Synthesis and evaluation of 4-substituted benzylamine derivatives as β-tryptase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 11, 2006, Pages 2986-2990

  Miyazaki, Yutaka ^a   Kato, Yutaka ^a   Manabe, Tadashi ^a   Shimada, Hiroyasu ^a   Mizuno, Masashi ^a   Egusa, Takayuki ^a   Ohkouchi, Munetaka ^a   Shiromizu, Ikuya ^a   Matsusue, Tomokazu ^a   Yamamoto, Ichiro ^a  

^a MOCHIDA PHARMACEUTICAL CO   (Japan)

Author keywords

Tryptase; Serine protease

Indexed keywords

AMIDINE; BENZYLAMINE DERIVATIVE; GUANIDINE DERIVATIVE; M 58539; SERINE PROTEINASE; TRYPTASE INHIBITOR; UNCLASSIFIED DRUG; ZINC;

ARTICLE; DRUG ACTIVITY; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; IC 50; MOLECULAR WEIGHT; SUBSTITUTION REACTION;

BENZYLAMINES; IONS; MOLECULAR STRUCTURE; NAPHTHALENES; SERINE ENDOPEPTIDASES; SERINE PROTEINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPTASES; ZINC;

EID: 33646059854     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.02.064     Document Type: Article

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19. 3) δ: 7.20 (2H, d, J = 8 Hz), 7.13 (2H, d, J = 8 Hz), 4.79 (1H, s), 4.28 (2H, d, J = 5 Hz), 3.33-3.10 (4H, m), 2.80 (2H, d, J = 7 Hz), 2.58 (2H, d, J = 8 Hz), 1.93-1.75 (2H, m), 1.46 (9H, s), 1.44 (9H, s).
20. 6) δ: 8.92 (2H, s), 8.61 (1H, d, J = 2 Hz), 8.35-8.15 (3H, m), 8.15-8.05 (1H, m), 8.12 (1H, d, J = 9 Hz), 7.90 (1H, dd, J = 2, 9 Hz), 7.40 (2H, d, J = 8 Hz), 7.26 (2H, d, J = 8 Hz), 4.05-3.90 (2H, m), 3.15-2.80 (6H, m), 2.87 (3H, s), 2.64 (2H, t, J = 8 Hz), 1.95-1.80 (2H, m).