7255-89-2Relevant articles and documents
From hit to lead. Combining two complementary methods for focused library design. Application to μ opiate ligands
Poulain,Horvath,Bonnet,Eckhoff,Chapelain,Bodinier,Déprez
, p. 3378 - 3390 (2007/10/03)
Compound 1 obtained by random screening and displaying a micromolar activity on the μ opiate receptor was chosen as a starting point for optimization. Two complementary concepts of similarity were used for the design of analogues and compared. These are based, respectively, on a computer-aided comparison of pharmacophoric patterns and on topological similarity. The structure-activity relationships are discussed in light of both similarity concepts. Compound 40, an N-methyl-3-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decyl)acetamide derivative, designed by combining the structure-activity relationships enlightened by each method, has a subnanomolar affinity for μ (h) receptor (IC50=0.9 nM). It is a promising lead, allowing the design of a new series of analogues substituted at the N-3 of the spirocycle moiety.
Dipeptides which promote release of growth hormone
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, (2008/06/13)
Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. STR1