1,721,062 research outputs found
A one-pot PPh3-promoted synthesis of new functionalized heterocycles derived from 2-aminobenzo[d]isothiazol-3-one
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On the Use of 2,5-Dimethyl-Pyrrol-1-yl-Benzoic Acid Derivatives as EPH-Ephrin Antagonists.
No full textA one-pot PPh3-promoted synthesis of new functionalized heterocycles derived from 2-aminobenzo[d]isothiazol-3-one
No full textInvestigation of the reaction between 3-benzisothiazolones, an isoindole isoster and activated acetylenes: synthesis of novel heterocyclic backbones for building bioactive molecules
Full text linkInvestigation of the reaction between benzo[d]isothiazol-3-one, 2-aminobenzo[d]isothiazol-3-one, its isoster 2-aminoisoindolin-1-one, and activated acetylenes, in the presence of triphenylphosphine, led us to synthesize novel heterocyclic compounds that could be attractive for the building of biologically active molecules. A one-pot PPh3-promoted tandem reaction, with acetylene dicarboxylates and dibenzoylacetylene, afforded new tricyclic pyrazolo-fused benzisothiazoles. The PPh3-promoted reaction between benzisothiazolones and methyl propiolate afforded 1,4-benzothiazepine-5-one derivatives, via an isothiazole ring expansion. These studies are providing additional insights in benzisothiazolone chemistry and describe simple and original synthetic accesses to novel derivatives
Aminoderivatives of benzothiazole/benzisothiazole heterocycles as intermediates in the synthesis of novel therapeutic agents
No full textSynthesis and antimicrobial activity of novel 2-thiazolylimino-5-arylidene-4-thiazolidinones
No full textNew 2-thiazolylimino-5-arylidene-4-thiazolidinones (compounds 4a-j), unsubstituted or carrying hydroxy, methoxy, nitro and chloro groups on the benzene ring, were synthesized and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria, yeasts and mould. The compounds were very potent towards all tested Gram positive microorganisms (MIC ranging from 0.03 microg/mL to 6 microg/mL in most of the cases) and Gram negative Haemophilus influenzae (MIC 0.15-1.5 microg/mL), whereas no effectiveness was exhibited against Gram negative Escherichia coli and fungi up to the concentration of 100 microg/mL. The 5-arylidene derivatives showed an antibacterial efficacy considerably greater than that of the parent 2-(thiazol-2-ylimino)thiazolidin-4-one 3, suggesting that the substituted and unsubstituted 5-arylidene moiety plays an important role in enhancing the antimicrobial properties of this class of compounds. The remarkable inhibition of the growth of penicillin-resistant staphylococci make these substances promising agents also for the treatment of infections caused by microorganisms resistant to currently available drugs
Synthesis of novel 5-arylidene-thiazol-4-ones 2-heteroarylamino substituted as potential antimicrobials
No full textSynthesis of benzisoxazole and benzisothiazole derivatives with potential antitumor activity
No full textThiazolyl and isothiazolyl azomethine derivatives with antiinflammatory and antioxidant activities. Synthesis, biological evaluation and structure activity relationships study
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