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Synthesis and antimicrobial activity of novel naphtho[2,1-b]furo-5H-[3,2-d][1,3,4]thiadiazolo[3,2-a]pyrimidin-5-ones

“…Thus reaction of 4, having similar functionality, on treatment with different aromatic acids in phosphrus oxychloride led to the formation of 2-aryl naphtho [ [1,3,4]…”

“…There has been considerable interest in the development of preparative methods for the production of pyrimidines. This seems to be because pyrimidines represent one of the most active classes of compounds, possessing a wide spectrum of biological activity [1][2][3] . Pyrimidines and their ring-fused derivatives have a broad spectrum of biological activity; best known as the heterocyclic core of the nucleic acid bases.…”

3-(4-Bromobenzoyl)prop-2-enoic acid as Precursor in Synthesis of Some Important Heterocyclic Compounds

“…The pyrimidines and their ring-fused derivatives are one of the most active classes of compounds, possessing a wide spectrum of biological activity [15]. They are known as heterocyclic core of the nucleic acid bases.These ring systems are often incorporated into drugs designed for anticancer [16,17], antiviral [18], Antihypertensive [19], analgesic [20], antipyretic [21], anti-inflammatory [22], anti-psoriasis [23] agents.…”

“…The reaction mixture was left to cool at r.t.then acidified with diluted HCl ,the formed solid was filtered off , washed with cold water, dried and crystallized from the proper solvent to afford pyridopyrimidine (13) Maleic anhydride (0.98 mg, 0.01 mol) was completely dissolved at room temperature in glacial acetic acid or THF (10 mL), and then pyridine derivative 4 (3.2 g,0.01 mol) was added to the solution; the resulting mixture was stirred under reflux for l h. The reaction mixture was allowed to cool at room temperature, then poured into water (20 ml), the precipitate formed was filtered off, washed with water,dried and crystallized from methanol to afford N-substituted maleamic acid 14 To a solution of -cyclic maleamic acid 14 (2.00 g, 5.2 mmol) and malononitrile (0.34 g, 5.2 mmol) in DMF (4 mL) few drops of piperidine was added; the resulting mixture was refluxed at 60 C for 5 h. The reaction mixture was allowed to cool at room temperature then acidified with diluted acetic acid 20 mL, the solid formed was filtered off, washed with water, dried and crystallized from methanol/water to afford furan derivative 15 A mixture ofN-cyclic maleamic acid 14 (2 g, 5.2 mmol) and malononitrile [36] (0.34 g, 5.2 mmol) in DMF (3 mL) in the presence of ammonium acetate was refluxed at 60 C for 3 h. The reaction mixture was allowed to cool at room temperature then poured into diluted solution of acetic acid 20 ml, the solid formed was filtered off, washed with water, dried and crystallized from ethanol/water to afford aminopyrrole derivative 16 ).respectively 2-[4-acetyl-3-(carboxymetbyl)-5-methylf uran-2-ylamino 1-6-(4-bromo phenyl)-3-cyanopyridine-4-carboxylic acid (17) A mixture of N-cyclic maleamic acid 14 (2 g, 5.2 mmol) and acetylacetone (0.53 mL, 5.2 mmol) in DMF (3 mL) in the presence of piperidine was refluxed at 60 C for 3 h. The reaction mixture was allowed to cool at room temperature then poured into diluted solution of acetic acid (200 mL), the solid formed was filtered off, washed with water, dried and crystallized from ethanol/ water to afford furan derivatives 17. M.wt=498(C 22 …”

Molecular Docking studies and in-silico ADMET Screening of Some novel Oxazine substituted 9-Anilinoacridines as Topoisomerase II Inhibitors

“…The intercalative property was referred to the planar aromatic system of the acridine moiety. In the same context, acridines have gained strong ground for various biological activities like antimicrobial, 1 antioxidant, 2 anticancer, [3][4][5] antimalarial, 6 analgesic, 7 antileishmanial, 8 antinociceptive, 9 acetyl cholinesterase inhibitors 10 and antiherpes 11 etc. Amsacrine is the best known compound of 9-anilinoacridines series.…”