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参考文献:Tuning And Predicting Biological Affinity: Aryl Nitriles As Cysteine Protease Inhibitors
标题:Tuning And Predicting Biological Affinity: Aryl Nitriles As Cysteine Protease Inhibitors
摘要:制备了一系列芳基腈基配体,以研究它们的亲电性对与胱氨酸蛋白酶罗德西亚酶和人类组织蛋白酶l的亲和力的影响.密度泛函理论计算提供了这些腈的相对反应性,使得能够预测它们的生物亲和力和细胞毒性,并明确了结构-活性关系.
DOI:10.1039/c2Ob00034B

专利信息

专利号:US-8063224-B2
优先权日:2006-12-01
标 题 :Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILIPPE; RAMTOHUL YEEMAN K
权利人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILIPPE; RAMTOHUL YEEMAN K; MERCK CANADA INC
摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.