- 2,6-Difluorobenzamide Inhibitors of Bacterial Cell Division Protein FtsZ: Design, Synthesis, and Structure–Activity Relationships
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A wide variety of drug-resistant microorganisms are continuously emerging, restricting the therapeutic options for common bacterial infections. Antimicrobial agents that were originally potent are now no longer helpful, due to their weak or null activity toward these antibiotic-resistant bacteria. In addition, none of the recently approved antibiotics affect innovative targets, resulting in a need for novel drugs with innovative antibacterial mechanisms of action. The essential cell division protein filamentous temperature-sensitive Z (FtsZ) has emerged as a possible target, thanks to its ubiquitous expression and its homology to eukaryotic β-tubulin. In the latest years, several compounds were shown to interact with this prokaryotic protein and selectively inhibit bacterial cell division. Recently, our research group developed interesting derivatives displaying good antibacterial activities against methicillin-resistant Staphylococcus aureus, as well as vancomycin-resistant Enterococcus faecalis and Mycobacterium tuberculosis. The aim of the present study was to summarize the structure–activity relationships of differently substituted heterocycles, linked by a methylenoxy bridge to the 2,6-difluorobenzamide, and to validate FtsZ as the real target of this class of antimicrobials.
- Straniero, Valentina,Zanotto, Carlo,Straniero, Letizia,Casiraghi, Andrea,Duga, Stefano,Radaelli, Antonia,De Giuli Morghen, Carlo,Valoti, Ermanno
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p. 1303 - 1318
(2017/09/01)
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- A metal catalyst-free and one-pot synthesis of (3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)methanol derivatives in water
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A robust and metal catalyst-free method has been developed for the general and green synthesis of racemic (3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)methanol derivatives. This simple, mild and practical method involves the reaction of 2-aminophenols with (±
- Singh, Shambhu Nath,Jayaprakash, Sarva,Venkateshwara Reddy,Nakhi, Ali,Pal, Manojit
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p. 84889 - 84893
(2015/10/28)
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- Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity
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The design, synthesis, and structure-activity relationship of two novel classes of benzoxazine derivatives with dual selective serotonin reuptake inhibitors and 5-HT1A receptor activities are described.
- Zhou, Dahui,Harrison, Boyd L.,Shah, Uresh,Andree, Terrance H.,Hornby, Geoffrey A.,Scerni, Rosemary,Schechter, Lee E.,Smith, Deborah L.,Sullivan, Kelly M.,Mewshaw, Richard E.
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p. 1338 - 1341
(2007/10/03)
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- A straightforward route to 4H-1,4-benzoxazine-2-carbaldehydes by Swern oxidation
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Swern oxidation of saturated (1,4-benzoxazine-2-yl)-methanols 2 furnished 4H-1,4-benzoxazine-2-carbaldehydes 3, which possess an α,β ethylenic bond. The reactivity of these compounds was examined.
- Bourlot, Anne-Sophie,Guillaumet, Gerald,Merour, Jean-Yves
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p. 191 - 196
(2007/10/03)
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- 5-phenylpyrrolo-1,4-benzoxazine and 5-phenylpyrrolo-1,4-benzothiazine compounds, process and intermediates for their production and pharmaceutical compositions containing them
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Pharmacologically active compounds of formula I STR1 which can be substituted in the phenyl rings and in which R1 denotes hydrogen or lower alkyl, R2 denotes hydrogen or lower alkyl, Y denotes oxygen or sulfur n represents an integer from 1 to 3 Z represents a bond, a CO group or a CH= group, Q denotes nitrogen or the CH group and R7, if Q denotes nitrogen, represents an optionally substituted pyridyl or phenyl radical or, if Q denotes the CH group, represents the N-methyl-N-(4-oxo-3H-pyrimidin-2-yl)amino group, and their acid addition salts and processes and intermediates for their preparation.
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