CAS: 57018-46-9; 4-Azidophenacylbromide

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CAS号20062-24-2 对叠氮基苯乙酮 | CAS号186581-53-3 重氮甲烷 | CAS号14848-01-2 4-叠氮基苯甲酰氯

📜对叠氮苯甲酸置于草酰氯,N,N-二甲基甲酰胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.33H,反应生成 4-叠氮苯甲酰甲基溴
参考文献:基于2-氨基咪唑支架的抗分枝杆菌生物膜剂的鉴定.
标题:基于2-氨基咪唑支架的抗分枝杆菌生物膜剂的鉴定.
摘要:结核病(tb)仍然是全球性的重大健康问题,因此迫切需要新的治疗方法.病原体结核分枝杆菌驻留在宿主巨噬细胞内并形成生物膜样群落的能力有助于该疾病的持久性和药物耐受性.可以预防或逆转生物膜样表型的化合物有可能与结核病抗生素一起使用,以克服这种耐受性并缩短治疗时间.我们使用耻垢分枝杆菌作为替代生物,报告了两种抑制和分散分枝杆菌生物膜的新的2-氨基咪唑化合物的鉴定,它们与异烟肼和利福平协同作用,可在体外根除预先形成的耻垢分枝杆菌生物膜,对马勒菌无毒,并展示小鼠血浆中的稳定性.
DOI:10.1002/cmdc.201900033

专利信息

专利号:US-2008051323-A1
优先权日:2004-08-21
标 题 :Chloroquine drug compositions and methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

专利号:US-2007060499-A1
优先权日:2005-09-15
标 题 :Chloroquine combination drugs and methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

专利号:US-2007166281-A1
优先权日:2004-08-21
标题 :Chloroquine coupled antibodies and other proteins with methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.

专利号:US-2006040879-A1
优先权日:2004-08-21
标 题:Chloroquine coupled nucleic acids and methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions and methods for preparing chloroquine-coupled nucleic acid compositions. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the nucleic acid needs to be released, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a nucleic acid directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.

专利号:US-2005153913-A1
优先权日:2001-04-10
标 题 :Nucleic acid carrier compositions and methods for their synthesis
发明人：KOSAK KENNETH M
摘要:This invention discloses compositions and methods for preparing pharmaceutical nucleic acid carriers. The compositions comprise a carrier substance coupled to a nucleic acid intercalator whereby the intercalator is coupled by intercalation to the nucleic acid. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.

专利号:US-6107039-A
优先权日:1996-07-24
标 题:Assays using base protected table 1
发明人：HANNA MICHELLE M
权利人:UNIV OKLAHOMA
摘要:The present invention is directed to protected thiol analogs of pyrimidine bases for syntheses of DNA and RNA by chemical or enzymatic methods. The subject analogs include reagents suitable for DNA or RNA synthesis via phosphoramidite, H-phosphonate or phosphotriester chemistry as well a reagents suitable for use by RNA and DNA polymerase, including thermostable polymerases employed by PCR or other nucleic acid amplification techniques. The nucleotide analogs synthesized by methods of this invention can thus be incorporated into oligonucleotides or polynucleotides, deprotected and derivatized with a functional group. In some cases the protecting groups are themselves antigenic and may be left on the oligonucleotides or polynucleotides for detection with antibodies. A method of synthesizing oligonucleotides with a functional group using the subject nucleotide analogs is also provided.