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Synthesis, in vitro and in vivo activity of novel 9-deoxo-9a-aza-9a-homoerythromycin A derivatives; A new class of macrolide antibiotics, the azalides.
Open accessAbstract
A series of erythromycin A-derived semisynthetic antibiotics, featuring incorporation of a basic nitrogen atom into a ring expanded (15-membered) macrocyclic lactone, have been prepared and biologically evaluated. Semisynthetic modifications focused upon (1) varied substitution at the macrocyclic ring nitrogen and (2) epimerization or amine substitution at the C-4'' hydroxyl site within the cladinose sugar. In general, the new azalides exhibit improved Gram-negative potency, expanding the spectrum of erythromycin A to fully include Haemophilus influenzae and Neisseria gonorrhoeae. When compared to erythromycin A, the azalides exhibit substantially increased half-life and area-under-the-curve values in all species studied. The overall in vitro/in vivo performance of N-methyl, C-4'' epimers 3a and 9; and C-4'' amine 11 identify these compounds as the most interesting erythromycin A-superior agents. Compound 3a has been advanced to clinical study.
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Cited by
The influence of natural products upon drug discovery (Antiquity to late 1999)
Newman, D. J., Cragg, G. M., & Snader, K. M. (2000) · Natural Product Reports · doi:10.1039/a902202c · Cited by 1,293
New Directions in Antibacterial Research
Chu, D. T. W., Plattner, J. J., & Katz, L. (1996) · Journal of Medicinal Chemistry · doi:10.1021/jm960294s · Cited by 298
Metadata
- Authors
- BRIGHT, G. M., NAGEL, A. A., BORDNER, J., DESAI, K. A., DIBRINO, J. N., NOWAKOWSKA, J., VINCENT, L., WATROUS, R. M., SCIAVOLINO, F. C., ENGLISH, A. R., RETSEMA, J. A., ANDERSON, M. R., BRENNAN, L. A., BOROVOY, R. J., CIMOCHOWSKI, C. R., FAIELLA, J. A., GIRARD, A. E., GIRARD, D., HERBERT, C., MANOUSOS, M., & MASON, R.
- Venue
- The Journal of Antibiotics
- Published
- 1988
- Volume
- 41
- Issue
- 8
- Pages
- 1029-1047
- ISSN
- 0021-8820 (ISSN-L)
- 1881-1469
- OpenAlex
- W2003567541
- Cited by
- 237
- References
- 0
- FWCI
- 10.28
- Type
- journal article
- Language
- en
- Open access
- bronze
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- CoChat. (2026). Citation check: Synthesis, in vitro and in vivo activity of novel 9-deoxo-9a-aza-9a-homoerythromycin A derivatives; A new class of macrolide antibiotics, the azalides. https://app.cochat.ai/papers/10.7164/antibiotics.41.1029
- The paper
- BRIGHT, G. M., NAGEL, A. A., BORDNER, J., DESAI, K. A., DIBRINO, J. N., NOWAKOWSKA, J., VINCENT, L., WATROUS, R. M., SCIAVOLINO, F. C., ENGLISH, A. R., RETSEMA, J. A., ANDERSON, M. R., BRENNAN, L. A., BOROVOY, R. J., CIMOCHOWSKI, C. R., FAIELLA, J. A., GIRARD, A. E., GIRARD, D., HERBERT, C., . . . MASON, R. (1988). Synthesis, in vitro and in vivo activity of novel 9-deoxo-9a-aza-9a-homoerythromycin A derivatives; A new class of macrolide antibiotics, the azalides. The Journal of Antibiotics. https://doi.org/10.7164/antibiotics.41.1029
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
