Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin

Authors
Pass, M Bolton, RE Coote, SJ Finch, H Hindley, S Lowdon, A McDonald, E McLaren, J Owen, M Pegg, NA Mooney, CJ Tang, CM Parry, S Patel, C
Citation
M. Pass et al., Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin, BIOORG MED, 9(3), 1999, pp. 431-436
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
3
Year of publication
1999
Pages
431 - 436
Database
ISI
SICI code
0960-894X(19990208)9:3<431:S[TILA>2.0.ZU;2-Q
Abstract
Synthesis of trans-fused lactones containing; the indane nucleus has result ed in a series of potent acylating inhibitors of thrombin. As an er;ample c ompound Ile has an apparent second order rate constant of 11x10(6) M(-1)sec (-1) for the inhibition of thrombin. The anticoagulant activity of these co mpounds is discussed. (C) 1999 Elsevier Science Ltd. All rights reserved.