A convenient synthesis of novel 5-aryl-pyrido[2,3-d]pyrimidines and screening of their preliminary antibacterial properties

Synthesis and Antifungal <i>in Vitro</i> Evaluation of Pyrazolo[3,4-<i>b</i>]pyridines Derivatives Obtained by Aza-Diels–Alder Reaction and Microwave Irradiation

“…1). According to the calculated atomic coefficients and the previous reports, 2,5) the possible mechanistic route to explain the formation of pyrazolo [3,4-b] pyridine involves in the initial step the cycloaddition between the formimidamide 1a and the β-nitrostyrene 2 with the corresponding formation of the Diels-Alder adduct 3′. This eliminates a dimethylamine molecule and is oxidized by air under thermal conditions to obtain the aromatic product corresponding 5-nitro-1-phenylpyrazolo[3,4-b] pyridine 3 2,5,11) (Chart 2).…”

“…2,3) To obtain sixmembered nitrogen-containing and/or pyridine fused polyheterocyclic compounds, the aza-Diels-Alder (A-DA) strategy is a powerful synthetic tool and mechanistically the cyclization may occur in a concerted manner or by step-wise reaction between the azadiene and dienophile. 4,5) According to our experience, the microwave assisted organic synthesis (MAOS) is a technique to simplify and improve classic organic synthesis because it allows cleaner and shorter reactions with higher yields and reducing byproducts. 6,7) Recently we have developed several MAOS methodologies to obtain pyrazolo [3,4-b] pyridines, 2,[8][9][10][11][12][13] since they are an important group of nitrogen-containing fused heterocycles useful for medicinal and organic chemistry with a wide spectrum of biological and pharmacological activities [14][15][16] as antibacterial, antidepressant, anti-hyperglycemic, anti-inflammatory, antitumor, and anxiolytic agents and are being used in the treatment of Alzheimer's diseases, drugs addiction, and infertility.…”

Synthesis of carbazole bearing pyridopyrimidine‐substituted sulfonamide derivatives and studies their carbonic anhydrase enzyme activity

“…Pyridopyrimidinones are an important class of heterocyclic compounds and the skeletal structure can be found in drugs and shown biological activities such as, antiallergic, antibacterial, antitumor, anti‐inflammatory, antileishmanial agents, ribofuranosides as potential therapeutic agents, carbonic anhydrase (CA) enzyme inhibition, and polyphenol oxidase enzyme inhibitor …”

Development of a Water-Mediated and Catalyst-Free Green Protocol for Easy Access to a Huge Array of Diverse and Densely Functionalized Pyrido[2,3-d:6,5-d′]dipyrimidines via One-Pot Multicomponent Reaction under Ambient Conditions

“…Among N -heterocycles, pyrimidine and its derivatives are reported for a wide range of biological profiles including antioxidant, anti-inflammatory, immunomodulating, antibacterial, antiviral, and antitumor activity. − Categorically, barbituric/2-thiobarbituric acids, an important class of pharmaceutically promising pyrimidine derivatives, find potential applications as building blocks for a series of barbiturate/thiobarbiturate drugs used as hypnotics, sedatives, anticonvulsants, anesthetics, antioxidants, antifungal, and as CNS depressants. − Combination of barbituric/thiobarbituric acid moiety with other pharmacophoric groups, thus, may offer a possibility to synthesize numerous derivatives with desired potential biological effects. With this view, pyrimidine-fused pyridines, especially pyrido­[2,3- d ]­pyrimidines, have been studied intensively over the recent past due to their wide spectrum of promising biological activities. − Among various tricyclic pyrimido­pyrido­pyrimidines, the pyrido­[2,3- d :6,5- d ′]­dipyrimidine scaffold has attracted much attention because a handful of such derivatives possess considerable α-glucosidase and α-amylase inhibitory activity, antibacterial, , antiviral, NAD-type redox catalytic, and anticorrosive , properties. In addition, such a scaffold has been reported to have the potential in self-assembling to constitute supramolecular structure as well …”