Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

Semisynthetic artemisinins and other bioactive peroxides are best known for their powerful antimalarial activities, and they also show substantial activity against schistosomes - another hemoglobin-degrading pathogen. Building on this discovery, we now describe the initial structure-activity relationship (SAR) of antischistosomal ozonide carboxylic acids OZ418 (2) and OZ165 (3). Irrespective of lipophilicity, these ozonide weak acids have relatively low aqueous solubilities and high protein binding values. Ozonides with para-substituted carboxymethoxy and N-benzylglycine substituents had high antischistosomal efficacies. It was possible to increase solubility, decrease protein binding, and maintain the high antischistosomal activity in mice infected with juvenile and adult Schistosoma mansoni by incorporating a weak base functional group in these compounds. In some cases, adding polar functional groups and heteroatoms to the spiroadamantane substructure increased the solubility and metabolic stability, but in all cases decreased the antischistosomal activity. © 2020 American Chemical Society.

World University root node

Department of Chemistry

School of Advanced Sciences

Vellore Campus

Fulltext

Journal of Medicinal Chemistry

Structure-Activity Relationship of Antischistosomal Ozonide Carboxylic Acids

Building on insights gained from the discovery of the antimalarial ozonide arterolane (OZ277), we now describe the structure-activity relationship (SAR) of the antimalarial ozonide artefenomel (OZ439). Primary and secondary amino ozonides had higher metabolic stabilities than tertiary amino ozonides, consistent with their higher pKa and lower log D7.4 values. For primary amino ozonides, addition of polar functional groups decreased in vivo antimalarial efficacy. For secondary amino ozonides, additional functional groups had variable effects on metabolic stability and efficacy, but the most effective members of this series also had the highest log D7.4 values. For tertiary amino ozonides, addition of polar functional groups with H-bond donors increased metabolic stability but decreased in vivo antimalarial efficacy. Primary and tertiary amino ozonides with cycloalkyl and heterocycle substructures were superior to their acyclic counterparts. The high curative efficacy of these ozonides was most often associated with high and prolonged plasma exposure, but exposure on its own did not explain the presence or absence of either curative efficacy or in vivo toxicity. © 2017 American Chemical Society.

Structure–Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439)

Ellagic acid (EA) is a lactone and polyphenolic functional groups-containing phyto-chemical that has been widely used as an anti-oxidant, anti-cancer and anti-aging cosmetic agent. EA is known as a stable redox active system only in organic medium, but irreversibly oxidized with coupled chemical reactions showing ill-defined redox peaks in aqueous solutions. Interestingly, we report here that electro-oxidation of EA tethered multiwalled carbon nanotube-modified glassy carbon electrode (GCE/MWCNT@EA) showed a well-defined pair of redox peaks with a surface-confined characteristics at Ef = 0.020 V vs Ag/AgCl corresponding to ortho-quinone moiety of oxidized EA in pH 7 phosphate buffer solution (PBS). No such behavior was noticed with EA adsorbed GCE. The GCE/MWCNT@EA was characterized by cyclic voltammetery (CV) and the transfer coefficient (α) and electrode to redox surface layer electron transfer rate constant (ks) were calculated. Physicochemical characterization of MWCNT@EA by FTIR, XRD and Raman Spectroscopy techniques revealed immobilized EA in its native form on MWCNT. Effect of various CNTs on EA electro-immobilization and the features that distinguish each other was highlighted. The GCE/MWCNT@EA showed excellent electrocatalytic activity toward N2H4 oxidation. The mechanism and kinetics of the catalytic reaction was investigated by CV, and the kinetic parameters ca., number of electrons in the rate determining step (na′), total number of electrons (n′), reaction order with respect to N2H4, catalyst reaction rate constant (kchem) were evaluated. Finally, amperometric i-t and flow injection analysis for highly selective sensing of hydrazine without any interference from other biochemicals were validated. © 2016 Elsevier B.V.

VIT Unitversity

Journal of Electroanalytical Chemistry

Electrochemical immobilization of ellagic acid phytochemical on MWCNT modified glassy carbon electrode surface and its efficient hydrazine electrocatalytic activity in neutral pH

Developments of new decomposition or degradation methods of environmentally hazardous azo dyes from textile industries are very important. Usually, strong acid-based chemical/electrochemical and neutral pH-based bacterial decomposition methods were widely used. Here, we report a mild, simple, and facile electrochemical method for decomposition of azo dye (Sudan yellow; SY) into a highly redox active copolymer of polyanilines via aniline derivatives as intermediates on a MWCNT modified glassy carbon electrode (GCE/MWCNT) surface unusually in a neutral pH using phosphate buffer solution (PBS) (GCE/MWCNT@SY-CoPANIpH7). One of the intermediate products, aniline (Mw = 93 mol g-1, calculated) was identified by an in situ cyclic voltammetry-electrochemical quartz crystal balance experiment. No such SY electrochemical reaction was observed on a naked GCE surface. Physico-chemical characterizations by TEM, Raman, IR, and UV-vis spectroscopic methods supported the formation of polymeric product on MWCNT surface (GCE/MWCNT@SY-CoPANIpH7). Electroanalytical performance of this new electrode was tested using ascorbic acid (AA) and Fe(CN)63-, as models. Interestingly, a dilute solution of Nafion (Nf) casted modified electrode system (GCE/MWCNT@SY-CoPANIpH7/Nf) showed improved electroanalytical performance, unlike the conventional Nafion modified system (GCE/MWCNT/Nf) with vanished peak current response due to the electrostatic repulsive interaction between the anionic AA (pKa = 4.10), Fe(CN)63- ion, and anionic sulfonic acid groups in Nafion. A zwitter ionic complex between a polaronic copolyaniline and sulfonic acid of Nafion is proposed as a possible structure for the newly developed hybrid system. Using the GCE/MWCNT@SY-CoPANIpH7/Nf, a selective flow injection analysis of AA has been demonstrated as an analytical application with good recovery values. © 2015 American Chemical Society.

Department of Database Systems

School of Computer Science and Engineering

The Journal of Physical Chemistry C

An Unusual Electrochemical Reductive Cleavage of Azo Dye into Highly Redox Active Copolymeric Aniline Derivatives on a MWCNT Modified Electrode Surface at Neutral pH and Its Electroanalytical Features