15515-58-9Relevant articles and documents
Elucidation of structural elements for selectivity across monoamine transporters: Novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues
Okunola-Bakare, Oluyomi M.,Cao, Jianjing,Kopajtic, Theresa,Katz, Jonathan L.,Loland, Claus J.,Shi, Lei,Newman, Amy Hauck
, p. 1000 - 1013 (2014/03/21)
2-[(Diphenylmethyl)sulfinyl]acetamide (modafinil, (±)-1) is a unique dopamine uptake inhibitor that binds the dopamine transporter (DAT) differently than cocaine and may have potential for the treatment of psychostimulant abuse. To further investigate structural requirements for this divergent binding mode, novel thio- and sulfinylacetamide and ethanamine analogues of (±)-1 were synthesized wherein (1) the diphenyl rings were substituted with methyl, trifluoromethyl, and halogen substituents and (2) substituents were added to the terminal amide/amine nitrogen. Halogen substitution of the diphenyl rings of (±)-1 gave several amide analogues with improved binding affinity for DAT and robust selectivity over the serotonin transporter (SERT), whereas affinity improved at SERT over DAT for the p-halo-substituted amine analogues. Molecular docking studies, using a subset of analogues with DAT and SERT homology models, and functional data obtained with DAT (A480T) and SERT (T497A) mutants defined a role for TM10 in the substrate/inhibitor S1 binding sites of DAT and SERT.
Synthesis, radiolabelling and biological evaluation of terminal oxamide derivatives of mercaptoacetyltriglycine
Okarvi,Torfs,Adriaens,Verbruggen
, p. 407 - 421 (2007/10/03)
99mTc-MAG3 is widely used in clinical nuclear medicine as a potential replacement of 131I-OIH for renal function studies. The terminal carbonylglycine in the MAG3 backbone is assumed to be essential for maintain
Benzhydryl derivatives having calmodulin inhibitor properties
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, (2008/06/13)
The invention relates to a benzhydryl derivative having the formula STR1 wherein each of the groups R1, R2, and R3 represents one to four substituents independently selected from the group consisting of hydrogen, lower alkyl, halogen, and CF3, and at least one of the groups R1, R2, and R3 is halogen or CF3 ; R4 represents hydrogen or methyl; n is 2, 3, or 4; m is 1, 2, or 3; and X represents O or S; or its pharmaceutically acceptable salts. The benzhydryl derivative of the invention can be used to treat patients who are suffering from diseases which are influenced by calmodulin.