Synthesis, biological activity and molecular modelling of new trisubstituted 8-azaadenines with high affinity for A1 adenosine receptors

Synthesis of 2Н-azolo[1,5-а][1,2,3]triazolo[4,5-е]pyrimidines

“…[1][2][3][4][5] Recent studies of biological activity mechanisms showed that 8-azapurines act as inhibitors of certain enzymesadenosine deaminase, phosphodiesterase, 6-8 as well as adenosine receptor antagonists. [9][10][11] Another type of azoloazines, [1,2,4]triazolo[1,5-a]-pyrimidines, have also shown various biological activity, primarily as antiviral agents. [12][13][14][15][16] The combination of both aforementioned azoloazine moieties in a single molecular structure has been once reported in the literature, 17 but the compound itself has not been characterized.…”

A QSAR Study for Modeling of 8-Azaadenine Analogues Proposed as A1 Adenosine Receptor Antagonists Using Genetic Algorithm Coupling Adaptive Neuro-Fuzzy Inference System (ANFIS)

“…38 The affinity of an antagonist for its binding site (Ki), i.e. its ability to bind to a receptor, will determine the duration of the inhibition of agonist activity.…”

“…presented for the prediction of some 8-azaadenine analogues proposed as A1 adenosine receptor antagonists synthesized by Giorgi et al 38 It has been demonstrated that ANFIS is a useful tool for QSAR modeling, comparable to the multiple linear regression (MLR) and radial basis function (RBF) methods. Finally, the accuracy of the proposed model was illustrated using Leave One Out, heuristic and randomized techniques.…”

“…Some of these compounds were shown to be very effective, because their affinity (Ki values) was found in the range of nanomolar units. [30][31][32][33][34][35][36][37][38] A number of models of QSAR have been developed about the QSAR modeling of A adenosine receptors.…”

Microwave assisted synthesis of annelated benzosuberone as new penta-heterocyclic ring systems

“…1 The inhibition of the farnesyl protein transferase, a novel approach to antitumour therapy, is based on compounds such as piperazinyl substituted cycloheptapyridines. 2 Various derivatives of 1,2,4-triazolopyrimidine have high affinity for binding with A 1 adenosine receptors, 3 and the others can be used as calcium-channel-blocking vasodilators, antihypertensive, cardiovascular, anxiolytic activities and photographic materials. [4][5][6][7] Thiazolo[3,2-a]pyrimidine derivatives have been ascertained as a new type of acetyl cholinesterase inhibitor for the treatment of Alzheimer disease.…”