CAS: 3810-35-3; N-(5-Nitrothiazol-2-yl)Thiophene-2-Carboxamide

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CAS号5271-67-0 2-噻吩甲酰氯 | CAS号121-66-4 2-氨基-5-硝基噻唑

📜2-噻吩甲酰氯,2-氨基-5-硝基噻唑置于三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 24.0H,以91%的收率获得替诺尼唑
参考文献:杂芳基硝唑尼特类似物的合成,体外生物测定和计算研究
标题:杂芳基硝唑尼特类似物的合成,体外生物测定和计算研究
摘要:抗原虫药物硝唑尼特(ntz)已显示出多种药理学特性,并已出现在多项临床试验中.在此,我们介绍了 Ntz 的四种杂芳基酰胺类似物的合成,表征,体外生物学研究和计算机研究.在合成的分子中,化合物2和化合物4对大肠杆菌( E.Coli )表现出非常好的抗菌活性,体外抗菌试验显示其优于母药硝唑尼特.化合物2显示出 20 Mm 的抑制区,是最低浓度 (12.5 µg/ml) 母药 Ntz (10 Mm) 的两倍.化合物1也表现出与硝唑尼特相似的抗菌作用.还通过在hela细胞系中采用细胞计数试剂盒 8 (Cck-8) 测定技术测试了类似物的体外细胞毒活性,化合物2被鉴定为潜在的抗癌剂,其 Ic 50值为 172 µg,这证明了其比硝唑尼特更有效 (Ic 50 = 428 µg).此外,这些化合物还针对各种细菌和癌症信号蛋白进行了分子对接研究.体外测试结果证实了计算机对接研究,化合物2和化合物4对蛋白质具
Doi:10.1002/prp2.800

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-9740034-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

专利号:JP-2000508664-A
优先权日:1996-04-22
标题:Solid-phase and combinatorial synthesis of substituted thiophenes and arrays of substituted thiophenes

专利号:EP-1021435-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

专利号:US-7199128-B2
优先权日:2005-02-02
标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
发明人：BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.