A series of O56-substituted carboxyester or carboxyamide derivatives of deglucoteicoplanin (TD) was prepared by condensation of the 56-hydroxyl function with various alkylating agents of general formula RBr, where R represents functional groups with different physico-chemical properties. The modifications at position 56 influenced the antimicrobial activity of the new derivatives; activity depended on the structure of various R groups, their ionic properties, and their steric hindrance. The activity of the new compounds did not show any significant improvement when compared with TD. The physico-chemical and antibacterial properties of the synthesized compounds are reported.
Synthesis and biological activity of O56-substituted carboxyesters and carboxamides of teicoplanin aglycone / P. Seneci, A. Trani, P. Ferrari, R. Scotti, R. Ciabatti. - In: JOURNAL OF ANTIBIOTICS. - ISSN 0021-8820. - 45:10(1992 Oct), pp. 1633-1644.
Synthesis and biological activity of O56-substituted carboxyesters and carboxamides of teicoplanin aglycone
P. SeneciPrimo
;
1992
Abstract
A series of O56-substituted carboxyester or carboxyamide derivatives of deglucoteicoplanin (TD) was prepared by condensation of the 56-hydroxyl function with various alkylating agents of general formula RBr, where R represents functional groups with different physico-chemical properties. The modifications at position 56 influenced the antimicrobial activity of the new derivatives; activity depended on the structure of various R groups, their ionic properties, and their steric hindrance. The activity of the new compounds did not show any significant improvement when compared with TD. The physico-chemical and antibacterial properties of the synthesized compounds are reported.
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