Syntheses of 1-Acyl-3-phenylacetylurea Derivatives

Syntheses and biological evaluation of 2-amino-3-acyl-tetrahydrobenzothiophene derivatives; antibacterial agents with antivirulence activity.

Developing new compounds targeting virulence factors (e.g., inhibition of pilus assembly by pilicides) is a promising approach to combating bacterial infection. A high-throughput screening campaign of a library of 17 500 small molecules identified 2-amino-3-acyl-tetrahydrobenzothiophene derivatives (hits 2 and 3) as novel inhibitors of pili-dependent biofilm formation in a uropathogenic Escheri...

1- and 3-deamidino derivatives of dihydrostreptomycin and some 1-N-acyl derivatives.

1-Deamidino-, 3-deamidino- and 1,3-di(deamidino)dihydrostreptomycin (1, 2, 3) were prepared by treatment of dihydrostreptomycin (DHSM) with ammonia at 100 degrees C. The 3-guanidino group of DHSM is suggested to be more important than the 1-guanidino group for the antibacterial activity of DHSM. 1-N-[(S)-4-Amino-2-hydroxybutyryl) and 1-N-[(S)-4-guanidino-2-hydroxybutyryl] derivatives (4, 6) of ...

Syntheses and biological evaluation of 2 - amino - 3 - acyl -

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Syntheses of Anisomycin Derivatives

The structure of anisomycin has been determined by X-ray investigation4 and the absolute configuration was confirmed by chemical correlation.5 Anisomycin has attracted considerable synthetic interest, and several synthetic studies, derivative syntheses as well as total syntheses, have been reported.6 Especially, the synthesis of its analogues has revealed the structure-activity relationship of ...

Syntheses and antimicrobial activities of 9-O-acyl derivatives of tylosin and demycarosyltylosin.