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Volumn 14, Issue 20, 2006, Pages 6807-6819

Arylamine based cathepsin K inhibitors: Investigating P3 heterocyclic substituents

Author keywords

Cathepsin K; Heterocyclic substituent; Inhibitor; SAR study

Indexed keywords

1 (BIPHENYL 3 YLAMINO) N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] CYCLOHEXANECARBOXAMIDE; [4 [[2 [(N BIPHENYL 3 YL LEUCYL)AMINO]BUTYL]AMINO]PHENOXY]ACETIC ACID 2 HYDROCHLORIDE; [4 [[2 [[N (2 OXO 6 PHENYL 2H PYRAN 4 YL)LEUCYL]AMINO]BUTYL]AMINO]PHENOXY] ACETIC ACID 2 HYDROCHLORIDE; [4 [[2 [[N (5 PHENYLISOXAZOL 3 YL)LEUCYL]AMINO]BUTYL]AMINO]PHENOXY]ACETIC ACID 2 HYDROCHLORIDE; [4 [[2 [[N (MORPHOLIN 4 YLCARBONYL)LEUCYL]AMINO]BUTYL]AMINO]PHENOXY]ACETIC ACID 2 HYDROCHLORIDE; AROMATIC AMINE; CATHEPSIN K INHIBITOR; N 1 [1 [[(4 METHOXYPHENYL)AMINO]METHYL]PROPYL] N 2 (2 OXO 6 PHENYL 2H PYRAN 4 YL)LEUCINAMIDE; N 1 [1 [[(4 METHOXYPHENYL)AMINO]METHYL]PROPYL] N 2 (5 PHENYLISOXAZOL 3 YL)LEUCINAMIDE; N 1 [1 [[(4 METHOXYPHENYL)AMINO]METHYL]PROPYL] N 2 (MORPHOLIN 4 YLCARBONYL)LEUCINAMIDE; N 2 1,1 BIPHENYL 3 YL N 1 1 [[[(4 METHOXYPHENYL)AMINO]METHYL]PROPYL] LEUCINAMIDE; N 2 BIPHENYL 3 YL N 1 [[(4 METHOXYPHENYL)AMINO]METHYL]LEUCINAMIDE; N [1 [[[4 (BENZYLOXY)PHENYL]AMINO]METHYL]PROPYL] N 2 (2 OXO 6 PHENYL 2H PYRAN 4 YL)LEUCINAMIDE; N [1 [[[4 (BENZYLOXY)PHENYL]AMINO]METHYL]PROPYL] N 2 (5 PHENYLISOXAZOL 3 YL)LEUCINAMIDE; N [1 [[[4 (BENZYLOXY)PHENYL]AMINO]METHYL]PROPYL] N 2 (MORPHOLIN 4 YLCARBONYL)LEUCINAMIDE; N [1 [[[4 (BENZYLOXY)PHENYL]AMINO]METHYL]PROPYL] N 2 BIPHENYL 3 YL LEUCINAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 (1 NAPHTHYLAMINO) CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(2 OXO 2H CHROMEN 4 YL)AMINO]CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(2 OXO 6 PHENYL 2H PYRAN 4 YL)AMINO]CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(3 PYRIDIN 2 YLPHENYL)AMINO] CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(3 PYRIDIN 3 YLPHENYL)AMINO] CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(3 PYRIDIN 4 YLPHENYL)AMINO] CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(4 PHENYLPYRIDIN 2 YL)AMINO]CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] 1 [(6 PHENYLPYRIDIN 2 YL)AMINO]CYCLOHEXANECARBOXAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] N 2 (2 OXO 6 PHENYL 2H PYRAN 4 YL)LEUCINAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] N 2 (5 PHENYL 1H PYRAZOL 3 YL)LEUCINAMIDE; N [2 [(4 METHOXYPHENYL)AMINO]ETHYL] N 2 (5 PHENYLISOXAZOL 3 YL)LEUCINAMIDE; UNCLASSIFIED DRUG;

EID: 33748095763     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2006.06.031     Document Type: Article
Times cited : (12)

References (22)
  • 6
    • 0031024171 scopus 로고    scopus 로고
    • A moderate lipophilicity is preferred for obtaining a good pharmacokinetics, see: and references cited therein
    • A moderate lipophilicity is preferred for obtaining a good pharmacokinetics, see:. Lipinski C.A., Lombardo F., Dominy B.W., and Feeney P.J. Adv. Drug Delivery Rev. 23 (1997) 3 and references cited therein
    • (1997) Adv. Drug Delivery Rev. , vol.23 , pp. 3
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4
  • 18
    • 0030026637 scopus 로고    scopus 로고
    • Purified procathepsin K is efficiently activated at lower pH, such as pH 4.0. In addition, the activity of mature cathepsin K at pH 3.8 was around 40% when compared at pH 6.0 using Cbz-Phe-Arg-AMC as a substrate. Therefore, the assays were carried out against recombinant human cathepsin K at pH 3.8. See:
    • Purified procathepsin K is efficiently activated at lower pH, such as pH 4.0. In addition, the activity of mature cathepsin K at pH 3.8 was around 40% when compared at pH 6.0 using Cbz-Phe-Arg-AMC as a substrate. Therefore, the assays were carried out against recombinant human cathepsin K at pH 3.8. See:. Brömme D., Okamoto K., Wang B.B., and Biroc S. J. Biol. Chem. 271 (1996) 2126
    • (1996) J. Biol. Chem. , vol.271 , pp. 2126
    • Brömme, D.1    Okamoto, K.2    Wang, B.B.3    Biroc, S.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.