Publications / Résultats
(Anglais)
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Jones, S.M., Urch, J.E., Brun, R., Harwood, J.L., Berry, C., Gilbert, I.H. Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents. Bioorg Med Chem. 12(4):683-92 (2004).
Dardonville,
C. & Brun, R. Bisguanidine, bis(2-aminoimidazoline), and polyamine
derivatives as potent and selective chemotherapeutic agents against
Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation. J.
Med. Chem. 47, 2296-2307 (2004).
Dardonville, C. Rinaldi, E., Barrett, M.P., Brun, R., Gilbert, I.H. & Hanau, S. Selective inhibition
of Trypanosoma brucei 6-phosphogluconate dehydrogenase by high energy
intermediate and transition state analogues. J. Med. Chem. 47(13),
3427-3437 (2004).
Sperandeo, N.R., Brinon, M.C. & Brun R.
Synthesis, antiprotozoal and cytotoxic activities of new
N-(3,4-dimethyl-5-isoxazolyl)-1,2-naphthoquinone-4-amino derivatives.
Farmaco 59(6):431-5 (2004).
Bringmann, G., Dreyer, M., Faber,
J.H., Dalsgaard, P.W., Staerk, D., Jaroszewski, J.W., Ndangalasi, H.,
Mbago, F., Brun, R. & Christensen, S.B. Ancistrotanzanine C and
Related 5,1'- and 7,3'-Coupled Naphthylisoquinoline Alkaloids from
Ancistrocladus tanzaniensis. J. Nat. Prod. 67(5):743-748 (2004).
Stewart, M.L., Bueno, G.J., Baliani, A., Klenke, B., Brun, R., Brock, J.M., Gilbert, I.H. & Barrett, M.P. Trypanocidal activity of melamine-based nitroheterocycles. Antimicrob. Agents Chemother. 48(5):1733-8 (2004).
Khabnadideh S, Pez D, Musso A, Brun R, Ruiz Pérez LM, González-Pacanowska D and
Gilbert IH. Design, Synthesis and Evaluation of 2,4-Diaminoquinazolines
as Inhibitors of Trypanosomal and Leishmanial Dihydrofolate Reductase.
Bioorg. Med. Chem. 13(7):2637-2649 (2005).
Whittingham JL, Leal I, Nguyen C, Kasinathan G, Bell E, Jones AF, Berry C, Benito A,
Turkenburg JP, Dodson EJ, Perez LM, Wilkinson AJ, Johansson NG, Brun R,
Gilbert IH, Pacanowska DG, Wilson KS. dUTPase as a Platform for
Antimalarial Drug Design: Structural Basis for the Selectivity of a
Class of Nucleoside Inhibitors. Structure (Camb). 13(2), 329-338 (2005).
Takasu K, Shimogama T, Saiin C, Kim HS, Wataya Y, Brun R, Ihara M. Synthesis
and evaluation of beta-carbolinium cations as new antimalarial agents
based on pi-delocalized lipophilic cation (DLC) hypothesis. Chem Pharm
Bull (Tokyo). 53(6), 653-61 (2005).
Bringmann G, Dreyer M, Kopff
H, Rischer H, Wohlfarth M, Hadi HA, Brun R, Meimberg H, Heubl G.
ent-Dioncophylleine A and related dehydrogenated naphthylisoquinoline
alkaloids, the first Asian dioncophyllaceae-type alkaloids, from the
"new"plant species Ancistrocladus benomensis. J Nat Prod. 68(5), 686-90
(2005).
Tasdemir D, Brun R, Perozzo R, Donmez AA. Evaluation of
antiprotozoal and plasmodial enoyl-ACP reductase inhibition potential
of turkish medicinal plants. Phytother Res. 19(2), 162-166 (2005). Baliani
A, Bueno GJ, Stewart ML, Yardley V, Brun R, Barrett MP, Gilbert IH.
Design and Synthesis of a Series of Melamine-based Nitroheterocycles
with Activity against Trypanosomatid Parasites. J Med Chem.
48(17):5570-5579 (2005).
Nguyen C, Kasinathan G, Leal-Cortijo I,
Musso-Buendia A, Kaiser M, Brun R, Ruiz-Perez LM, Johansson NG,
Gonzalez-Pacanowska D, Gilbert IH. Deoxyuridine Triphosphate
Nucleotidohydrolase as a Potential Antiparasitic Drug Target. J Med
Chem. 48(19):5942-5954 (2005).
Jones SM, Urch JE, Kaiser M, Brun
R, Harwood JL, Berry C, Gilbert IH. Analogues of Thiolactomycin as
Potential Antimalarial Agents. J Med Chem. 48(19):5932-5941 (2005).
George
TG, Johnsamuel J, Delfin DA, Yakovich A, Mukherjee M, Phelps MA, Dalton
JT, Sackett DL, Kaiser M, Brun R, Werbovetz KA. Antikinetoplastid
antimitotic activity and metabolic stability of dinitroaniline
sulfonamides and benzamides. Bioorg Med Chem. 14(16), 5699-710 (2006).
Tasdemir
D, Kaiser M, Brun R, Yardley V, Schmidt TJ, Tosun F, Ruedi P.
Antitrypanosomal and antileishmanial activities of flavonoids and their
analogues: in vitro, in vivo, structure-activity relationship, and
quantitative structure-activity relationship studies. Antimicrob Agents
Chemother. 50(4),1352-64 (2006).
Dardonville C, Barrett MP, Brun
R, Kaiser M, Tanious F, Wilson WD. DNA Binding Affinity of Bisguanidine
and Bis(2-aminoimidazoline) Derivatives with in Vivo Antitrypanosomal
Activity. J Med Chem. 49(12), 3748-3752 (2006).
Takasu K, Pudhom
K, Kaiser M, Brun R, Ihara M. Synthesis and antimalarial efficacy of
aza-fused rhodacyanines in vitro and in the P. berghei mouse model. J
Med Chem. 49(15), 4795-8 (2006).
Calderon AI, Romero LI,
Ortega-Barria E, Brun R, Correa MA, Gupta MP. Evaluation of larvicidal
and in vitro antiparasitic activities of plants in a biodiversity plot
in the Altos de Campana National Park, Panama. Pharmaceut Biol 44(7),
1-16 (2006).
Pez, D., Leal, I., Zuccotta, F., Boussard, C., Brun, R., Croft, S.L.,
Yardley, V., Ruiz Perez, L.M., Pacanowska, D.G. & Gilbert, I.H.
2,4-diaminopyrimidines as inhibitors of leishmanial and trypanosomal
dihydrofolate reductase. Bioorg. Med. Chem. 11, 4693-4711 (2003).
Klenke,
B., Barrett, M.P., Brun, R. & Gilbert, I.H. Antiplasmodial activity
of a series of 1,3,5-triazine-substituted polyamines. J. Antimicrob.
Chemother. 52 (2):290-293 (2003).
Dardonville, C., Rinaldi, E.,
Hanau, S., Barrett, M.P., Brun, R. & Gilbert, I.H. Synthesis and
biological evaluation of substrate-based inhibitors of
6-phosphogluconate dehydrogenase as potential drugs against African
trypanosomiasis. Bioorg. Med. Chem. 11, 3205-3214 (2003).
Sperandeo,
N. & Brun, R. Synthesis and biological evaluation of
pyrazolyl-Naphtho-quinones as new potential antiprotozoal agents.
ChemBioChem 4, 69-72 (2003).
Chowdhury, S.F., Guerrero, R.H.,
Brun, R., Ruiz-Perez, L.M., Gonzalez Pacanowska, D.& Gilbert, I.H.
Synthesis and Testing of 5-Benzyl-2,4-diaminopyrimidines as Potential
Inhibitors of Leishmanial and Trypanosomal Dihydrofolate Reductase. J.
Enzyme Inhib. Med. Chem. 17, 293-302 (2002).
Griesbeck, A.G.,
El-Idreesy, T.T., Fiege, M. & Brun, R. Synthesis of anti-malaria
active 1,2,4-trioxanes via photooxygenation of a chiral allylic
alcohol. Organic Letters, 4, 4193-4195 (2002).
Bringmann, G.,
Menche, D., Kraus, J., Mühlbacher, J., Peters, K., Peters, E.-M., Brun,
R., Bezabih, M. & Abegaz, B.M. Atropo-enantioselective total
synthesis of knipholone and related antiplasmodial
phenylanthraquinones. J. Org. Chem. 67, 5595-610 (2002).
Klenke,
B., Stewart, M., Barrett, M.P., Brun, R. & Gilbert, I. Synthesis
andbiological evaluation of s-triazine substituted polyamines as
potential new anti-trypanosomal drugs. J. Med. Chem. 44, 3440-3452
(2001).
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