177583-27-6Relevant articles and documents
AMINE-DERIVATIVES HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY AND THE USES THEREOF
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Page/Page column 22, (2010/12/26)
This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl,Y is —S(O)n- wherein n is 1 or 2, or —CO—,R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl,X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, andZ is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.
Structure-activity studies of cyclic ketone inhibitors of the serine protease plasmin: Design, synthesis, and biological activity
Xue, Fengtian,Seto, Christopher T.
, p. 8467 - 8487 (2008/02/05)
Three series of cyclic ketone inhibitors were synthesized and evaluated against the serine protease plasmin. Peptide inhibitors that incorporated 3-oxotetrahydrofuran and 3-oxotetrahydrothiophene 1,1-dioxide groups had the highest activities. Alkylamino substituents, which were designed to bind in the S1 subsite of plasmin, were attached to the inhibitors. Compounds 5c and 5g, which incorporated 6-aminohexyl substituents, were found to be optimal and demonstrated IC50 values in the low micromolar range. Incorporating conformationally constrained peptide segments into the inhibitors did not improve their activities.
