Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers
Publication
, Journal Article
Howson, W; Armstrong, W; Cassidy, K; Novelli, R; Tchorzewska, M; Jaxa-Chamiec, A; Dolle, R; Hallam, T; Leigh, B; Merritt, J; Moores, K; Rink, T
Published in: European Journal of Medicinal Chemistry
January 1, 1990
Receptor mediated calcium entry (RMCE) is a now recognised mechanism by which the influx of Ca2+ into cells can occur. Agents which antagonise or block this mechanism are expected to possess anti-platelet aggregation and anti-inflammatory activities. The first series of RMCE blockers based upon the lead compound SC 38249, has been prepared. Their synthesis, activity against ADP evoked Ca2+ signals in human platelets and their anti-platelet aggregation activity is described. A trend between the c log P of these compounds and their activity as inhibitors of Ca2+ influx into human platelets stimulated by ADP was observed. This SAR study led to a 40-fold increase in activity over the initial lead compound. © 1990.
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Published In
European Journal of Medicinal Chemistry
DOI
EISSN
1768-3254
ISSN
0223-5234
Publication Date
January 1, 1990
Volume
25
Issue
7
Start / End Page
595 / 602
Related Subject Headings
- Medicinal & Biomolecular Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 3214 Pharmacology and pharmaceutical sciences
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry
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Howson, W., Armstrong, W., Cassidy, K., Novelli, R., Tchorzewska, M., Jaxa-Chamiec, A., … Rink, T. (1990). Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers. European Journal of Medicinal Chemistry, 25(7), 595–602. https://doi.org/10.1016/0223-5234(90)90184-5
Howson, W., W. Armstrong, K. Cassidy, R. Novelli, M. Tchorzewska, A. Jaxa-Chamiec, R. Dolle, et al. “Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers.” European Journal of Medicinal Chemistry 25, no. 7 (January 1, 1990): 595–602. https://doi.org/10.1016/0223-5234(90)90184-5.
Howson W, Armstrong W, Cassidy K, Novelli R, Tchorzewska M, Jaxa-Chamiec A, et al. Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers. European Journal of Medicinal Chemistry. 1990 Jan 1;25(7):595–602.
Howson, W., et al. “Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers.” European Journal of Medicinal Chemistry, vol. 25, no. 7, Jan. 1990, pp. 595–602. Scopus, doi:10.1016/0223-5234(90)90184-5.
Howson W, Armstrong W, Cassidy K, Novelli R, Tchorzewska M, Jaxa-Chamiec A, Dolle R, Hallam T, Leigh B, Merritt J, Moores K, Rink T. Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers. European Journal of Medicinal Chemistry. 1990 Jan 1;25(7):595–602.
Published In
European Journal of Medicinal Chemistry
DOI
EISSN
1768-3254
ISSN
0223-5234
Publication Date
January 1, 1990
Volume
25
Issue
7
Start / End Page
595 / 602
Related Subject Headings
- Medicinal & Biomolecular Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 3214 Pharmacology and pharmaceutical sciences
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry