Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives

Abstract

A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.

Magnetic nanoporous MCM‐41 supported ionic liquid/palladium complex: An efficient nanocatalyst with high recoverability

“…[16][17][18] However, magnetic iron oxides suffer from several problems such as being unstable in acidic and alkaline conditions, aggregation over long periods of time and oxidation in the presence of air. [40][41][42][43] Although several methods have been developed until now for the synthesis of the pyrano[2,3-d]pyrimidine derivatives using different catalysts systems, some of these protocols suffer from disadvantages of long reaction times, homogenous catalysts, product separation, toxic solvent and catalyst recovery. [19,20] Among the different species, silica is the most commonly used material to stabilize magnetic NPs.…”

Synthesis and Biological Evaluation of some Novel Pyrano[2,3-<i>d</i>]Pyrimidine Derivatives

“…If pyrano [2,3-d]pyrimidine moieties are clubbed into one molecule, then resultant derivative enhances its pharmaceutical activity as abundant in biologically active compounds such as antitumour [5], cardiotonic [6], antibronchitic [7] and antifungal activity [8]. Some of them exhibit antihypertensive activity [9], antimalarial [10], analgesic [10,11], and antimicrobial and antiviral evaluation [12,13] properties. Pyrano [2,3-d]pyrimidines are building blocks used to evaluate their antimicrobial activities and various derived natural products [14].…”

Dibutylamine (DBA): A highly efficient catalyst for the synthesis of pyrano[2,3-d]pyrimidine derivatives in aqueous media

“…Therefore chemotherapeutic efficacy of annulated pyrano [2,3-d]pyrimidines is related to their ability to inhibit enzymes action for DNA biosynthesis, such as dihydrofolate reductase (DHFR), thymidylate synthetase (TSase), thymidine phosphorylase (TPase) and reverse transcriptase (RTase). Pyrano [2,3-d] M a n u s c r i p t 2 pyrimidine moieties that are annulated in to one molecule, then resultant derivative enhances its pharmaceutical activity such as, antitumor [8], antihypertensive [9], antibacterial activity [10] and antileishmanial activity [11]. Therefore, for the preparation of these complex molecules, large efforts have been made towards the synthetic manipulation of annulated uracils that occupy a distinct and unique place in medicinal chemistry.…”