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Volumn 7, Issue 3, 1997, Pages 331-336

Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2-P3 bicyclic lactam moiety

Author keywords

[No Author keywords available]

Indexed keywords

ARGININE DERIVATIVE; BLOOD CLOTTING FACTOR 10A; CVS 1862; SERINE PROTEINASE INHIBITOR; THROMBIN; TISSUE PLASMINOGEN ACTIVATOR; TRYPSIN; UNCLASSIFIED DRUG;

EID: 0031552086     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00004-8     Document Type: Article
Times cited : (42)

References (61)
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    • (a) Dedicated with genuine affection and respect to Professor Madeleine M. Joullie, Department of Chemistry, University of Pennsylvania, on the occasion of her 70th birthday (b) Presented in part at the Gordon Research Conference on Heterocyclic Chemistry, New Hampshire, July 7-12, 1996
    • 1. (a) Dedicated with genuine affection and respect to Professor Madeleine M. Joullie, Department of Chemistry, University of Pennsylvania, on the occasion of her 70th birthday. (b) Presented in part at the Gordon Research Conference on Heterocyclic Chemistry, New Hampshire, July 7-12, 1996.
  • 3
    • 0011386164 scopus 로고
    • J. B. Lippincott: Philadelphia
    • 2. (a) Colman, R. W.; Marder, V. J.; Salzman, E.; W. Hirsch, J. In Hemostasis and Thrombosis: Basic Principles and Clinical Practice; 3rd ed.; Colman, R. W.; Hirsch, J.; Marder, V. J.; Salzman, E. W.; Eds.; J. B. Lippincott: Philadelphia, 1994; 3.
    • (1994) , pp. 3
    • Colman, R.W.1    Hirsch, J.2    Marder, V.J.3    Salzman, E.W.4
  • 10
    • 77956798630 scopus 로고
    • Bristol, J. A., Ed.; Academic Press: San Diego
    • 4. (a) Scarborough, R. M. In Ann. Rep. Med. Chem. Bristol, J. A., Ed.; Academic Press: San Diego, 1995; vol. 30, 71.
    • (1995) Ann. Rep. Med. Chem. , vol.30 , pp. 71
    • Scarborough, R.M.1
  • 13
    • 0000363572 scopus 로고
    • Advances in the design and development of thrombin inhibitors
    • 1 see: Balasubramanian, B. N., Ed.; Advances in the Design and Development of Thrombin Inhibitors. Bioorg. Med. Chem. 1995, 3, 999-1156.
    • (1995) Bioorg. Med. Chem. , vol.3 , pp. 999-1156
    • Balasubramanian, B.N.1
  • 48
    • 77957226741 scopus 로고
    • Allen, R. C., Ed.; Academic Press: San Diego, Chapter 26
    • 16. (a) Morgan, B. A.; Gainor, J. A. In Ann. Rep. Med. Chem. Allen, R. C., Ed.; Academic Press: San Diego, 1989; vol. 24, Chapter 26, pp 243-252.
    • (1989) Ann. Rep. Med. Chem. , vol.24 , pp. 243-252
    • Morgan, B.A.1    Gainor, J.A.2
  • 49
    • 0011478438 scopus 로고
    • Hansch, C.; Sammes, P. G.; Taylor, J. B., Eds.; Pergamon Press: Oxford, Chapter 8.
    • (b) Rich, D. H. in Comprehensive Medicinal Chemistry; Hansch, C.; Sammes, P. G.; Taylor, J. B., Eds.; Pergamon Press: Oxford, 1990; Vol. 2, Chapter 8.
    • (1990) Comprehensive Medicinal Chemistry , vol.2
    • Rich, D.H.1
  • 51
    • 0011477638 scopus 로고    scopus 로고
    • All new compounds were characterized by full spectroscopic (NMR, IR, low/high resolution MS) data. Yields refer to spectroscopically and chromatographically homogenous (≥95% by HPLC, TLC) materials
    • 17. All new compounds were characterized by full spectroscopic (NMR, IR, low/high resolution MS) data. Yields refer to spectroscopically and chromatographically homogenous (≥95% by HPLC, TLC) materials.
  • 54
    • 0011385884 scopus 로고    scopus 로고
    • The intermediate glutamic acid derivative 6 is commercially available, however its very high price led us to develop the protocol described, which is operationally very convenient and proceeds from reasonably priced starting material 5
    • 19. The intermediate glutamic acid derivative 6 is commercially available, however its very high price led us to develop the protocol described, which is operationally very convenient and proceeds from reasonably priced starting material 5.
  • 61
    • 0011440598 scopus 로고    scopus 로고
    • The in vitro enzyme assays were performed according to the protocols described in reference 10a
    • 22. The in vitro enzyme assays were performed according to the protocols described in reference 10a.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.