We report on the initial result of the coupling of 4-amino-7- 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 micromolar levels (7-31 μM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.
Source:
Journal of Medicinal Chemistry, 2008, 51, 15, 4388-4391
TY - JOUR
AU - Śolaja, B.A.
AU - Opsenica, Dejan
AU - Smith, K. S.
AU - Milhous, Wilbur K.
AU - Terzić, Nataša
AU - Opsenica, Igor
AU - Burnett, J.C.
AU - Nuss, J.
AU - Gussio, R.
AU - Bavari, S.
PY - 2008
UR - http://cer.ihtm.bg.ac.rs/handle/123456789/451
AB - We report on the initial result of the coupling of 4-amino-7- 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 micromolar levels (7-31 μM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.
PB - American Chemical Society (ACS)
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 = "Śolaja, B.A. and Opsenica, Dejan and Smith, K. S. and Milhous, Wilbur K. and Terzić, Nataša and Opsenica, Igor and Burnett, J.C. and Nuss, J. and Gussio, R. and Bavari, S.",
year = "2008",
url = "http://cer.ihtm.bg.ac.rs/handle/123456789/451",
abstract = "We report on the initial result of the coupling of 4-amino-7- 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 micromolar levels (7-31 μM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.",
publisher = "American Chemical Society (ACS)",
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"
}
Śolaja B, Opsenica D, Smith KS, Milhous WK, Terzić N, Opsenica I, Burnett J, Nuss J, Gussio R, Bavari S. Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. Journal of Medicinal Chemistry. 2008;51(15):4388-4391
Śolaja, B.A., Opsenica, D., Smith, K. S., Milhous, W. K., Terzić, 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.
Journal of Medicinal ChemistryAmerican Chemical Society (ACS)., 51(15), 4388-4391.
https://doi.org/10.1021/jm800737y
Śolaja B.A., Opsenica Dejan, Smith K. S., Milhous Wilbur K., Terzić Nataša, Opsenica Igor, Burnett J.C., Nuss J., Gussio R., Bavari S., "Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A" 51, no. 15 (2008):4388-4391,
https://doi.org/10.1021/jm800737y .
