183500-37-0Relevant articles and documents
Highly improved antiparasitic activity after introduction of an N -benzylimidazole moiety on protein farnesyltransferase inhibitors
Bosc, Damien,Mouray, Elisabeth,Cojean, Sandrine,Franco, Caio Haddad,Loiseau, Philippe M.,Freitas-Junior, Lucio H.,Moraes, Carolina Borsoi,Grellier, Philippe,Dubois, Jo?lle
supporting information, p. 173 - 186 (2016/01/25)
In our search for new protein farnesyltransferase inhibitors with improved antiparasitic activities, we modified our previously developed 3-arylthiophene series of inhibitors by replacing the thioisopropyl group by different substituted imidazolylmethanamino moieties. Twenty four new derivatives were synthesized and evaluated against human and parasite farnesyltransferases, and their anti-parasitic activity was determined against Plasmodium falciparum, Trypanosoma brucei, Trypanosoma cruzi, and Leishmania donovani. Introduction of a N-p-substituted-benzylimidazole led to significantly increase the inhibition of parasite proliferation in the submicromolar range. The structure of the best inhibitors was parasite dependent. Three compounds possess IC50 values at the same range as the reference miltefosine against L. donovani proliferation and other new derivatives display high level of anti-trypanosomal activity against T. cruzi, higher or in the same order of magnitude as the reference compounds benznidazole and nifurtimox.
N-benzyl imidazole derivatives and their use as aldosterone synthase inhibitors
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Page/Page column 13, (2009/09/26)
The invention relates to the use of a N-benzyl 5-substituted imidazole derivative having the general formula I wherein R is (C1-3)alkyl, (C1-3)alkyloxy, halogen, nitro or cyano; R1 is (C1-6)alkyl, optionally substituted with OH, (C1-3)alkyloxy, (C1-3)alkylcarbonyloxy, (C1-3)alkyloxycarbonyl or halogen, or (C1-3)alkyloxycarbonyl; or R1 is phenyl, optionally substituted with 1-3 substituents independently selected from (C1-3)alkyl, (C1-3)alkyloxy, hydroxylmethyl and halogen; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of a disorder or disease in a subject mediated by aldosterone synthase or responsive to inhibition of aldosterone synthase.
Novel N-(4-piperidinyl)benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity
Ryckebusch, Adina,Gilleron, Pauline,Millet, Regis,Houssin, Raymond,Lemoine, Amelie,Pommery, Nicole,Grellier, Philippe,Sergheraert, Christian,Henichart, Jean-Pierre
, p. 1324 - 1326 (2007/10/03)
Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity against the parasite at submicromolar concentrations.