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Erythromycin Series. XII. Antibacterial in Vitro Evaluation of 10-dihydro-10-deoxo-11-azaerythromycin A: Synthesis and Structure-Activity Relationship of Its Acyl Derivatives

Erythromycin Series. XII. Antibacterial in Vitro Evaluation of 10-dihydro-10-deoxo-11-azaerythromycin A: Synthesis and Structure-Activity Relationship of Its Acyl Derivatives

S Djokić, G Kobrehel, G Lazarevski

J Antibiot (Tokyo). 1987 Jul;40(7):1006-15.

PMID: 3484349

Abstract:

Antibacterial in vitro evaluation of 10-dihydro-10-deoxo-11-azaerythromycin A (5), the new 15-membered semi-synthetic macrolide antibiotic with nitrogen as additional atom in the aglycone ring of erythromycin A (1), was reported. Although amine (5) and its 13,14-cyclic carbonate (14) were less active than 1 against erythromycin-sensitive Staphylococcus aureus strains they showed advantageous properties against Gram-negative test organisms and clinical isolates. Also, a large number of acyl derivatives of 5 were synthesized and evaluated. N-11 monoacyl compounds exhibited 2 to 50 times lower in vitro antibacterial efficacy than the parent amine (5).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP76801859	Azaerythromycin A		76801-85-9	Price

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