Synthesis and biological evaluation-of ureido derivatives as VLA-4 antagonists

被引：0
作者：
Sattiyeri, Viswajanani J.
Soni, Ajay
Gupta, Lavleen K.
Ray, Abhijit
Ahmad, Sharif
Gupta, Jang B.
Salman, Mohammad
机构：
[1] New Drug Discovery Res, Dept Med Chem, Ranbaxy Res Labs, Gurgaon 122001, Haryana, India
[2] New Drug Discovery Res, Dept Pharmacol, Ranbaxy Res Labs, Gurgaon 122001, Haryana, India
[3] Jamia Millia Islamia, Dept Chem, Mat Res Lab, New Delhi 110025, India
来源：
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY | 2006年 / 45卷 / 11期
关键词：
VLA-4; antagonists; bioisosteres; ureido derivatives;
D O I：
暂无
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Bioisosteric replacement based design strategy was employed in order to improve pharniacokinetic properties Of TBC 3486, a potent VLA-4 antagonist. However, newly synthesized analogs did not show any significant activity.
引用
收藏
页码：2534 / 2541
页数：8
相关论文
共 22 条
[1]  
*ACD LABS, 2003, 7 00 REL PROD VERS 7
[2]  
BURGER A, 1970, MED CHEM, P287
[3]  
FOSTER PS, 1999, PROG INFLAM RES, P251
[4]  
FURNISS BS, 1989, VOGELS TXB PRACTICAL, P784
[5]   VLA PROTEINS IN THE INTEGRIN FAMILY - STRUCTURES, FUNCTIONS, AND THEIR ROLE ON LEUKOCYTES [J].
HEMLER, ME .
ANNUAL REVIEW OF IMMUNOLOGY, 1990, 8 :365-400
[6]   Antagonists of VLA-4 [J].
Holland, GW ;
Biediger, RJ ;
Vanderslice, P .
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 37, 2002, 37 :65-74
[7]  
HOLLAND GW, 2000, 219 ACS NAT M ACS WA
[8]   Conformational and topographical considerations in designing agonist peptidomimetics from peptide leads [J].
Hruby, VJ ;
Balse, PM .
CURRENT MEDICINAL CHEMISTRY, 2000, 7 (09) :945-970
[9]  
KASSIR JM, 1999, Patent No. 9952898
[10]   Very late antigen 4 (VLA4) antagonists as anti-inflammatory agents [J].
Lin, KC ;
Castro, AC .
CURRENT OPINION IN CHEMICAL BIOLOGY, 1998, 2 (04) :453-457
123