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Volumn 6, Issue 6, 1996, Pages 377-383

Preparation of Argatroban Analog Thrombin Inhibitors with Reduced Basic Guanidine Moiety, and Studies of Their Cell Permeability and Antithrombotic Activities

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EID: 0000616292     PISSN: 10542523     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article
Times cited : (15)

References (31)
  • 7
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    • Patent Appl. WO 92/16549, Oct.1, 1992
    • (a) Sturzebecher, J.; Wikstroem, P. Patent Appl. WO 92/16549, Oct.1, 1992.
    • Sturzebecher, J.1    Wikstroem, P.2
  • 8
    • 1842616740 scopus 로고    scopus 로고
    • European Patent Appl. 669317A1, Aug. 30, 1995
    • (b) Onshima, O.; Iwase, N.; Sugiyama, S. European Patent Appl. 669317A1, Aug. 30, 1995.
    • Onshima, O.1    Iwase, N.2    Sugiyama, S.3
  • 9
    • 0001077363 scopus 로고
    • pKa of L-canavanine : 2.35, 7.01, 9.22 Boyar, A.; Marsh, R. E. J. Am. Chem. Soc., 1982, 104, 1995. Tomiyama, T. J. Biol. Chem.,1935, 111, 45-49. pKa of L-arginine : 2.18, 9.09, 13.2 The Merck Index; 10th ed.; Windholz, M. Ed.; Merck & Co., Inc., 1983; p797.
    • (1982) J. Am. Chem. Soc. , vol.104 , pp. 1995
    • Boyar, A.1    Marsh, R.E.2
  • 10
    • 0001077363 scopus 로고
    • pKa of L-canavanine : 2.35, 7.01, 9.22 Boyar, A.; Marsh, R. E. J. Am. Chem. Soc., 1982, 104, 1995. Tomiyama, T. J. Biol. Chem.,1935, 111, 45-49. pKa of L-arginine : 2.18, 9.09, 13.2 The Merck Index; 10th ed.; Windholz, M. Ed.; Merck & Co., Inc., 1983; p797.
    • (1935) J. Biol. Chem. , vol.111 , pp. 45-49
    • Tomiyama, T.1
  • 11
    • 0001077363 scopus 로고
    • Merck & Co., Inc.
    • pKa of L-canavanine : 2.35, 7.01, 9.22 Boyar, A.; Marsh, R. E. J. Am. Chem. Soc., 1982, 104, 1995. Tomiyama, T. J. Biol. Chem.,1935, 111, 45-49. pKa of L-arginine : 2.18, 9.09, 13.2 The Merck Index; 10th ed.; Windholz, M. Ed.; Merck & Co., Inc., 1983; p797.
    • (1983) The Merck Index; 10th Ed. , pp. 797
    • Windholz, M.1
  • 12
    • 0027359371 scopus 로고
    • (a) pKa of 4,4-Difluoro-L-arginine : 1.4, 8.1, 11.2 , Kim, K. S.; Qian, L. Tetrhedron Lett.. 1993, 34, 7195.
    • (1993) Tetrhedron Lett.. , vol.34 , pp. 7195
    • Kim, K.S.1    Qian, L.2
  • 13
    • 1842512286 scopus 로고    scopus 로고
    • pKa of compound 4 : 8.50, 9.15, 10.76 (for sulfonamide proton)
    • (b) pKa of compound 4 : 8.50, 9.15, 10.76 (for sulfonamide proton).
  • 27
    • 1842564724 scopus 로고    scopus 로고
    • note
    • 50 determinations). The enzymatic reaction was started with 10 μL of 3 mM S-2238 substrate and continued at room temperature. The change in optical density was measured at 405 nm. A kinetic microplate reader (Molecular Devices Corporation Vmax) was used to measure the change in optical density over time.
  • 28
    • 1842616737 scopus 로고    scopus 로고
    • note
    • 2 asphyxiation. Survival of >20% in any group was considered significant, and the dose by a particular route producing 50% survival was calculated by log-linear interpolation.
  • 31
    • 0019511561 scopus 로고
    • N-Hydroxyguanidine in Neosaxitoxin being easily biotransformed to guanidine in shell fish (Shimizu, Y; Yoshioka, Y. Science, 1981, 212,547) it deserves further metabolic studies in human as a potential prodrug of arginine containing molecules.
    • (1981) Science , vol.212 , pp. 547
    • Shimizu, Y.1    Yoshioka, Y.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.