CAS: 2637-37-8; Quinoline-2-Thiol

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📜2-氯喹啉置于硫脲,Sodium Hydroxide体系中,用 乙醇 用作溶剂,化学反应生成2-喹啉硫醇
参考文献:作为针对 Tlr2 和 P53 途径的潜在辐射防护分子的新型喹啉衍生物的设计,合成,生物学评估和计算机研究
标题:作为针对 Tlr2 和 P53 途径的潜在辐射防护分子的新型喹啉衍生物的设计,合成,生物学评估和计算机研究
摘要:太空电离辐射,辐射装置或核灾难是对人类健康和公共安全的重大威胁.本文以p53凋亡途径和tlr2通路为靶点,寻找潜在的减轻辐射损伤的新型化合物,设计,合成了一系列新型喹啉衍生物,并评价了它们的生物活性.合成的大多数化合物均表现出显着的辐射防护作用,其中该化合物的性能最好.因此,我们验证了其辐射防护活性并研究了其优异活性的机制.结果表明,该化合物不仅显着提高了小鼠受辐射致死后30天的存活率(80%),而且显着减轻了辐射对小鼠造血系统和肠道组织的损伤.机理研究表明,该化合物作用于p53通路,减少辐射诱导的细胞凋亡,同时刺激tlr2上调辐射防护因子的表达.分子动力学研究表明该化合物能够有效地与tlr2蛋白结合,并进一步揭示了结合机制.总而言之,我们研究的所有结果表明喹啉衍生物是一种有效的辐射防护化合物,具有进一步开发的巨大治疗潜力.
Doi:10.1016/j.Ejmech.2024.116239

专利信息

专利号:US-8735586-B2
优先权日:2007-06-26
标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR
权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

专利号:US-5656662-A
优先权日:1990-01-12
标 题:Synthesis of optically pure 4-alkenyl- or 4-alkanyl-2-hydroxytetronic acids
发明人：MANTRI PADMAJA; WITIAK DONALD T
权利人:UNIV OHIO STATE RES FOUND
摘要:The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, thus making them useful in the treatment of coronary artery diseases, especially atherosclerosis, and additionally, as inhibitors of various inflammatory cytokines, making them useful in the treatment of both acute and chronic inflammation, as well in the treatment of cachexia, rheumatoid arthritis, multiple sclerosis, Crohn's disease and ulcerative colitis. The invention further relates to pharmaceutical compositions of the instant compounds.

专利号:EP-2173747-B1
优先权日:2007-06-26
标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS
权利人:SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

专利号:US-5399339-A
优先权日:1990-07-04
标 题:Process for the preparation of nitride complexes of transition metals
发明人：PASQUALINI ROBERTO; COMAZZI VERONIQUE; BELLANDE EMMANUEL
权利人:CIS BIO INT
摘要:Process for the preparation of nitride complexes of transition metals for use as radiopharmaceutical products or for the synthesis of novel pharmaceutical products. The process consists in reacting an oxygenic transition metal compound such as 99m Tc , 186 Re or 188 Re , with a first nitrogenous ligand such as sodium nitride or a nitrogenous compound such as S-methyl, N-methyl dithiocarbazate, and a reducing agent consisting of either tin (II) or a dithionite. The product so obtained can be used for the preparation of radiopharmaceutical products by a reaction with a second ligand such as sodium dithiocarbamate.

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-2008119515-A1
优先权日:2003-03-10
标题:Heterocyclic Kinase Inhibitors: Methods of Use and Synthesis
发明人：SIDDIQUI M ARSHAD; BELANGER DAVID B; DAI CHAOYANG; ZHAO LIANYUN
权利人:SIDDIQUI M ARSHAD; BELANGER DAVID B; DAI CHAOYANG; ZHAO LIANYUN
摘要:Inhibitors of kinases, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptom.