Structure–Activity studies for a novel series of tricyclic dihydropyrimidines as KATP channel openers (KCOs)

Synthesis, Characterization and Biological Evaluation of some Novel Pyrazolo[1,5-a]Pyrimidine Derivatives

“…Several compounds of this class display interesting antitrypanosomal [4] and antischistosomal activities [6]. They are used as HMG-CoA reductaseinhibitors [7], COX-2 selective inhibitors [8], 30,50-cyclic-AMP phosphodiesteraseinhibitors [9], CRF1 antagonists [10][11], selective peripheral benzodiazepine receptor ligands [12][13][14][15][16], potassium channel [17] and histamine-3 receptor ligands [18], CDK9 inhibitor [19]and antianxiety agents [20].…”

Dihydroazolopyrimidine Сrownophanes. Synthesis and Tuberculostatic Activity

“…[3,4] Среди дигидропиразоло[1,5-a] пиримидинов обнаружен ряд эффективных модулято-ров Ca-и K-каналов. [5][6][7][8][9][10] Триазоло[1,5-a]пиримидины оказались перспективными антагонистами аденозин A 2A рецептора при лечении болезни Паркинсона. [11] Не-которые дигидротриазоло [1,5-a]пиримидины проявили антиконвульсантную на уровне Карбамазепина [12] и анти-пролиферативную [13] клеточную активность.…”

“…-дибензо [13,14:8,9] [1,4,7]триоксацикло-тетрадецино [11,10-e]азоло [1,5-a] Azolo [1,5-a]pyrimidines are considered to be purine analogues and they form one of the most promising groups of biologically active compounds [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16] in medicinal chemistry. One of the strategies enhancing biochemical activity of azolo [1,5-a]pyrimidines is introduction of functional groups responsible for solubility and transport into their pharmacophore nucleus.…”

“…One of the strategies enhancing biochemical activity of azolo [1,5-a]pyrimidines is introduction of functional groups responsible for solubility and transport into their pharmacophore nucleus. [1,16] In this study, we wish to report ultrasound-and microwave-assisted one-pot cascade synthesis of macroheterocyclic 1-phenyl-2-(21-phenyl-10,11,13,14,20,20a-hexahydro-4aH-dibenzo-[13,14:8,9] [1,4,7] trioxacyclotetradecino [11,10-e]azolo [1,5-a]pyrimidin-20-yl)-1-ethanones. US and MV irradiation of the reaction mixtures under alkaline catalysis was found to promote a significant reduction of the reaction times (from 35 to 2 hours) and shift of the equilibrium in favor of 6,7-dihydroazolo [1,5-a]pyrimidine crownophanes in excellent yields (from 18 [24] to 75 %).…”

One Pot Multi Component Synthetic Approach towards the Formation of 1,2,4-Triazolo[1,5 a]Pyrimidine Analogues and their Biological Evaluation

“…There are literary data about the synthesis of triazolopyrimidines by treatment of 5-amino-1,2,4-triazole or 5-aminotetrazole with aldehydes and ethyl acetoacetate or cyclic -diketones [7][8][9][10][11]. The cyclocondensations were realized by heating of the starting materials in ethanol with catalytic amounts of hydrochloric acid under reflux conditions [7][8][9] or using DMF as solvent [10][11].…”