C2md00288d 379..384
نویسندگان
چکیده
The inhibition of the soluble epoxide hydrolase (sEH) is a promising new therapy in the treatment of cardiovascular, inflammation and other disorders. A piperazino functionality as the tertiary pharmacophore remarkably improved the drug-like profile of the 1,3-disubstituted urea sEH inhibitors. However, the potency was more dependent on the overall best balance of the hydrophilicity and lipophilicity. Based on the sEH-inhibitor complex structure, further structural optimization on the piperazino-containing 1,3-disubstituted urea scaffold was conducted for an improved potency. The 1-adamantylacetamide and para-phenylcarbonyl group were identified to be an optimal primary pharmacophore and secondary pharmacophore motif, respectively, generating sub-nanomolar sEH inhibitors with favorable water solubility.
منابع مشابه
The Effect of Environment on Variegation Patterns in Maize Pericarp.
PAGE Statement of the problem. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 372 Materials and methods. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 373 Localities in which plants were grown.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ....
متن کاملDrug Safety 2009;
. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 379 1. Literature Search Methodology . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 380 1.1 Search Strategy . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ...
متن کاملSurvey of numerical techniques for grouping.
[This corrects the article on p. 379 in vol. 35.][This corrects the article on p. 381 in vol. 35.][This corrects the article on p. 384 in vol. 35.][This corrects the article on p. 387 in vol. 35.][This corrects the article on p. 388 in vol. 35.][This corrects the article on p. 389 in vol. 35.].
متن کاملFirst draft prepared
Explanation.................................................................................................... 333 Evaluation for acceptable daily intake .......................................................... 333 Biochemical aspects ................................................................................ 333 Absorption, distribution and excretion ......................................
متن کامل