Indazole N-oxide derivatives as antiprotozoal agents: synthesis, biological evaluation and mechanism of action studies
- PMID: 16483783
- DOI: 10.1016/j.bmc.2006.01.007
Indazole N-oxide derivatives as antiprotozoal agents: synthesis, biological evaluation and mechanism of action studies
Abstract
A series of indazole N-oxide derivatives have been synthesized and their antichagasic and leishmanocidal properties studied. 3-Cyano-2-(4-iodophenyl)-2H-indazole N1-oxide exhibited interesting antichagasic activity on the two parasitic strains and the two parasitic stages evaluated. Furthermore, besides its trypanocidal activity, 3-cyano-2-(4-nitrophenyl)-2H-indazole N1-oxide showed leishmanocidal activity in the three parasitic strains evaluated. To gain insight into the mechanism of action, electrochemical behaviour, ESR experiment, inhibition of parasitic respiration and QSAR were performed.
Similar articles
-
Synthesis and biological properties of new 5-nitroindazole derivatives.Bioorg Med Chem. 2005 May 2;13(9):3197-207. doi: 10.1016/j.bmc.2005.02.043. Bioorg Med Chem. 2005. PMID: 15809155
-
Study of 5-nitroindazoles' anti-Trypanosoma cruzi mode of action: electrochemical behaviour and ESR spectroscopic studies.Eur J Med Chem. 2009 Apr;44(4):1545-53. doi: 10.1016/j.ejmech.2008.07.018. Epub 2008 Jul 23. Eur J Med Chem. 2009. PMID: 18762357
-
New potent 5-nitroindazole derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and mechanism of action studies.Bioorg Med Chem. 2009 Dec 15;17(24):8186-96. doi: 10.1016/j.bmc.2009.10.030. Epub 2009 Oct 20. Bioorg Med Chem. 2009. PMID: 19900812
-
In vitro assays for evaluation of drug activity against Leishmania spp.Res Microbiol. 2004 May;155(4):224-30. doi: 10.1016/j.resmic.2004.01.001. Res Microbiol. 2004. PMID: 15142618 Review.
-
Diamidines as antitrypanosomal, antileishmanial and antimalarial agents.Curr Opin Investig Drugs. 2006 Feb;7(2):147-57. Curr Opin Investig Drugs. 2006. PMID: 16499285 Review.
Cited by
-
Synthetic Medicinal Chemistry in Chagas' Disease: Compounds at The Final Stage of "Hit-To-Lead" Phase.Pharmaceuticals (Basel). 2010 Mar 25;3(4):810-838. doi: 10.3390/ph3040810. Pharmaceuticals (Basel). 2010. PMID: 27713281 Free PMC article. Review.
-
Antileishmanial activity of 5-nitroindazole derivatives.Ther Adv Infect Dis. 2023 Oct 30;10:20499361231208294. doi: 10.1177/20499361231208294. eCollection 2023 Jan-Dec. Ther Adv Infect Dis. 2023. PMID: 37915499 Free PMC article.
-
New hits as phase II enzymes inducers from a focused library with heteroatom-heteroatom and Michael-acceptor motives.Future Sci OA. 2015 Nov 1;1(3):FSO20. doi: 10.4155/fso.15.18. eCollection 2015 Nov. Future Sci OA. 2015. PMID: 28031894 Free PMC article.
-
Identification of potent chemotypes targeting Leishmania major using a high-throughput, low-stringency, computationally enhanced, small molecule screen.PLoS Negl Trop Dis. 2009 Nov 3;3(11):e540. doi: 10.1371/journal.pntd.0000540. PLoS Negl Trop Dis. 2009. PMID: 19888337 Free PMC article.
-
Indazole Derivatives Against Murine Cutaneous Leishmaniasis.Pharmaceuticals (Basel). 2025 Jul 25;18(8):1107. doi: 10.3390/ph18081107. Pharmaceuticals (Basel). 2025. PMID: 40872500 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Miscellaneous