Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines
作者:Xu Hui、Julie Desrivot、Christian Bories、Philippe M. Loiseau、Xavier Franck、Reynald Hocquemiller、Bruno Figadère
DOI:10.1016/j.bmcl.2005.11.025
日期:2006.2
A series of 29 new quinoxalines was synthesized and evaluated in vitro against several parasites (Leishmania donovani, Trypanosoma brucei brucei, and Trichomonas vaginalis). Several of them displayed interesting activities, and particularly four quinoxaline amides showed in vitro antileishmanial properties (IC50 less than 20 microM).
The synthesis of new 2,4-diaminofuro[2,3-<i>d</i>]pyrimidines with 5-biphenyl, phenoxyphenyl and tricyclic substitutions as dihydrofolate reductase inhibitors
作者:Aleem Gangjee、Nauzer P. Dubash、Sherry F. Queener
DOI:10.1002/jhet.5570370442
日期:2000.7
was more than 3 times as selective for Pneumocystis carinii dihydrofolatereductase compared to rat liver dihydrofolatereductase. Compounds 4b and 4c also exhibited selectivity. Compounds in the C8-S9 bridged series showed comparable potencies, and each showed higher selectivity for Pneumocystis carinii dihydrofolatereductase compared to rat liver dihydrofolatereductase.
合成非经典的2,4-二氨基-5-取代的呋喃并[2,3- d ]嘧啶4a-i,5a-b和7a-f,作为先前报道的抗叶酸剂1a-b的扩展芳环类似物。扩展的芳族体系设计为更好地与机会性病原体卡氏肺孢子虫二氢叶酸还原酶的苯丙氨酸残基(Phe69)相互作用,以提供有效和选择性的卡氏肺孢子虫二氢叶酸还原酶抑制剂。通过亲核取代2,4-二氨基-5-(氯甲基)呋喃[2,3- d ]嘧啶3合成目标化合物与适当的芳香胺或硫醇。将该化合物作为来自卡氏肺孢子虫和弓形体的二氢叶酸还原酶的抑制剂进行了评估,并使用大鼠肝脏二氢叶酸还原酶作为哺乳动物参照物,确定了它们的选择性。在C8-N9桥连的系列中,与大鼠肝二氢叶酸还原酶相比,具有3-(2-甲氧基二苯并呋喃)侧链的化合物4e表现出最大的效力,对卡氏肺孢子虫二氢叶酸还原酶的选择性是其3倍以上。化合物4b和4c也表现出选择性。C8-S9桥连化合物中的化合物显示出可比的效价,
EPOXY COMPOUND AND MANUFACTURING METHOD THEREOF
申请人:Ono Koutaro
公开号:US20110040111A1
公开(公告)日:2011-02-17
A novel epoxy compound represented by the following formula and a method for producing the same are provided:
wherein R
1
and R
2
are members selected from the group consisting of hydrogen, aliphatic hydrocarbon group having 1 to 4 carbon atoms, alicyclic hydrocarbon group having 3 to 6 carbon atoms, aromatic hydrocarbon group having 6 to 10 carbon atoms, halogen atom, ether group, ester group, acyl group and nitro group, n is an integer of 1 to 4, and m is an integer of 1 to 5.
A series of 4-aminoquinazoline derivatives is prepared by the nucleophilic substitution reaction of 6,7,8-trimethoxy-4-chloroquinazoline and aryl amine. The structures of the compounds are confirmed by elemental analysis, IR, and H-1 NMR spectral data. The compounds are also evaluated for their ability to inhibit tumor cells PC3, A431, Beap-37, and BGC823 by MTT assays. Among them, 6b and 6e are found as potent inhibitors, with IC50 values ranging from 5.8 to 9.8 mu M, in vitro assay. (c) 2007 Elsevier Ltd. All rights reserved.