Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials
Murugesan Dinakaran
1
,
Alka Mital
1
,
Marcel Kaiser
2, 3
,
D. Shackleford
4
,
Julia Morizzi
4
,
Kasiram Katneni
4
,
M. Campbell
4
,
Alan Hudson
5
,
Susan C Charman
4
,
Clive Yeates
6
,
Ian Gilbert
1
5
Pharmacons, Kent, U.K.
|
6
InPharma Consultancy, Herts, U.K.
|
Publication type: Journal Article
Publication date: 2013-03-21
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
23517371
Drug Discovery
Molecular Medicine
Abstract
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC(50) ~ 9 nM), good selectivity (>2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalarial.
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70
Total citations:
70
Citations from 2024:
10
(14.28%)
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GOST
Copy
Dinakaran M. et al. Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials // Journal of Medicinal Chemistry. 2013. Vol. 56. No. 7. pp. 2975-2990.
GOST all authors (up to 50)
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Dinakaran M., Mital A., Kaiser M., Shackleford D., Morizzi J., Katneni K., Campbell M., Hudson A., Charman S. C., Yeates C., Gilbert I. Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials // Journal of Medicinal Chemistry. 2013. Vol. 56. No. 7. pp. 2975-2990.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/jm400009c
UR - https://doi.org/10.1021/jm400009c
TI - Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials
T2 - Journal of Medicinal Chemistry
AU - Dinakaran, Murugesan
AU - Mital, Alka
AU - Kaiser, Marcel
AU - Shackleford, D.
AU - Morizzi, Julia
AU - Katneni, Kasiram
AU - Campbell, M.
AU - Hudson, Alan
AU - Charman, Susan C
AU - Yeates, Clive
AU - Gilbert, Ian
PY - 2013
DA - 2013/03/21
PB - American Chemical Society (ACS)
SP - 2975-2990
IS - 7
VL - 56
PMID - 23517371
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2013_Dinakaran,
author = {Murugesan Dinakaran and Alka Mital and Marcel Kaiser and D. Shackleford and Julia Morizzi and Kasiram Katneni and M. Campbell and Alan Hudson and Susan C Charman and Clive Yeates and Ian Gilbert},
title = {Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials},
journal = {Journal of Medicinal Chemistry},
year = {2013},
volume = {56},
publisher = {American Chemical Society (ACS)},
month = {mar},
url = {https://doi.org/10.1021/jm400009c},
number = {7},
pages = {2975--2990},
doi = {10.1021/jm400009c}
}
Cite this
MLA
Copy
Dinakaran, Murugesan, et al. “Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials.” Journal of Medicinal Chemistry, vol. 56, no. 7, Mar. 2013, pp. 2975-2990. https://doi.org/10.1021/jm400009c.
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