%0 Journal Article %1 Pastorin2005 %A Pastorin, G. %A Bolcato, C. %A Cacciari, B. %A Kachler, S. %A Klotz, K. N. %A Montopoli, C. %A Moro, S. %A Spalluto, G. %D 2005 %J Farmaco %K & *Drug *Purines/chemical A1/antagonists A2A/antagonists A2B/antagonists A3/*antagonists Adenosine Binding Conformation Design Drug Evaluation, Humans Models, Molecular Preclinical Protein Rats Relationship Secondary Sites Structure Structure, Structure-Activity inhibitors synthesis/chemistry/pharmacology Receptor %N 8 %P 643-51 %T Synthesis, biological and modeling studies of 1,3-di-n-propyl-2,4-dioxo-6-methyl-8-(substituted) 1,2,3,4-tetrahydro 1,2,4-triazolo 3,4-f-purines as adenosine receptor antagonists %U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15961085 %V 60 %X A new series of potential adenosine receptor antagonists with a 1,2,4-triazolo-3,4-f-purine structure bearing at the 1 and 3 position n-propyl groups have been synthesized, and their affinities at the four human adenosine receptor subtypes (A(1), A(2A), A(2B) and A(3)) have been evaluated. In this case the presence of n-propyl groups seems to induce potency at the A(2A) and A(3) adenosine receptor subtypes as opposed to our previously reported series bearing methyl substituents at the 1 and 3 positions. In particular the non-acylated derivative 17 showed affinity at these two receptor subtypes in the micromolar range. Indeed, preliminary molecular modeling investigations according to the experimental binding data indicate a modest steric and electrostatic antagonist-receptor complementarity.

@article{Pastorin2005, abstract = {A new series of potential adenosine receptor antagonists with a [1,2,4]-triazolo-[3,4-f]-purine structure bearing at the 1 and 3 position n-propyl groups have been synthesized, and their affinities at the four human adenosine receptor subtypes (A(1), A(2A), A(2B) and A(3)) have been evaluated. In this case the presence of n-propyl groups seems to induce potency at the A(2A) and A(3) adenosine receptor subtypes as opposed to our previously reported series bearing methyl substituents at the 1 and 3 positions. In particular the non-acylated derivative 17 showed affinity at these two receptor subtypes in the micromolar range. Indeed, preliminary molecular modeling investigations according to the experimental binding data indicate a modest steric and electrostatic antagonist-receptor complementarity.}, added-at = {2010-12-14T18:12:02.000+0100}, author = {Pastorin, G. and Bolcato, C. and Cacciari, B. and Kachler, S. and Klotz, K. N. and Montopoli, C. and Moro, S. and Spalluto, G.}, biburl = {https://www.bibsonomy.org/bibtex/2ffae8adc25f63b281bf174b9094534d6/pharmawuerz}, endnotereftype = {Journal Article}, interhash = {1a310863144732f454ae9b06030c1df0}, intrahash = {ffae8adc25f63b281bf174b9094534d6}, issn = {0014-827X (Print) 0014-827X (Linking)}, journal = {Farmaco}, keywords = {& *Drug *Purines/chemical A1/antagonists A2A/antagonists A2B/antagonists A3/*antagonists Adenosine Binding Conformation Design Drug Evaluation, Humans Models, Molecular Preclinical Protein Rats Relationship Secondary Sites Structure Structure, Structure-Activity inhibitors synthesis/chemistry/pharmacology Receptor}, month = Aug, note = {Pastorin, G Bolcato, C Cacciari, B Kachler, S Klotz, K-N Montopoli, C Moro, S Spalluto, G Research Support, Non-U.S. Gov't France Farmaco (Societa chimica italiana : 1989) Farmaco. 2005 Aug;60(8):643-51.}, number = 8, pages = {643-51}, shorttitle = {Synthesis, biological and modeling studies of 1,3-di-n-propyl-2,4-dioxo-6-methyl-8-(substituted) 1,2,3,4-tetrahydro [1,2,4]-triazolo [3,4-f]-purines as adenosine receptor antagonists}, timestamp = {2010-12-14T18:20:21.000+0100}, title = {Synthesis, biological and modeling studies of 1,3-di-n-propyl-2,4-dioxo-6-methyl-8-(substituted) 1,2,3,4-tetrahydro [1,2,4]-triazolo [3,4-f]-purines as adenosine receptor antagonists}, url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15961085}, volume = 60, year = 2005 }