?Searching for novel antagonists of adenosine A1 receptors among azolo[1,5-a]pyrimidine nitro derivatives

Introduction: Ligands of adenosine A1Rs are potential candidates for the development drugs treatment paroxysmal supraventricular tachycardia, angina pectoris, hypertriglyceridemia, type 2 diabetes mellitus, neuropathic pain, and heart failure. At same time, there is a deficiency that can regulate functions A1 receptors. A number A1-antagonists at various stages clinical trials; other not very selective or characterized by an insufficient breadth their therapeutic action. Therefore, search new medicinal compounds prevention A1-depended diseases among nitro derivatives tetrazolo[1,5-a]pyrimidine 1,2,4-triazolo[1,5-a]pyrimidine scientific interest.
 Materials methods: The active was carried out in silico vitro methods. first stage, computer forecast A1-antagonistic activity using Microcosm BioS software. second prediction results were verified model isolated mouse atria.
 Results discussion: Based on method maximum similarity to standards, most III, VIII, XVII selected. After testing atria method, compound VIII A1-blocking effect concentration 10 ?mol/L.
 Conclusion: promising with identified; it derivative under code VIII. It interest us further in-depth study its pharmacological properties.