组装模式，在温和和环保的条件下，以优异的产率产生了一种新型的三环骨架。 [3] 为了开发选择性 TRPM2 抑制剂，采用基于三维相似性的筛选策略，使用非选择性 TRPM2 抑制剂 2-APB 的能量最小化构象作为查询结构，从而发现了一种新型三环 TRPM2 抑制剂 Z- 4 具有苯并[d]咪唑并[1,2-a]咪唑骨架。 [4] 通过 2,4-二氯的分子间和分子内杂环化，开发了一种区域选择性合成苯并[f]嘧啶并[4,5-b][1,5]恶唑辛作为新型三环体系的有效两步策略-5-(氯甲基)-6-甲基嘧啶和2-氨基苄醇在室温和温和条件下的短反应时间，然后用一些仲胺胺化。 [5] 目的评价新型三环角膜基质注射液（TCSI）伏立康唑治疗真菌性角膜炎的疗效和安全性。 [6] 摘要 通过 2,4-dichloro-5-(氯甲基）-6-甲基嘧啶和 6-氨基-4-芳基-2-硫代-1,2,3,4-四氢嘧啶-5-甲腈，反应时间短，条件温和。 [7] 在这里，我们展示了 WEHI-9625，一种新型的三环砜小分子，与 VDAC2 结合并促进其抑制由小鼠 BAK 驱动的细胞凋亡的能力。 [8] 环丁烯醇经历 Prins 环化以生成具有五个连续立体中心的新型三环杂环的单一非对映异构体。 [9] 一系列新型三环喹唑啉酮亚氨基糖 1 (a-c) 由苄基保护糖通过三个步骤合成。 [10] 评估了所有新型三环衍生物对单纯疱疹病毒 1 和 2（HSV-1、HSV-2）和胸苷激酶缺陷型（抗 ACV）HSV-1 的抑制活性。 [11] – 描述了新型三环稠合呋喃[2,3-b]吡啶衍生物的合成。 [12] 在无伴发病理的大鼠和实验性心肌梗死大鼠的动脉血栓形成模型中检测了二氮杂[1,2-α]苯并咪唑的新型三环衍生物 (DAB-15) 的抗血栓形成活性。 [13] 有趣的是，后者被认为经历了轻松的还原消除，提供了一种新的三环单齿 NHC 配体。 [14] 药物化学设计工作产生了两个新的三环核心，它们增强了 M4 PAM 效力，恢复了 CNS 渗透，表现出良好的 DMPK 特性，并在逆转苯丙胺诱导的大鼠过度运动方面提供了强大的体内功效。 [15] 已经提出了一种新颖的三环嵌套电磁带隙（TN-EBG）结构来抑制高速数字系统中的同时切换噪声（SSN）。 [16] 这封信描述了基于新型三环三唑并咪唑并吡啶内酰胺核心的新型毒蕈碱乙酰胆碱受体亚型 1 (M1) 正变构调节剂 (PAM) 的化学优化，没有 M1 激动剂，例如。 [17] 一种新型三环杂环化合物 5,5'-(furan-2,5-diyl)bis (1,3,4-thiadiazol-2-amine) (3) 易于合成，具有优异的荧光性能，可是 Pd2+ 在非常宽的 pH 范围内的化学传感器。 [18] 基于特权结构策略，设计、合成了一系列具有 11-金刚烷基取代的新型三环母体衍生物，并评估了它们对甲型 H3N2 病毒的活性。 [19] F-GE180 是一种新型三环吲哚化合物，与 TSPO 具有高亲和力 [3]，已在多种临床前模型中使用并取得了令人满意的结果 [4-6]。 [20] 在异戊烯化后，观察到副反应，导致形成具有新型三环核碱基的核脂（→4a，4b）。 [21]
novel tricyclic system
An efficient two-steps strategy for the regioselective synthesis of the benzo[f]pyrimido[4,5-b][1,5]oxazocine as a novel tricyclic system has been developed via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 2-aminobenzylalcohol in room temperature and short reaction times under mild conditions, followed amination with some secondary amines. [1] ABSTRACT Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions. [2]通过 2,4-二氯的分子间和分子内杂环化，开发了一种区域选择性合成苯并[f]嘧啶并[4,5-b][1,5]恶唑辛作为新型三环体系的有效两步策略-5-(氯甲基)-6-甲基嘧啶和2-氨基苄醇在室温和温和条件下的短反应时间，然后用一些仲胺胺化。 [1] 摘要 通过 2,4-dichloro-5-(氯甲基）-6-甲基嘧啶和 6-氨基-4-芳基-2-硫代-1,2,3,4-四氢嘧啶-5-甲腈，反应时间短，条件温和。 [2]
novel tricyclic derivative
All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1. [1] Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats with experimental myocardial infarction. [2]评估了所有新型三环衍生物对单纯疱疹病毒 1 和 2（HSV-1、HSV-2）和胸苷激酶缺陷型（抗 ACV）HSV-1 的抑制活性。 [1] 在无伴发病理的大鼠和实验性心肌梗死大鼠的动脉血栓形成模型中检测了二氮杂[1,2-α]苯并咪唑的新型三环衍生物 (DAB-15) 的抗血栓形成活性。 [2]