89977-78-6Relevant academic research and scientific papers
Design and synthesis of 1,2,4-triazolo[1,5-a]pyrimidine derivatives as PDE 4B inhibitors endowed with bronchodilator activity
Abd El-Aleam, Rehab H.,George, Riham F.,Lee, Kevin J.,Keeton, Adam B.,Piazza, Gary A.,Kamel, Amr A.,El-Daly, Mahmoud E.,Hassan, Ghaneya S.,Abdel-Rahman, Hamdy M.
, (2019)
A series of 1,2,4-triazolo[1,5-a]pyrimidine derivatives was designed, synthesized, and screened for their phosphodiesterase (PDE 4B) inhibitory activity and bronchodilation ability. Compound 7e showed 41.80% PDE 4B inhibition at 10 μM. Eight compounds were screened for their bronchodilator activity, where compounds 7f and 7e elicited promising bronchodilator activity with EC50 values of 18.6 and 57.1 μM, respectively, compared to theophylline (EC50 = 425 μM). Molecular docking at the PDE 4B active site revealed a binding mode and docking scores comparable to those of a reference ligand, consistent with their PDE 4B inhibition activity.
Synthesis of 1,2,4-triazolo[1,5-a]pyrimidine derivatives: Antimicrobial activity, DNA Gyrase inhibition and molecular docking
Abd El-Aleam, Rehab H.,George, Riham F.,Hassan, Ghaneya S.,Abdel-Rahman, Hamdy M.
, (2020)
A series of 1,2,4-triazolo[1,5-a]pyrimidine derivatives was designed, synthesized and screened for their antibacterial and antifungal activities as well as their safety profile. Compounds 2b, 3a, 6b, 8b, 8c, 8h, 9a,b, 10b, 11a,b and 12a,b showed high activity against Gram-positive and Gram-negative bacteria with MIC values ranging from 0.25 to 2.0 μg/mL. Many compounds were safe with no cytotoxicity against human embryonic kidney and red blood cells at concentration up to 32 μg/mL. Moreover, compound 9a showed the highest inhibitory activity against DNA Gyrase with IC50 = 0.68 μM compared to ciprofloxacin IC50 = 0.85 μM. Molecular docking at DNA Gyrase active site revealed binding mode and docking scores comparable to that of ciprofloxacin confirming their antibacterial activity via DNA Gyrase inhibition.
Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists
Aghazadeh Tabrizi, Mojgan,Baraldi, Pier Giovanni,Ruggiero, Emanuela,Saponaro, Giulia,Baraldi, Stefania,Poli, Giulio,Tuccinardi, Tiziano,Ravani, Annalisa,Vincenzi, Fabrizio,Borea, Pier Andrea,Varani, Katia
, p. 11 - 27 (2016/03/04)
CB2 cannabinoid receptor ligands are known to be therapeutically important for the treatment of numerous diseases. Recently, we have identified the heteroaryl-4-oxopyridine/7-oxopyrimidine derivatives as highly potent and selective CB2 receptor ligands, showing that the pharmakodynamics of the new compounds was controlled by the nature of the heterocycle core. In this paper we describe the synthesis and biological evaluation of 7-oxo-4-pentyl-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxamide derivatives that led to the identification of novel CB2 receptor inverse agonists. Cyclic AMP experiments on CB2 receptors expressed in CHO cells revealed that introduction of structural modifications at position 2 of triazolopyrimidine template changes the functional activity from partial to inverse agonism. The molecular docking analysis of the novel structures is reported.
Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB2 cannabinoid receptor partial agonists
Aghazadeh Tabrizi, Mojgan,Baraldi, Pier Giovanni,Saponaro, Giulia,Moorman, Allan R.,Romagnoli, Romeo,Preti, Delia,Baraldi, Stefania,Corciulo, Carmen,Vincenzi, Fabrizio,Borea, Pier Andrea,Varani, Katia
, p. 1098 - 1112 (2013/03/28)
Recent developments indicate that CB2 receptor ligands have the potential to become therapeutically important. To explore this potential, it is necessary to develop compounds with high affinity for the CB2 receptor. Very recently, we
