N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists

被引:10
作者
Porter, JR [1 ]
Archibald, SC [1 ]
Brown, JA [1 ]
Childs, K [1 ]
Critchley, D [1 ]
Head, JC [1 ]
Hutchinson, B [1 ]
Parton, TAH [1 ]
Robinson, MK [1 ]
Shock, A [1 ]
Warrellow, GJ [1 ]
Zomaya, A [1 ]
机构
[1] Celltech R&D Ltd, Slough SL1 4EN, Berks, England
关键词
D O I
10.1016/S0960-894X(02)00241-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The SAR studies to optimise both potency and rate of clearance in the rat for a series of pyrimidine and pyridine based VLA-4 antagonists are described. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1595 / 1598
页数:4
相关论文
共 13 条
[1]   Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists [J].
Archibald, SC ;
Head, JC ;
Gozzard, N ;
Howat, DW ;
Parton, TAH ;
Porter, JR ;
Robinson, MK ;
Shock, A ;
Warrellow, GJ ;
Abraham, WM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (09) :997-999
[2]   Diamine containing VLA-4 antagonists [J].
Astles, PC ;
Harris, NV ;
Morley, AD .
BIOORGANIC & MEDICINAL CHEMISTRY, 2001, 9 (08) :2195-2202
[3]   N-(2-benzoylphenyl)-L-tyrosine PPARγ agonists.: 3.: Structure-activity relationship and optimization of the N-aryl substituent [J].
Cobb, JE ;
Blanchard, SG ;
Boswell, EG ;
Brown, KK ;
Charifson, PS ;
Cooper, JP ;
Collins, JL ;
Dezube, M ;
Henke, BR ;
Hull-Ryde, EA ;
Lake, DH ;
Lenhard, JM ;
Oliver, W ;
Oplinger, J ;
Pentti, M ;
Parks, DJ ;
Plunket, KD ;
Tong, WQ .
JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (25) :5055-5069
[4]   Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent α4β1 integrin antagonists [J].
Duplantier, AJ ;
Beckius, GE ;
Chambers, RJ ;
Chupak, LS ;
Jenkinson, TH ;
Klein, AS ;
Kraus, KG ;
Kudlacz, EM ;
McKechney, MW ;
Pettersson, M ;
Whitney, CA ;
Milici, AJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (19) :2593-2596
[5]  
ELICES M, 1999, CURR OPIN ANTIINFLAM, V1, P14
[6]  
FRINK EJ, 1990, ANESTH ANALG, V71, P484
[7]   The discovery of sulfonylated dipeptides as potent VLA-4 antagonists [J].
Hagmann, WK ;
Durette, PL ;
Lanza, T ;
Kevin, NJ ;
de Laszlo, SE ;
Kopka, HE ;
Young, D ;
Magriotis, PA ;
Li, B ;
Lin, LS ;
Yang, G ;
Kamenecka, T ;
Chang, LL ;
Wilson, J ;
MacCoss, M ;
Mills, SG ;
Van Riper, G ;
McCauley, E ;
Egger, LA ;
Kidambi, U ;
Lyons, K ;
Vincent, S ;
Stearns, R ;
Colletti, A ;
Teffera, J ;
Tong, S ;
Fenyk-Melody, J ;
Owens, K ;
Levorse, D ;
Kim, P ;
Schmidt, JA ;
Mumford, RA .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (20) :2709-2713
[8]   Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent α4β1 integrin antagonists [J].
Müller, G ;
Albers, M ;
Fischer, R ;
Hessler, G ;
Lehmann, TE ;
Okigami, H ;
Tajimi, M ;
Bacon, K ;
Rölle, T .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (23) :3019-3021
[9]  
Porter J R, 2000, IDrugs, V3, P788
[10]   Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists [J].
Porter, JR ;
Archibald, SC ;
Brown, JA ;
Childs, K ;
Critchley, D ;
Head, JC ;
Hutchinson, B ;
Parton, TAH ;
Robinson, MK ;
Shock, A ;
Warrellow, GJ ;
Zomaya, A .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (12) :1591-1594