Abstract
| Original language | English |
|---|---|
| Pages (from-to) | 496 - 500 |
| Number of pages | 5 |
| Journal | A C S Medicinal Chemistry Letters |
| Volume | 5 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - 2014 |
Cite this
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Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei. / Rashad, Adel A; Jones, Amy J; Avery, Vicky M; Baell, Jonathan Bayldon; Keller, Paul Anthony.
In: A C S Medicinal Chemistry Letters, Vol. 5, No. 5, 2014, p. 496 - 500.Research output: Contribution to journal › Article › Research › peer-review
TY - JOUR
T1 - Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei
AU - Rashad, Adel A
AU - Jones, Amy J
AU - Avery, Vicky M
AU - Baell, Jonathan Bayldon
AU - Keller, Paul Anthony
PY - 2014
Y1 - 2014
N2 - The high throughput screening of a library of over 87,000 drug-like compounds against the African sleeping sickness parasite resulted in the discovery of hits with a wide range of molecular diversity. We report here the medicinal chemistry development of one such hit, a tetrahydroisoquinoline disulfonamide, with the synthesis and testing of 26 derivatives against the trypanosome subspecies. Activities in the 2-4 ?M range were revealed with a selectivity index suitable for further development.
AB - The high throughput screening of a library of over 87,000 drug-like compounds against the African sleeping sickness parasite resulted in the discovery of hits with a wide range of molecular diversity. We report here the medicinal chemistry development of one such hit, a tetrahydroisoquinoline disulfonamide, with the synthesis and testing of 26 derivatives against the trypanosome subspecies. Activities in the 2-4 ?M range were revealed with a selectivity index suitable for further development.
UR - http://pubs.acs.org/doi/pdf/10.1021/ml400487t
U2 - 10.1021/ml400487t
DO - 10.1021/ml400487t
M3 - Article
VL - 5
SP - 496
EP - 500
JO - A C S Medicinal Chemistry Letters
JF - A C S Medicinal Chemistry Letters
SN - 1948-5875
IS - 5
ER -