CAS: 86984-32-9; 6-Chloro-5-Nitroquinoline

相似化合物

341010-40-0 1209246-34-3 226073-82-1

上下游产品

CAS号612-57-7 6-氯喹啉 | CAS号106-47-8 对氯苯胺 | CAS号635-22-3 4-氯-3-硝基苯胺 | CAS号56-81-5 甘油 | CAS号341010-40-0 5-氨基-6-氯喹啉 | CAS号42606-37-1 6-氨基-5-硝基喹啉 | CAS号606-42-8 5,6-Dichloroqui...

6-氯喹啉置于硫酸,硝酸体系中,用88%的收率获得产物6-氯-5-硝基喹啉
参考文献:一种用于设计强效,高选择性和脑渗透性 N-肉豆蔻酰基转移酶抑制剂的分子杂交方法.
标题:一种用于设计强效,高选择性和脑渗透性 N-肉豆蔻酰基转移酶抑制剂的分子杂交方法.
摘要:晶体学已经指导了两个系列的布氏锥虫 N-肉豆蔻酰转移酶 (Nmt) 抑制剂的杂交,从而产生了一个新的高选择性系列.结合来自两种药效团的选择性增强元素的效果被证明是相加的,并导致化合物对 Tbnmt 与 Hsnmt 的选择性超过 1000 倍.混合系列的进一步优化已经确定了具有显着杀锥虫活性的化合物,能够穿过血脑屏障.通过使用 Cf-1 Mdr1A 缺陷小鼠,我们能够在 2 期非洲昏睡病小鼠模型中证明体内完全治愈.这项工作和以前的工作为 Nmt 作为人类非洲锥虫病在外周和中枢神经系统疾病阶段的药物靶点提供了非常有力的验证.
DOI:10.1021/acs.Jmedchem.8B00884

专利信息

专利号:US-5656634-A
优先权日:1991-03-21
标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT)
发明人：CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J
权利人:PFIZER
摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

专利号:US-5596001-A
优先权日:1993-10-25
标题 :4-aryl-3-(heteroarylureido)quinoline derivatves
发明人：HAMANAKA ERNEST S
权利人:PFIZER
摘要:Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.