CAS: 77168-63-9; 4-(Pyridin-4-yl)Thiazole-2-Thiol

相似化合物

2103-88-0 2103-95-9 30235-28-0

4-乙酰吡啶置于氢溴酸,溴,溶剂黄146体系中,用 乙醇,水 作为反应溶剂,化学反应 6.0H,反应生成 2-巯基-4-(4-吡啶基)噻唑
参考文献:具有广谱抗菌和强效抗 Mrsa 活性的季铵化吡啶-噻唑-截短侧耳素衍生物的发现
标题:具有广谱抗菌和强效抗 Mrsa 活性的季铵化吡啶-噻唑-截短侧耳素衍生物的发现
摘要:化合物的季铵化已成为抗生素开发的一种有前景的分子设计策略.在此,我们报道了一系列含有季胺c-14侧链的新型截短侧耳素衍生物的设计,合成,抗菌活性和构效关系.大多数这些衍生物对测试的细菌表现出广谱抗菌活性. 10B是最有效的抗菌剂,对临床分离的5种耐甲氧西林金黄色葡萄球菌(mrsa)具有优异的抗菌活性,显着的抗支原体活性,快速的杀菌作用以及强大的破坏细菌生物膜的能力.进一步的机理研究表明10B通过破坏细菌细胞膜来发挥抗菌作用.此外,10B在全身性 Mrsa 感染的小鼠模型中表现出高生存保护和有效的体内抗菌功效(ed 50 = 4.94 Mg/kg).这些发现表明,10B是治疗多重耐药传染病,特别是 Mrsa 感染的有希望的候选药物.
DOI:10.1021/acs.Jmedchem.2C02135

专利信息

专利号:WO-2016128580-A1
优先权日:2015-02-13
标题 :Cephalosporin intermediate and process for its preparation
发明人：RICCI ANTONIO; ZANON JACOPO
权利人:FRESENIUS KABI ANTI-INFECTIVES SRL
摘要:Provided is a synthesis of cephalosporin derivatives, characterized by the use of the new intermediates for the preparation of cephalosporin derivatives, a crystalline toluene hemi-solvate of benzhydryl (6R,7R)-7β-[(phenylacetyl)amino]-3-[4-pyridyl-2-thiazolylthio]-3-cephem-4-carboxylate, and a crystalline 4-[2-[[(6R,7R)-7-amino-2 carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]-thio]-4-thiazolyl]-1-methyl-pyridinium chloride, hydrochloride (1:1:1), obtained by a specific process and processes for preparation thereof.

专利号:US-12384771-B2
优先权日:2022-03-29
标题 :Pleuromutilin derivative containing thiazole-pyridine benzyl quaternary ammonium salt side chain and preparation method and use thereof
发明人：LIANG CHENGUAN; Kang Kairui; KE CHANGHUA; WANG YANZI; LIU YUTING; Yang Xiuding; ZHOU YING; LI JIAXUAN
权利人:UNIV SHAANXI SCIENCE & TECH
摘要:The present invention discloses a pleuromutilin derivative containing thiazole-pyridine benzyl quaternary ammonium salt side chain and a preparation method and use thereof and belongs to the field of medicinal chemistry. A pleuromutilin derivative with thiazole-pyridine benzyl quaternary ammonium salt side chain is successfully prepared by structural reconstruction of pleuromutilin and then structural modification with a quaternary ammonium salt compound. This compound synthesis method has the advantages of easily available raw materials, simple operation and high product yield, and is suitable for industrial production. The results of in vitro pharmacological experiments show that the pleuromutilin derivative of the present invention have good antibacterial and anti-mycoplasma activities, as well as good solubility, and these results show that the pleuromutilin derivative is of great value in the development of an anti-pathogenic microorganism drug.