Synthesis and antimicrobial activity of 2H-pyrimido[2,1-b]benzothiazol-2-ones

Abstract

4-Phenyl-2H-pyrimido[2,1-b]benzothiazol-2-ones have been synthesized in quantitative yields by the reaction of 2-aminobenzothiazoles with alkynoic acid. The antimicrobial activity of the synthesized compounds was tested against bacterial species, Bacillus coagulans, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. The synthesized compounds have shown significant activity against microorganisms which can be correlated with the fused heterocyclic systems.

A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry

“…Compound (5) displayed significant activity against B. coagulans and P. aeruginosa, compared with the standard, chloramphenicol. Fusion of two biodynamic heterosystems, BTA and pyrimidine, resulted in formation of a new heterocyclic scaffold with significant bioactivity [62]. 2-Substituted BTA derivatives were prepared and tested for antimicrobial activity against both, Gram positive and Gram negative bacteria, with ampicillin as a standard.…”

Reagent-controlled regiodivergent intermolecular cyclization of 2-aminobenzothiazoles with β-ketoesters and β-ketoamides

“…As trace amounts of benzo[4,5]thiazolo[3,2- a ]pyrimidin-4-ones, 5a , were observed in the synthesis of benzo[ d ]imidazo[2,1- b ]-thiazoles, we searched for a suitable reagent to regioselectively form this instead of 3a and 4 . This tricyclic backbone can be found in compounds that possess a wide range of medicinal properties including those with antimalarial [ 74 ], anticancer [ 75 – 76 ], antiallergic [ 77 – 78 ], antibacterial [ 79 ], and antimicrobial properties [ 80 – 81 ]. In addition, they have been found to be biologically active antagonists of adenosine receptors [ 82 ], inhibitors of cyclic-AMP-diphosphoesterase [ 83 ], and benzodiazepine receptor ligands [ 84 – 85 ].…”

A Review: Antimicrobial Agents Based on Nitrogen and Sulfur Containing Heterocycles

“…Substituted thiazines ring-based chemical compounds are considered as organic compounds holding four carbon atoms and one N and S atom at various place in the rings containing six members present in various structures. Further, a variety of organic compounds are synthesized by the use of 1, 3 and 1,4 thiazines [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15].…”