Biological effects of a new set 1,2,4-triazolo[1,5-a]quinazolines on heart rate and blood pressure

Abstract

BackgroundSeveral quinazoline and triazole derivatives are reported to possess a wide-range of interesting pharmacological effects. Although various triazoloquinazoline subclasses having been synthesized and studied, the preparation of 1,2,4-triazolo[1,5-a]quinazolines as antihypertensive agent is still relatively unexplored. In continuation of our earlier research, we aimed at the synthesis and development of various potent antihypertensive 1,2,4-triazoloquinazoline derivatives.ResultsA new series of 1,2,4-triazolo[1,5-a]quinazoline derivatives have been synthesized. Their structures were mainly established by spectroscopic methods of analysis (IR, MS, 1H and 13C NMR). Their in vivo antihypertensive activity was evaluated by tail cuff method using Muromachi Blood Pressure Monitor (Model MK 2000) for rats and mice. Some of the tested compounds were found to exhibit valuable effects in terms of heart rate and blood pressure. According to the biological results, some of tested derivatives have abolished completely the tachycardia of the parent compounds and may be studied and modified as potential adrenoblockers and cardiac stimulant.ConclusionNew series of fifteen 1,2,4-triazolo[1,5-a]quinazolines were synthesized by convenient methodology from four key molecules, whereby their structures were established by advanced spectroscopic analyses. Some lead compounds have abolished completely the tachycardia of the parent compounds, that may be examined as potent adrenoblockers and some other compounds seem to be a cardiac stimulant or may be modified to enhance their hypotensive activity.

Synthesis and antioxidant activity of 2-methylthio-pyrido[3,2-e][1,2,4] triazolo[1,5-a]pyrimidines

“…The DPPH, FRAP and RPC assays were applied to assess the in vitro antioxidant activity of the pyrido-triazolopyrimidines (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17). The obtained results were presented in figures 1-3 and compared with standard synthetic antioxidant.…”

“…Triazolo-annelated quinazolines were found to be potent adenosine antagonists, herbicidal and fungicidal agents [1][2][3]. In addition, further chemical transformation of their inherent lactam groups and substituent types at positions 2 and 5 were offered access to a variety of derivatives that have shown antihistamine, antimicrobial, antiviral, antihypertensive, anti-inflammatory, antitumor and antioxidant activities [4][5][6][7][8][9][10][11]. In light of the abovementioned facts, we are interested in the conversion of triazolquinazoline moiety into a pyridotriazolopyrimidine scaffold.…”

“…The emergence of various diseases resulting from oxidative stress such as diabetes, cancer, stroke, and cardiovascular dysfunctions, requires a permanent revaluation search and adjustment of adequate strategy to design and develop new bioactive substances to protect the human body against such diseases. In continuation of our on-going program research dealing with antioxidants, this research deals with the preparation and characterization of 2-methylthio-pyrido-triazolopyrimidines (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17); thereafter, evaluating their antioxidant activity using different assays.…”

Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents

“…Unambiguous conrmation of all products was nally achieved by clear identication of the 1 H and 13 C resonances of the accompanying functional groups or moieties, such as -SCH 3 , -SO 2 CH 3 , -OPh, benzyl, and phenethyl, and through comparison with data of structurally related compounds. [19][20][21][22][23][24]…”

Antihistamine Activity of 1,2,4-Triazolo[1,5-a]quinazolines

“…In addition, a number of synthesized 1,2,4-triazolo-4H-[4,3-a]quinazolin-5-ones have been found to display as good antihistamine agents 7,8 . In view of these points, the present work is an extension of our ongoing efforts in the field of triazolo-quinzolines chemistry [9][10][11][12][13][14][15][16] , towards the development and designing of new compounds. Therefore, we aimed to investigate a new set of synthesized 1,2,4-triazolo-[1,5a]quinazolines as antihistamine agents.…”