Abstract
Structure-activity relationships of phenazines against Mycobacterium leprae were investigated by using an in vitro radiorespirometric assay. In general, activity in ascending order was observed in compounds containing no chlorine atoms, a monochlorinated phenazine nucleus, and chlorines in the para positions of both the anilino and phenyl rings. The most active compounds contained a 2,2,6,6-tetramethylpiperidine substitution at the imino nitrogen. Most of these chlorinated phenazines were considerably more active in vitro than clofazimine (B663).
Full text
PDFSelected References
These references are in PubMed. This may not be the complete list of references from this article.
- BARRY V. C., CONALTY M. L. Antituberculosis activity in the phenazine series. II. N3-substituted anilinoaposafranines (rimino-compounds) and some derivatives. Am Rev Tuberc. 1958 Jul;78(1):62–73. doi: 10.1164/artpd.1958.78.1.62. [DOI] [PubMed] [Google Scholar]
- BROWNE S. G., HOGERZEIL L. M. "B 663" in the treatment of leprosy. Preliminary report of a pilot trial. Lepr Rev. 1962 Jan;33:6–10. [PubMed] [Google Scholar]
- Franzblau S. G., Harris E. B. Biophysical optima for metabolism of Mycobacterium leprae. J Clin Microbiol. 1988 Jun;26(6):1124–1129. doi: 10.1128/jcm.26.6.1124-1129.1988. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Franzblau S. G., Hastings R. C. Rapid in vitro metabolic screen for antileprosy compounds. Antimicrob Agents Chemother. 1987 May;31(5):780–783. doi: 10.1128/aac.31.5.780. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Franzblau S. G. Oxidation of palmitic acid by Mycobacterium leprae in an axenic medium. J Clin Microbiol. 1988 Jan;26(1):18–21. doi: 10.1128/jcm.26.1.18-21.1988. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hastings R. C., Franzblau S. G. Chemotherapy of leprosy. Annu Rev Pharmacol Toxicol. 1988;28:231–245. doi: 10.1146/annurev.pa.28.040188.001311. [DOI] [PubMed] [Google Scholar]
- Hastings R. C., Gillis T. P., Krahenbuhl J. L., Franzblau S. G. Leprosy. Clin Microbiol Rev. 1988 Jul;1(3):330–348. doi: 10.1128/cmr.1.3.330. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Imkamp F. M. A treatment of corticosteroid-dependent lepromatous patients in persistent erythema nodosum leprosum. A clinical evaluation of G.30320 (B663). Lepr Rev. 1968 Jul;39(3):119–125. doi: 10.5935/0305-7518.19680022. [DOI] [PubMed] [Google Scholar]
- Mittal A., Seshadri P. S., Conalty M. L., O'Sullivan J. F., Nath I. Rapid, radiometric in vitro assay for the evaluation of the anti-leprosy activity of clofazimine and its analogues. Lepr Rev. 1985 Jun;56(2):99–108. [PubMed] [Google Scholar]
- O'Sullivan J. F., Conalty M. L., Morrison N. E. Clofazimine analogues active against a clofazimine-resistant organism. J Med Chem. 1988 Mar;31(3):567–572. doi: 10.1021/jm00398a013. [DOI] [PubMed] [Google Scholar]
- Roberts G. D., Goodman N. L., Heifets L., Larsh H. W., Lindner T. H., McClatchy J. K., McGinnis M. R., Siddiqi S. H., Wright P. Evaluation of the BACTEC radiometric method for recovery of mycobacteria and drug susceptibility testing of Mycobacterium tuberculosis from acid-fast smear-positive specimens. J Clin Microbiol. 1983 Sep;18(3):689–696. doi: 10.1128/jcm.18.3.689-696.1983. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wheeler P. R. Measurement of hypoxanthine incorporation in purified suspensions of Mycobacterium leprae: a suitable method to screen for anti-leprosy agents in vitro. J Med Microbiol. 1988 Mar;25(3):167–174. doi: 10.1099/00222615-25-3-167. [DOI] [PubMed] [Google Scholar]
- Yawalkar S. J., Vischer W. Lamprene (clofazimine) in leprosy. Basic information. Lepr Rev. 1979 Jun;50(2):135–144. doi: 10.5935/0305-7518.19790020. [DOI] [PubMed] [Google Scholar]