Search: onr:"swepub:oai:lup.lub.lu.se:fbb51695-c54c-4e7f-999b-2406f567aa22" >
SAR:s for the Antip...
-
Terrazas, PaolaLund University,Lunds universitet,Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH,Universidad Mayor de San Simon
(author)
SAR:s for the Antiparasitic Plant Metabolite Pulchrol. 1. The Benzyl Alcohol Functionality
- Article/chapterEnglish2020
Publisher, publication year, extent ...
Numbers
-
LIBRIS-ID:oai:lup.lub.lu.se:fbb51695-c54c-4e7f-999b-2406f567aa22
-
https://lup.lub.lu.se/record/fbb51695-c54c-4e7f-999b-2406f567aa22URI
-
https://doi.org/10.3390/molecules25133058DOI
Supplementary language notes
-
Language:English
-
Summary in:English
Part of subdatabase
Classification
-
Subject category:art swepub-publicationtype
-
Subject category:ref swepub-contenttype
Notes
-
Pulchrol (1) is a natural benzochromene isolated from the roots of Bourreria pulchra, shown to possess potent antiparasitic activity towards both Leishmania and Trypanozoma species. As it is not understood which molecular features of 1 are important for the antiparasitic activity, several analogues were synthesized and assayed. The ultimate goal is to understand the structure-activity relationships (SAR:s) and create a QSAR model that can be used for the development of clinically useful antiparasitic agents. In this study, we have synthesized 25 2-methoxy-6,6-dimethyl-6H-benzo[c]chromen analogues of 1 and its co-metabolite pulchral (5a), by semi-synthetic procedures starting from the natural product pulchrol (1) itself. All 27 compounds, including the two natural products 1 and 5a, were subsequently assayed in vitro for antiparasitic activity against Trypanozoma cruzi, Leishmania brasiliensis and Leishmania amazoniensis. In addition, the cytotoxicity in RAW cells was assayed, and a selectivity index (SI) for each compound and each parasite was calculated. Several compounds are more potent or equi-potent compared with the positive controls Benznidazole (Trypanozoma) and Miltefosine (Leishmania). The compounds with the highest potencies as well as SI-values are esters of 1 with various carboxylic acids.
Subject headings and genre
Added entries (persons, corporate bodies, meetings, titles ...)
-
Salamanca, EfrainHigher University of San Andrés
(author)
-
Dávila, MarceloUniversidad Mayor de San Simon
(author)
-
Manner, SophieLund University,Lunds universitet,Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH(Swepub:lu)orgk-sma
(author)
-
Giménez, AlbertoHigher University of San Andrés
(author)
-
Sterner, OlovLund University,Lunds universitet,Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH(Swepub:lu)ok2-ost
(author)
-
Centrum för analys och syntesKemiska institutionen
(creator_code:org_t)
Related titles
-
In:Molecules (Basel, Switzerland): MDPI AG25:131420-3049
Internet link
Find in a library
To the university's database