Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A
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2008
Authors
Šolaja, Bogdan A.Opsenica, Dejan M.
Smith, Kirsten S.
Milhous, Wilbur K.
Terzić-Jovanović, Nataša
Opsenica, Igor
Burnett, James C.
Nuss, Jon
Gussio, Rick
Bavari, Sina
Article (Published version)
Metadata
Show full item recordAbstract
We report on the initial result of the coupling of 4-amino7-chloroquinoline with steroidal and adamantane constituents to provide small molecules with excellent in vitro antimalarial activities (IC90 (W2) down to 6.74 nM). The same entities also inhibit the botulinum neurotoxin serotype A light chain metalloprotease at low nlicromolar levels (7-3 1 yM). Interestingly. structural features imparting increased antimalarial activity also provide increased inetalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.
Source:
Journal of Medicinal Chemistry, 2008, 51, 15, 4388-4391Publisher:
- Amer Chemical Soc, Washington
Funding / projects:
- NCI NIH HHS [Y3-CM-100505]
DOI: 10.1021/jm800737y
ISSN: 0022-2623
PubMed: 18637666
WoS: 000258289800007
Scopus: 2-s2.0-49449118829
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Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Šolaja, Bogdan A. AU - Opsenica, Dejan M. AU - Smith, Kirsten S. AU - Milhous, Wilbur K. AU - Terzić-Jovanović, Nataša AU - Opsenica, Igor AU - Burnett, James C. AU - Nuss, Jon AU - Gussio, Rick AU - Bavari, Sina PY - 2008 UR - https://cherry.chem.bg.ac.rs/handle/123456789/961 AB - We report on the initial result of the coupling of 4-amino7-chloroquinoline with steroidal and adamantane constituents to provide small molecules with excellent in vitro antimalarial activities (IC90 (W2) down to 6.74 nM). The same entities also inhibit the botulinum neurotoxin serotype A light chain metalloprotease at low nlicromolar levels (7-3 1 yM). Interestingly. structural features imparting increased antimalarial activity also provide increased inetalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets. PB - Amer Chemical Soc, Washington T2 - Journal of Medicinal Chemistry T1 - Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A VL - 51 IS - 15 SP - 4388 EP - 4391 DO - 10.1021/jm800737y ER -
@article{ author = "Šolaja, Bogdan A. and Opsenica, Dejan M. and Smith, Kirsten S. and Milhous, Wilbur K. and Terzić-Jovanović, Nataša and Opsenica, Igor and Burnett, James C. and Nuss, Jon and Gussio, Rick and Bavari, Sina", year = "2008", abstract = "We report on the initial result of the coupling of 4-amino7-chloroquinoline with steroidal and adamantane constituents to provide small molecules with excellent in vitro antimalarial activities (IC90 (W2) down to 6.74 nM). The same entities also inhibit the botulinum neurotoxin serotype A light chain metalloprotease at low nlicromolar levels (7-3 1 yM). Interestingly. structural features imparting increased antimalarial activity also provide increased inetalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.", publisher = "Amer Chemical Soc, Washington", journal = "Journal of Medicinal Chemistry", title = "Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A", volume = "51", number = "15", pages = "4388-4391", doi = "10.1021/jm800737y" }
Šolaja, B. A., Opsenica, D. M., Smith, K. S., Milhous, W. K., Terzić-Jovanović, N., Opsenica, I., Burnett, J. C., Nuss, J., Gussio, R.,& Bavari, S.. (2008). Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. in Journal of Medicinal Chemistry Amer Chemical Soc, Washington., 51(15), 4388-4391. https://doi.org/10.1021/jm800737y
Šolaja BA, Opsenica DM, Smith KS, Milhous WK, Terzić-Jovanović N, Opsenica I, Burnett JC, Nuss J, Gussio R, Bavari S. Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. in Journal of Medicinal Chemistry. 2008;51(15):4388-4391. doi:10.1021/jm800737y .
Šolaja, Bogdan A., Opsenica, Dejan M., Smith, Kirsten S., Milhous, Wilbur K., Terzić-Jovanović, Nataša, Opsenica, Igor, Burnett, James C., Nuss, Jon, Gussio, Rick, Bavari, Sina, "Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A" in Journal of Medicinal Chemistry, 51, no. 15 (2008):4388-4391, https://doi.org/10.1021/jm800737y . .