The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Structure−Activity Relationships for a Series of Quinoline-Based Compounds Active against Replicating and Nonreplicating Mycobacterium tuberculosis
Abstract
Tuberculosis (TB) remains as a global pandemic that is aggravated by a lack of health care, the spread of HIV, and the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) strains. New anti-TB drugs are urgently required to shorten the long 6-12 month treatment regimen and to battle drug-resistant Mtb strains. We have identified several potent quinoline-based anti-TB compounds, bearing an isoxazole containing side-chain. The most potent compounds, 7g and 13, exhibited submicromolar activity against the replicating bacteria (R-TB), with minimum inhibitory concentrations (MICs) of 0.77 and 0.95 microM, respectively. In general, these compounds also had micromolar activity against the nonreplicating persistent bacteria (NRP-TB) and did not show toxicity on Vero cells up to 128 microM concentration. Compounds 7g and 13 were shown to retain their anti-TB activity against rifampin, isoniazid, and streptomycin resistant Mtb strains. The results suggest that quinoline-isoxazole-based anti-TB compounds are promising leads for new TB drug development.
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Cites
A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis
Andries, K., Verhasselt, P., Guillemont, J., Göhlmann, H. W. H., Neefs, J.-M., Winkler, H., Van Gestel, J., Timmerman, P., Zhu, M., Lee, E., et al. (2005) · Science · doi:10.1126/science.1106753 · Cited by 2,191
Franzblau, S. G., Witzig, R. S., McLaughlin, J. C., Torres, P., Madico, G., Hernandez, A., Degnan, M. T., Cook, M. B., Quenzer, V. K., Ferguson, R. M., et al. (1998) · Journal of Clinical Microbiology · doi:10.1128/jcm.36.2.362-366.1998 · Cited by 964
Self-citationDiarylquinolines target subunit c of mycobacterial ATP synthase
Koul, A., Dendouga, N., Vergauwen, K., Molenberghs, B., Vranckx, L., Willebrords, R., Ristic, Z., Lill, H., Dorange, I., Guillemont, J., et al. (2007) · Nature Chemical Biology · doi:10.1038/nchembio884 · Cited by 547
Tuberculosis — metabolism and respiration in the absence of growth
Boshoff, H. I. M., & Barry, C. E. (2005) · Nature Reviews Microbiology · doi:10.1038/nrmicro1065 · Cited by 448
Substituted 4-methylquinolines as a new class of anti-tuberculosis agents
Jain, R., Vaitilingam, B., Nayyar, A., & Palde, P. B. (2003) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(03)00074-x · Cited by 62
Cited by
The recent progress of isoxazole in medicinal chemistry
Zhu, J., Mo, J., Lin, H.-Z., Chen, Y., & Sun, H.-P. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.05.013 · Cited by 417
Metadata
- Authors
- Lilienkampf, A., Mao, J., Wan, B., Wang, Y., Franzblau, S. G., & Kozikowski, A. P.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2009-03-09
- Volume
- 52
- Issue
- 7
- Pages
- 2109-2118
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1985884232
- Cited by
- 308
- References
- 5
- FWCI
- 12.57
- Type
- journal article
- Language
- en
- Open access
- closed
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