SYNTHETIC, SPECTRAL, ANTIMICROBIAL AND QSAR STUDIES ON NOVEL MANNICH BASES OF GLUTARIMIDES
摘要:
A series of forty Mannich bases of glutarimides with sulfonamides and secondary amines were synthesized and evaluated in vitro against six pathogenic Gram-positive and Gram-negative bacteria. The synthesized Mannich bases were characterized by elemental and spectral analysis. The modeling anti-bacterial activities of these newly synthesized Mannich bases against six bacteria was attempted employing H-1 NMR chemical shift, physicochemical properties and topological indices as the correlating parameters. Our results, based on Quantitative Structure-Activity Relationships (QSARs), have indicated that statistically significant models are obtained for modeling the anti-bacterial activities The results are discussed critically using a variety of statistical parameters.
GLUTARIMIDES 3-ARYL-3-CARBOXYALKYL SUBSTITUES, LEUR PREPARATION PAR CYCLISATION D'ACIDES DICARBOXYLIQUES DE LA 4-ARYL-4-CYANOHEPTANE ET LEUR UTILISATION POUR LA PREPARATION DE 3-ARYL-3-HYDROXYALKYLPIPERIDINES
申请人:SANOFI-SYNTHELABO
公开号:EP0888304B1
公开(公告)日:2001-10-04
SYNTHETIC, SPECTRAL, ANTIMICROBIAL AND QSAR STUDIES ON NOVEL MANNICH BASES OF GLUTARIMIDES
作者:ANJU DAS MANIKPURI、SHEELA JOSHI、PADMAKAR V KHADIKAR
DOI:10.4067/s0717-97072010000300001
日期:——
A series of forty Mannich bases of glutarimides with sulfonamides and secondary amines were synthesized and evaluated in vitro against six pathogenic Gram-positive and Gram-negative bacteria. The synthesized Mannich bases were characterized by elemental and spectral analysis. The modeling anti-bacterial activities of these newly synthesized Mannich bases against six bacteria was attempted employing H-1 NMR chemical shift, physicochemical properties and topological indices as the correlating parameters. Our results, based on Quantitative Structure-Activity Relationships (QSARs), have indicated that statistically significant models are obtained for modeling the anti-bacterial activities The results are discussed critically using a variety of statistical parameters.
A boron-catalyzed Michael reaction using pairs of carboxylicacids was developed. The reaction occurs through dual activation of the two substrates by a boron catalyst, which facilitates boron enolate formation from the donor carboxylicacid with simultaneous activation of the α,β-unsaturated carboxylicacid as the acceptor. α-Aryl and α-alkenyl carboxylicacids were applicable as donors. The versatility