scispace - formally typeset
Search or ask a question
Author

K. M. Muraleedharan

Bio: K. M. Muraleedharan is an academic researcher from Indian Institute of Technology Madras. The author has contributed to research in topics: Artemisinin & Carboxylic acid. The author has an hindex of 12, co-authored 47 publications receiving 751 citations. Previous affiliations of K. M. Muraleedharan include University of Mississippi & Indian Institute of Chemical Technology.

Papers
More filters
Journal ArticleDOI
TL;DR: Van Tamelen and Shamma as discussed by the authors proposed that halolactonisation arise by the intramolecular carboxylic acid-mediated opening of the initially formed halonium ion intermediate.

203 citations

Journal ArticleDOI
TL;DR: The study suggests the possibility of developing artemisinin analogues as potential drug candidates against both malaria and leishmaniasis.
Abstract: Artemisinin (1) and its analogues have been well studied for their antimalarial activity. Here we present the antimalarial activity of some novel C-9-modified artemisinin analogues synthesized using artemisitene as the key intermediate. Further, antileishmanial activity of more than 70 artemisinin derivatives against Leishmania donovani promastigotes is described for the first time. A comprehensive structure-activity relationship study using CoMFA is discussed. These analogues exhibited leishmanicidal activity in micromolar concentrations, and the overall activity profile appears to be similar to that against malaria. Substitution at the C-9beta position was shown to improve the activity in both cases. The 10-deoxo derivatives showed better activity compared to the corresponding lactones. In general, compounds with C-9alpha substitution exhibited lower antimalarial as well as antileishmanial activities compared to the corresponding C-9beta analogues. The importance of the peroxide group for the observed activity of these analogues against leishmania was evident from the fact that 1-deoxyartemisinin analogues did not exhibit antileishmanial activity. The study suggests the possibility of developing artemisinin analogues as potential drug candidates against both malaria and leishmaniasis.

93 citations

Journal ArticleDOI
TL;DR: Progress made in the past decade pertaining to the development of anti-parasitic agents based on artemisinin is presented and an outline on its seco analogs and art Artemisinin bundles are given for a broader perspective on structure-activity relationships.

64 citations

Journal ArticleDOI
TL;DR: 7β-hydroxyartemisinin, obtained from microbial transformation, is utilized as a semi-synthetic precursor for the synthesis of novel 7β-substituted art Artemisinin anti-malarial agents.
Abstract: Semi-synthetic derivatives of the anti-malarial drug artemisinin hold great promise in the search for an effective and economical treatment of chloroquine-resistant forms of malaria. Unfortunately, synthetic functionalization of the artemisinin skeleton is often tedious and/or impractical. We seek to utilize 7β-hydroxyartemisinin, obtained from microbial transformation, as a semi-synthetic precursor for the synthesis of novel 7β-substituted artemisinin anti-malarial agents. Here we employ liquid cultures of Cunninghamella elegans as a means for the rational and economical bioconversion of artemisinin to 7β-hydroxyartemisinin in 78.6% yield. In addition, there were three other bioconversion products: 7β-hydroxy-9α-artemisinin (6.0%), 4α-hydroxy-1-deoxoartemisinin (5.4%), and 6β-hydroxyartemisinin (6.5%).

56 citations

Journal ArticleDOI
TL;DR: Transformation of the anti-malarial drug artemisinin by the fungi Eurotium amstelodami and Aspergillus niger were investigated and metabolites from each fungal extract were isolated and identified using mass spectrometry and nuclear magnetic resonance.
Abstract: Transformation of the anti-malarial drug artemisinin by the fungi Eurotium amstelodami and Aspergillus niger were investigated. Cultures were grown in sucrose/malt broth with artemisinin for 14 days and extracted with ethyl acetate. Extracts were characterized by liquid chromatography. Two metabolites from each fungal extract were isolated and identified using mass spectrometry and nuclear magnetic resonance. 5β-hydroxyartemisinin and 7β-hydroxyartemisinin were isolated in 63 and 32% yields, respectively, from the extract of E. amstelodami, and 80 and 19%, respectively, from the extract of A. niger.

38 citations


Cited by
More filters
Journal Article
TL;DR: In this paper, the authors explore recent advances in the design and engineering of materials wholly or principally constructed from peptides, and focus on materials that are able to respond to changes in their environment (pH, ionic strength, temperature, light, oxidation/reduction state, presence of small molecules or the catalytic activity of enzymes) by altering their macromolecular structure.
Abstract: This article explores recent advances in the design and engineering of materials wholly or principally constructed from peptides. We focus on materials that are able to respond to changes in their environment (pH, ionic strength, temperature, light, oxidation/reduction state, presence of small molecules or the catalytic activity of enzymes) by altering their macromolecular structure. Such peptide-based responsive biomaterials have exciting prospects for a variety of biomedical and bionanotechnology applications in drug delivery, bio-sensing and regenerative medicine.

452 citations

Journal ArticleDOI
TL;DR: Propargylamines have been synthesized by a gold(III) salen complex-catalyzed three-component coupling reaction of aldehydes, amines, and alkynes in water in excellent yields at 40 degrees C with excellent diastereoselectivities.

311 citations

Journal ArticleDOI
TL;DR: Evidence for each mechanism of action attributed to artemisinin includes interference with parasite transport proteins, disruption of parasite mitochondrial function, modulation of host immune function and inhibition of angiogenesis, and the evidence for each is reviewed.

298 citations

Journal ArticleDOI
TL;DR: Preliminary investigations suggest that the chiral catalyst may serve as a bifunctional reagent by interacting with both a carboxylic acid nucleophile and NBS electrophile.
Abstract: A catalytic enantioselective syn-1,4-bromolactonization of conjugated (Z)-enynes was reported. Diastereomeric ratios >20:1 and up to 99% enantiomeric excesses were observed. Di-, tri-, and tetra-substituted bromoallenes were prepared together with lactone heterocycles efficiently and stereoselectively. Preliminary investigations suggest that the chiral catalyst may serve as a bifunctional reagent by interacting with both a carboxylic acid nucleophile and NBS electrophile.

286 citations