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Volumn 7, Issue 17, 1997, Pages 2205-2210

Design and synthesis of conformationally constrained arginal thrombin inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

ARGATROBAN; BMY 44621; EFEGATRAN; TETRAPEPTIDE; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

EID: 0030886277     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00403-4     Document Type: Article
Times cited : (21)

References (19)
  • 1
    • 0010576203 scopus 로고    scopus 로고
    • Orlando, FL, August 25-29, Abstr. 126
    • . Presented in part at the 212th ACS National Meeting, Orlando, FL, August 25-29, 1996; Abstr. 126.
    • (1996) 212th ACS National Meeting
  • 5
    • 0000363572 scopus 로고
    • Advances in the design and development of thrombin inhibitors
    • . Balasubramanian, B.N., Ed.; Advances in the Design and Development of Thrombin Inhibitors, Bioorg. Med. Chem., 1995, 3, 999.
    • (1995) Bioorg. Med. Chem. , vol.3 , pp. 999
    • Balasubramanian, B.N.1
  • 8
    • 0000148871 scopus 로고    scopus 로고
    • See references cited therein for a detailed discussion of reaction mechanism and NMR investigations
    • . Colombo, L.; Di Giacomo, M.; Belvisi, L.; Manzoni, L.; Scolastico, C.; Salimbeni, A. Gazz Chim. Ital., 1996, 12, 543. See references cited therein for a detailed discussion of reaction mechanism and NMR investigations.
    • (1996) Gazz Chim. Ital. , vol.12 , pp. 543
    • Colombo, L.1    Di Giacomo, M.2    Belvisi, L.3    Manzoni, L.4    Scolastico, C.5    Salimbeni, A.6
  • 12
    • 0342446224 scopus 로고    scopus 로고
    • note
    • . Minimum energy conformations of the bicyclic fragments were obtained using different molecular mechanics force fields (MM2*, MM3*, AMBER* implemented in the MacroModel/BatchMin V4.5 program) and then superimposed by rigid fit to the X-ray bound structure of PPACK. Only the results obtained using MM2* conformers are presented in the paper, but similar results can be derived with the other force fields.
  • 17
    • 0040676155 scopus 로고
    • Bergmeyer HU ed.; Academic Press, 1 edition
    • . Inhibition of human α-thrombin (0.02 NIH U/ml; Sigma Co., St.Louis, MO, USA) and of human plasmin (0.02 U/ml; Boehringer Mannheim, Milan, Italy) were tested with Chromozym TH and Chromozym PL substrates from Boehringer Mannheim, according to the protocols provided by the supplier. Bovine trypsin (Boehringer Mannheim) inhibition was assayed using benzoylarginine ethyl ester as substrate, according to Rick, W.; Trypsin, In Methods in Enzymatic Analysis, Bergmeyer HU ed.; Academic Press, 1 edition; 1963, 807.
    • (1963) Methods in Enzymatic Analysis , pp. 807
    • Rick, W.1    Trypsin2
  • 19
    • 0342446223 scopus 로고    scopus 로고
    • manuscript in preparation
    • . Cirillo, R. et al., manuscript in preparation.
    • Cirillo, R.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.