ArticleMolecules (Basel, Switzerland)2014
Antileishmanial lead structures from nature: analysis of structure-activity relationships of a compound library derived from caffeic Acid bornyl ester.
Article in Molecules (Basel, Switzerland), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 32 citations in OpenAlex.
- Discovery and Development of Caffeic Acid Analogs as Versatile Therapeutic Agents.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Biological Activity of Hybrid Molecules Based on Major Constituents ofLife (Basel, Switzerland) · 2023Article
- Structure-Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents.ChemMedChem · 2020Article
- A Comprehensive QSAR Study on Antileishmanial and Antitrypanosomal Cinnamate Ester Analogues.Molecules (Basel, Switzerland) · 2019Article
- Pharmacokinetic profile and metabolite identification of bornyl caffeate and caffeic acid in rats by high performance liquid chromatography coupled with mass spectrometry.RSC advances · 2019Article
- Caffeates and Caffeamides: Synthetic Methodologies and Their Antioxidant Properties.International journal of medicinal chemistry · 2019Review
- Perifosine Mechanisms of Action in Leishmania Species.Antimicrobial agents and chemotherapy · 2017Article
- Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni.Molecules (Basel, Switzerland) · 2015Article
- Antileishmanial and cytotoxic compounds from Valeriana wallichii and identification of a novel nepetolactone derivative.Molecules (Basel, Switzerland) · 2015Article
- Article
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bioassay-guided fractionation of a chloroform extract of Valeriana wallichii (V. wallichii) rhizomes lead to the isolation and identification of caffeic acid bornyl ester (1) as the active component against Leishmania major (L. major) promastigotes (IC50 = 48.8 µM). To investigate the structure-activity relationship (SAR), a library of compounds based on 1 was synthesized and tested in vitro against L. major and L. donovani promastigotes, and L. major amastigotes. Cytotoxicity was determined using a murine J774.1 cell line and bone marrow derived macrophages (BMDM). Some compounds showed antileishmanial activity in the concentration range of pentamidine and miltefosine which are the standard drugs in use. In the L. major amastigote assay compounds 15, 19 and 20 showed good activity with relatively low cytotoxicity against BMDM, resulting in acceptable selectivity indices. Molecules with adjacent phenolic hydroxyl groups exhibited elevated cytotoxicity against murine cell lines J774.1 and BMDM. The Michael system seems not to be essential for antileishmanial activity. Based on the results compound 27 can be regarded as new lead structure for further structure optimization.
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