CAS: 499-55-8; 3-Fluorobenzohydrazide

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CAS号455-68-5 3-氟苯甲酸甲酯 | CAS号451-02-5 3-氟苯甲酸乙酯 | CAS号455-38-9 间氟苯甲酸 | CAS号445-29-4 邻氟苯甲酸 | CAS号203268-63-7 5-(3-氟苯基)-1,3,4... | CAS号350672-16-1 2-(chloromethyl... | CAS号116324-98-2 2-hydroxy-1-nap... | CAS号502685-67-8 5-(3-氟苯基)-1,2-二... | CAS号5378-32-5 2-(3-fluorophen...

📜间氟苯甲酸置于硫酸,一水合肼体系中,用 Neat (No Solvent) 作为反应溶剂,化学反应生成 3-氟苯甲酰肼
参考文献:1,2,4-三唑-3-硫酮化合物作为二嗪金属β-内酰胺酶的抑制剂.
标题:1,2,4-三唑-3-硫酮化合物作为二嗪金属β-内酰胺酶的抑制剂.
摘要:金属β-内酰胺酶(mbls)引起革兰氏阴性细菌对β-内酰胺类抗生素的耐药性并引起人们的严重关注,因为它们可以使最后的碳青霉烯类药物失活,并且仍然缺乏具有临床价值的mbl抑制剂.我们之前确定了在其二嗪活性位点内4-氨基-2,4-二氢-5-(2-甲基苯基)-3H-1,2,4-三唑-3-硫酮(化合物iiia)的原始结合模式. L1 Mbl.在这里,我们提出了l1与相应的非氨基化合物iiib(1,2-二氢-5-(2-甲基苯基)-3H-1,2,4-三唑-3-硫酮)的配合物的晶体结构.出乎意料的是,Iiib的结合模式与iiia相似,但相反.3D结构表明三唑-硫酮骨架适合结合二锌金属酶的催化位点.根据这些结果,我们合成了iiia或iiib的54个类似物.有19个显示的ic50值在微摩尔范围内,朝着五个代表性mbl(即l1,Vim-4,Vim-2,Ndm-1和imp-1)中的至少一个显示.其中五个对至少四
DOI:10.1002/cmdc.201700186

专利信息

专利号:US-8981092-B2
优先权日:2008-09-19
标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity
发明人：MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO
权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL
摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

专利号:CN-114835656-A
优先权日:2022-05-13
标 题:A kind of ethyl 1,3,4-oxadiazole acetate and its synthesis method