- Title
- New thiazolidine-2,4-dione derivatives combined with organometallic ferrocene: Synthesis, structure and antiparasitic activity
- Creator
- Oderinlo, Ogunyemi O, Tukulula, Matshawandile, Isaacs, Michelle, Taylor, Dale, Smith, Vincent J, Khanye, Setshaba D, Hoppe, Heinrich C
- Date
- 2018
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/122978
- Identifier
- vital:35382
- Identifier
- https://doi.org/10.1002/aoc.4385
- Description
- Favourable physicochemical properties of an organometallic ferrocene and antiplasmodial potency of compounds containing the thiazolidine‐2,4‐dione framework (TZD‐4) prompted us to explore compounds containing both the thiazolidine‐2,4‐dione core and the ferrocenyl unit with the primary aim of identifying compounds with promising antiprotozoal activities. Thus, a new series of rationally designed ferrocene‐based thiazolidine‐2,4‐dione derivatives, containing a selection of secondary cyclic amines, was synthesised and fully characterised using standard spectroscopic techniques. The resulting compounds were screened for their antiplasmodial and antitrypanosomal activities against both the chloroquine‐resistant (Dd2) strain of Plasmodium falciparum and the Nagana Trypanosoma brucei brucei 427. The general trend that emerged indicated that the target compounds were more selective towards T. b. brucei compared to the P. falciparum parasite. Moreover, the analogues bearing methylpiperazine (8a) and piperidine (8b) rings were more active against T. b. brucei compared to hit compound TZD‐4. Except compound 8b, which appeared promising, none of the synthesised compounds showed better activity than TZD‐4 against the P. falciparum parasite. All the synthesised compounds were non‐toxic and often showed >90% viability of the HeLa cell line screened.
- Format
- 9 pages, pdf
- Language
- English
- Relation
- Applied Organometallic Chemistry, Oderinlo, O.O., Tukulula, M., Isaacs, M., Hoppe, H.C., Taylor, D., Smith, V.J. and Khanye, S.D., 2018. New thiazolidine-2, 4-dione derivatives combined with organometallic ferrocene: Synthesis, structure and antiparasitic activity. Applied Organometallic Chemistry, 32(7), p.e4385., Applied Organometallic Chemistry number 32 1 9 March 2018 1099-0739
- Rights
- Applied Organometallic Chemistry
- Rights
- Use of this resource is governed by the terms and conditions of the Wiley Online Library Terms of Use Statement (https://onlinelibrary.wiley.com/terms-and-conditions)
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Khanye, David Setshaba (Associate Prof)
RU Centre for Chemico- and Biomedicinal Research (CCBR)
Hoppe, Heinrich C (Prof)
Isaacs, Michelle (Mrs)
RU Department of Pharmacy
RU Department of Biochemistry, Microbiology and Bioinformatics
SDG 03. Good Health and Well-Being
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