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Bioorg Med Chem ; 23(13): 3192-207, 2015 Jul 01.
Article in English | MEDLINE | ID: mdl-25982416

ABSTRACT

In order to probe the S1 and S1' mammalian aminopeptidase N subsites, racemic 1- or 4-substituted 7-aminobenzocyclohepten-6-one derivatives were synthesized and evaluated for their ability to inhibit mammalian aminopeptidase N. We focused on improving the physicochemical and ADME properties of this series by targeting lipophilicity and LELP score. Some 4-heteroaryl substituted analogues displayed reduced lipophilicity and enhanced inhibition potency with Ki values in the nanomolar range.


Subject(s)
Aminobenzoates/chemical synthesis , Benzocycloheptenes/chemical synthesis , CD13 Antigens/antagonists & inhibitors , Protease Inhibitors/chemical synthesis , Aminobenzoates/chemistry , Animals , Benzocycloheptenes/chemistry , CD13 Antigens/chemistry , CD13 Antigens/isolation & purification , Kidney/chemistry , Kidney/enzymology , Molecular Docking Simulation , Molecular Structure , Protease Inhibitors/chemistry , Stereoisomerism , Structure-Activity Relationship , Swine , Thermodynamics
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