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Antiparasitic activities of new lawsone Mannich bases

DOI zum Zitieren der Version auf EPub Bayreuth: https://doi.org/10.15495/EPub_UBT_00005759
URN to cite this document: urn:nbn:de:bvb:703-epub-5759-5

Title data

Al Nasr, Ibrahim ; Jentzsch, Jana ; Winter, Isabel ; Schobert, Rainer ; Ersfeld, Klaus ; Koko, Waleed S. ; Mujawah, Adil A. H. ; Khan, Tariq A. ; Biersack, Bernhard:
Antiparasitic activities of new lawsone Mannich bases.
In: Archiv der Pharmazie. Vol. 352 (2019) Issue 11 . - No. 1900128.
ISSN 1521-4184
DOI der Verlagsversion: https://doi.org/10.1002/ardp.201900128

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Abstract

A series of new lawsone Mannich bases derived from salicylaldehydes or nitrofurfural were prepared and tested for their activities against Leishmania major, Toxoplasma gondii, and Trypanosoma brucei brucei parasites. The hydrochloride salts 5a and 6a of the Mannich bases 2a and 3a, derived from unsubstituted salicylaldehyde and long-chained alkyl amines, were selectively and strongly active against T. gondii cells and appear to be new promising drug candidates against this parasite. Compound 6a showed an even higher activity against T. gondii than the known lawsone Mannich base 1b. Compound 4a, derived from salicylaldehyde and 2-methylaminopyridine, was also distinctly active against T. gondii cells. The derivatives 3a (salicyl derivative), 3b (3,5-dichloro-2-hydroxyphenyl derivative), and 3d (5-nitrofuranyl derivative) as well as the hydrochlorides 6a and 6b were also efficacious against T. b. brucei cells with compounds 3a and 3b being more selective for T. b. brucei over Vero cells when compared with the known control compound 1b. The derivatives 5a, 5c, 6a, and 6c proved to be up to five times more active than 1b against L. major promastigotes and up to four times more efficacious against L. major amastigotes.

Further data

Item Type: Article in a journal
Keywords: antiparasitic drugs; lawsone; Mannich base; neglected tropical diseases; salicyl derivatives
DDC Subjects: 500 Science > 500 Natural sciences
500 Science > 540 Chemistry
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Biology > Professor Genetics > Professor Genetics - Univ.-Prof. Dr. Klaus Ersfeld
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Organic Chemistry I > Chair Organic Chemistry I - Univ.-Prof. Dr. Rainer Schobert
Faculties
Faculties > Faculty of Biology, Chemistry and Earth Sciences
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Biology
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Biology > Professor Genetics
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Organic Chemistry I
Language: English
Originates at UBT: Yes
URN: urn:nbn:de:bvb:703-epub-5759-5
Date Deposited: 03 Sep 2021 08:21
Last Modified: 03 Sep 2021 08:21
URI: https://epub.uni-bayreuth.de/id/eprint/5759

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