58481-23-5Relevant academic research and scientific papers
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors
Wang, Yuguang,Chackalamannil, Samuel,Hu, Zhiyong,Boyle, Craig D.,Lankin, Claire M.,Xia, Yan,Xu, Ruo,Asberom, Theodros,Pissarnitski, Dmitri,Stamford, Andrew W.,Greenlee, William J.,Skell, Jeffrey,Kurowski, Stanley,Vemulapalli, Subbarao,Palamanda, Jairam,Chintala, Madhu,Wu, Ping,Myers, Joyce,Wang, Peng
, p. 3149 - 3152 (2007/10/03)
We have discovered potent and selective xanthine PDE5 inhibitors. Compound 25 (PDE5 IC50=0.6 nM, PDE6/PDE5=101) demonstrated similar functional efficacy and PK profile to Sildenafil (PDE5 IC50=3.5 nM, PDE6/PDE5=7).
Structure-activity relationships in a series of xanthine derivatives with antibronchoconstrictory and bronchodilatory activities
Merlos,Gomez,Vericat,Bartroli,Garcia-Rafanell,Forn
, p. 653 - 658 (2007/10/02)
Thirty-one 1,3,7,8-substituted xanthine derivatives have been synthesized and evaluated for bronchodilator and anti-bronchoconstrictory activities in in vitro tracheal relaxation and in vivo bronchospasm inhibition models. Activity tests have been complemented with phosphodiesterase inhibition and toxicological data. Structure-activity relationships are discussed. Compound 21 (1,3-diisobutyl-8-methylxanthine) has been selected for further pharmacological development because of its good activity profile and favourable therapeutic index, which is 14- and 38-fold greater than that of theophylline and IBMX, respectively.
