Catalytic regioselective synthesis of pyrazole based pyrido[2,3-d]pyrimidine-diones and their biological evaluation

Abstract

A new type of biopolymer-based heterogeneous catalyst, cellulose supported acidic ionic liquid (Cell-IL), which was developed earlier in our lab, has been found to be very effective for the regioselective synthesis of pyrazole based pyrido[2,3-d]pyrimidine-diones. Its regioselectivity was confirmed by (1)H NMR spectroscopy. All the newly synthesized compounds were characterized by LC-MS, (1)H NMR, (13)C NMR, IR spectroscopy and elemental analysis. The newly synthesized compounds were evaluated for their in vitro antimalarial activity against Plasmodium falciparum, in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain and also for their antibacterial activity against a panel of pathogenic strains of bacteria and fungi. Some of them exhibited excellent activity when compared with first line drugs.

One-pot synthesis of annulated pyrido[2,3-d:6,5-d]dipyrimidine derivatives using nitrogen based DBU catalyst in aqueous ethanol medium

“…Comparatively fewer methods have been described for the synthesis of fused pyrido[2,3-d:6,5-d]dipyrimidine derivatives. However, similar annulated pyrimidine derivatives such as Pyrido [2,3-d]pyrimidines were reported using different reagents in the presence of catalysts, such as L-proline [20], piperidine [21], ionic liquid (Cell-IL) [22], ZrO 2 [23] and without catalyst [24,25]. Reported methods appearing in the literature usually require forcing conditions, prolonged reaction time, create wastes, complex synthetic pathway and low yields.…”

Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs

“…In continuation of our efforts to synthesize some novel heterocyclic motifs with biological interest [27][28][29][30][31][32][33][34][35][36][37][38][39][40], herein we report the design, synthesis, antimicrobial evaluation, cytotoxicity and genotoxicity of quinoline based 1,2,4-oxadiazole scaffold. Potent 1,2,4-oxadiazole moiety is linked to quinoline moiety at C-3 position to observe the synergistic effect of these rings towards antimicrobial activity.…”

Synthesis of Pyrazolo‐[4́,3́:5,6]pyrido[2,3‐d]pyrimidine‐diones Catalyzed by a Nano‐sized Surface‐Grafted Neodymium Complex of the Tungstosilicate via Multicomponent Reaction

“…In recent years biological activities of pyrazole, pyridine and pyrimidine based organic molecules have been approved, thus, heterocyclic systems containing the basic aforementioned heterocycles have attracted the attention of synthetic organic chemists …”

“…[13] In recent years biological activities of pyrazole, pyridine and pyrimidine based organic molecules have been approved, thus, heterocyclic systems containing the basic aforementioned heterocycles have attracted the attention of synthetic organic chemists. [14] Polyoxometalates (POMs), as a unique class of anionic metal oxide clusters, are gaining more interest due to numerous advantageous properties and widespread applications. [15] Among the various applications of POMs, catalysis is one of the most important area of applications.…”