A convenient synthesis of some new fused pyridine and pyrimidine derivatives of antimicrobial profiles

Abstract

Some novel triazolo [1,5-a]pyridine (4-6), thiazolo[3,2-a]pyridine (7), thiazolo[3,2-a]pyrimidines (9, 11), oxoimidazo[1,2-a]pyrimidine (10), and pyrimido[2,1-b]quinazoline (12) have been synthesized. The structures of target compounds were confirmed by elemental analyses and spectral data. The antimicrobial activity of some of the target synthesized compounds were tested against various microorganisms such as Salmonella typhimurium, Pseudomonas aeruginos and Staphylococcus aureus (bacteria), Aspergillus flavus (fungus), and Candida albicans (yeast fungus) by the disc diffusion method. In general, the novel synthesized compounds showed a good antimicrobial activity against these microorganisms.

Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers

“…The 5H-pyrido[2′,3′:4,5]pyrimido[2,1-b]quinazoline-5,7(12H)-dione analogues 8a–d were synthesised through the reaction of compounds 7b–e with anthranilic acid in the presence of catalytic amount of sodium ethoxide under reflux condition 60 . Their chemical structures were confirmed by elemental and spectral data for example the 1 H NMR of compound 8d revealed an increase in the integration of aromatic region at δ 6.76–8.15 ppm, and the presence of D 2 O exchangeable singlet signal assigned for one proton of NH group at δ 11.64 ppm.…”

“…The 2-hydrazinopyrido[2,3-d]pyrimidin-4(3H)-one derivatives 9a–e were depicted through the nucleophilic attack of hydrazine hydrate upon the key derivatives 7a–e following the reported method 60 . The newly hydrazinyl derivative 9a was proved by spectral data.…”

“…A mixture of 2-hydrazinylpyrido[2,3-d]pyrimidine 9 b–e (1 mmol) and ethyl chloroformate (0.22 g, 2 mmol) in dry pyridine (10 ml) was heated under reflux for 9 h 60 . The reaction mixture was cooled and the obtained solid was filtered, washed with ethanol, dried, and crystallised from DMF: EtOH (1:2).…”

“…A mixture of 2-hydrazinylpyrido[2,3-d]pyrimidines 9a–e (0.002 mol) and ammonium thiocyanate (2.38 g, 0.3 mol) in glacial acetic acid (15 ml) was heated under reflux for 10 h. The reaction mixture was cooled, poured onto iced water and the precipitate was filtered, dried and washed with hot ethanol 60 .…”

Novel Pyrazolines and Benzothiazepines as Tubulin Polymerization Inhibitors: Synthesis, Biological Evaluation, and Molecular Docking

“…[11][12][13] In addition, promising compounds D-F were synthesised to inhibit tubuline polymerization (Figure 2). [14][15][16] As a part of our research on bioactive heterocyclic and pharmaceutical compounds, [17][18][19][20][21] in this work, we developed anti-tubulin agents, based on chalcones as important precursors with novel backbone compounds for the synthesis of a variety of heterocyclic compounds using benzothiazepine and pyrazoline rings to act as linkers between essential rings based upon reported structures, in a trial to test a new ideas in both structural evolution and therapeutic approaches. .…”