Artemisinin (1) and its analogues have been well studied for their antimalarial activity. Here we present the activity of some novel C-9-modified artemisinin synthesized using artemisitene as key intermediate. Further, antileishmanial more than 70 derivatives against Leishmania donovani promastigotes is described first time. A comprehensive structure−activity relationship study CoMFA discussed. These exhibited leishmanicidal in micromolar concentrations, overall profile appears to be similar...

Abstract Hydrogen sulfide (H 2 S) is emerging as an important gasotransmitter in both physiological and pathological states. Rapid measurement of H S remains a challenge. We report microfluidic method for rapid sulphide blood plasma using Dansyl-Azide, fluorescence (FL) based probe. have measured known quantities externally added (exogenous) to buffer human plasma. Surprisingly, decrease FL intensity with increase exogenous concentration was observed which attributed the interaction between...

The present study focuses on exploring the physical properties of lipid membranes based polyhydroxy oxanorbornane (PH-ONB) headgroup, designed as synthetic analogues naturally occurring archaeal membranes. Specifically, we two variants PH-ONB headgroup-based lipids differing in number hydroxy groups with one having (ONB-2OH) and other three (ONB-3OH). These form stable bilayer begins a comprehensive analysis fluorescence characteristics nitrobenzoxadiazole (NBD)-tagged ONB-based different...

The usefulness of SmCl3 as an excellent catalyst for chemoselective esterifications and selective removal acid sensitive protecting groups such Boc, THP, TBDMS in the presence one another is demonstrated through suitable examples.

The AC susceptibility and the low-field magnetisation measurements on disordered spinel system ZnxCo1-xFeCrO4 (x=0.0, 0.2, 0.4, 0.5, 0.8) are reported. X-ray analysis shows that lattice parameter a minimum at x=0.5, indicating redistribution of cations in A B sites introduction Zn2+. DC magnesidation indicate two transitions for x=0.0 0.2 while only one x>or=0.4. high-temperature peak chi corresponds to ferrimagnetic transition TN. magnetic phase below lower-temperature Tf could be...

The authors report here on X-ray diffraction, magnetic hysteresis, resistivity and thermoelectric power measurements carried out at different temperatures for the system GexFe1-xNiCrO4(x=0.0, 0.2, 0.4, 0.6, 0.8 1.0), which crystallises with a spinel structure. On basis of site-preference energy values individual cations (as given by Miller, Smit Wijn) cation distribution is expected to be (Gax3+Fe1-x3+) (Ni2+Cr3+)-O4, Ga3+ Fe3+ ions being A sites Ni2+ Cr3+ B sites, thus providing selective...

Anti or gauche? trans-β2,3-Amino acid residues that are known to promote extended structures in their peptides show specific rotamer preferences response an intramolecular hydrogen-bonding possibility, which facilitates the 11-helical 1:1 α,β-hybrid (see figure). Preferences for gauche conformation all internal β and anti C-terminal residue these were confirmed by NMR spectroscopic X-ray diffraction experiments. Detailed facts of importance specialist readers published as "Supporting...

Disordered spinel ferrites exhibit relaxation behaviour in their Mossbauer spectra. The results of the low-field magnetisation measurements on a representative system show for first time that undergoes ferrimagnetic transition at TN and then, cooling, enters into cluster spin-glass state below Tf with different clusters randomly frozen. observed features spectra could be related to instability higher temperatures.

A convenient synthetic approach toward nucleoside analogs where beta-hydroxyphosphonate- or 1,2-dihydroxy units are connected to the nucleic acid base through a triazole spacer is discussed.

This report introduces N-methylpyrrolidone hydroperoxide (NMPOOH)/base as an excellent reagent system for hydroxy-directed syn selective epoxidation of electron-deficient olefins, characterized by high diastereoselectivity, short reaction times and remarkable chemoselectivity, especially in presence oxidatively labile nitrogen or sulfur atoms. NMPOOH also proves efficient the oxidation aromatic aldehydes, removal oxazolidinone chiral auxiliary, functionalization alkenes alkynes, showing wide...

Achiral amphiphiles with hydroxylated oxanorbornane headgroups showed specific morphological characteristics and hierarchical preferences depending upon the nature of lipophilic units. Detailed scanning electron microscopic (SEM) studies that twisted ribbonlike aggregates are characteristic monoalkoxyaryl lipids hydrocarbon chain length in range C10-C13; these systems also had a preference toward lamellar arrangement. Asymmetric packing is unique occurrence shows presence molecular chirality...

Biocatalysis of artemisinin by different strains Mucor ramannianus.* illustrates a simple approach to bioengineering for attaining useful biotransformation preparative or downstream development. Three M. ramannianus. on the malt/sucrose medium were compared their native ability metabolize antimalarial and produce significant yields hydroxylated derivatives. The transformed into metabolites, in particular 7β.-hydroxyartemisinin at 88% yield 6β.-hydroxyartemisinin 51% yield.

The microbial metabolism of 10-deoxoartemisinin (1), a derivative the antimalarial drug artemisinin, was investigated. Various strains fungi were investigated for their ability to transform 1. Of these microorganisms, only Cunninghamella elegans capable transforming 1 5β-hydroxy-10-deoxoartemisinin (2), 4α-hydroxy-1,10-deoxoartemisinin (3), and 7β-hydroxy-10-deoxoartemisinin (4). metabolites 2 4 retained an intact peroxide group are therefore useful scaffolds synthetic modification in search...

A novel reaction pathway involving 1,3-diketones and 2,2′-dithiodibenzoylchloride that gives access to benzothiophenes with spiroketal, lactone, carbonyl, hydroxyl carboxylic acid functionalities is discussed.

Anticancer activities of a series benzisothiazolones having alkyl, aryl and aralkyl substituents on the nitrogen atom mechanistic basis cytotoxicity are presented. Cellular responses like DNA laddering, disruption mitochondrial membrane potential caspase-3 activation incubation HeLa cells with representative compounds from this group suggested induction apoptosis through an intrinsic pathway. Their ability to arrest cell cycle at G2/M phase was confirmed by flow cytometric analysis.

A simple replacement of a H atom by Br transformed non-gelating aryl triazolyl amino acid benzyl ester to versatile gelator, which formed shape-persistent, self-healing and mouldable gels.