Bioreduction mediated by plants is a highly selective and environmentally friendly approach to synthesise optically active alcohols. Herein the bioreduction of 1-(3,4)-dimethylphenyl)ethanone to the corresponding chiral alcohol 1-(3,4-dimethylphenyl)ethanol has been evaluated using nine differen...
The effect of temperature on the fluorescence intensity of 4-(5-methyl-3-furan-2-yl-benzofuran-2-yl)-7-methyl-chromen-2-one (MFBMC) in different solvents, has been studied in the temperature range 293–333 K. A mechanism of fluorescence quenching with increase in temperature is discussed in term...
Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly desirable for implementing malaria elimination strategies. MMV019918 (1, 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine) was selected from the MMV Malaria Box for its dual activity...
A BINOL-phosphoric acid-catalyzed furylogous Pinacol rearrangement is developed. This reaction produces spiro cyclopentanone in good yields under mild conditions. The enantioselective version of this reaction is also investigated using chiral phosphoric acid (CPA) as the catalyst.
A novel series of 1-{[3-(furan-2-yl)-5-substituted phenyl-4,5-dihydro-1,2-oxazol-4-yl]methyl}-4-methyl piperazine, compounds 3a–l have been synthesized. The synthetic work was carried out beginning from 2-acetylfuran through Claisen Schmidt condensation with different types of aromatic aldehyde...
Protic ionic liquids (PILs) composed of N-alkyl (= hexyl, octyl and 2-ethylhexyl) ethylenediaminum cation with trifluoromethanesulfonate (TFS) or trifluoroacetate (TFA) anion such as HOct(TFA), HEtHex(TFA), HHex(TFS), HOct(TFS) and HEtHex (TFS) were newly synthesized and HHex(TFA) was synthesize...
Tuberculosis (TB) is a major infectious disease associated increasingly with drug resistance. Thus, new anti-tubercular agents with novel mechanisms of action are urgently required for the treatment of drug-resistant TB. In prior work, we identified compound 1 (cyclohexyl(4-(isoquinolin-5-ylsulf...
A series of novel benzisothiazolylpiperazine derivatives combining potent dopamine D2 and D3, and serotonin 5-HT1A and 5-HT2A receptor properties were synthesized and evaluated for their potential antipsychotic properties. The most-promising derivative was 9j. The unique pharmacological features...
SummaryBackground & aimsCancer cachexia (CC) syndrome and anorexia–cachexia syndrome are common terms used to describe changes in metabolism with increased inflammatory activity and can progressively develop through various stages such as pre-cachexia; cachexia; and refractory cachexia. Therefo...
Correlation between Fe content and z value on the structural and magnetic properties of the Sm(CobalFexCu0.06Zr0.025)z magnets (x = 0.20, 0.25, 0.28, and z = 7, 9.5) has been investigated. It is found that the cellular phases in the magnets grow up with increasing Fe content, so the cell boundar...
The software z-Tree is used for thousands of economic experiments worldwide. z-Tree stores experimental data in a way that minimizes the risk of losing data. However, it may be cumbersome to manually read this data into a statistical package. The purpose of the R-package zTree is to make the pro...
The polar flagella of Vibrio alginolyticus are driven by sodium motive force and those motors are specifically and strongly inhibited by phenamil, an amiloride analog that is thought to interact with a sodium channel of the flagellar motor. To study the sodium ion coupling site, we isolated moti...
Inducing differentiation and maturation of resident multipotent stem cells (MSCs) is an important strategy to regenerate hard tissues in mal-calcification conditions. Here we explore a co-delivery approach of therapeutic molecules comprised of ion and drug through a mesoporous bioglass nanoparti...
ALK and ROS1 kinases have become promising therapeutic targets since Crizotinib was used to treat non-small-cell lung cancer clinically. Aiming to explore new potent inhibitors, a series of 2-amino-4-(1-piperidine) pyridine derivatives that stabilized a novel DFG-shifted conformation in the kina...
Janus kinases (JAKs) regulate various cancers and immune responses and are targets for the treatment of cancers and immune diseases. A new series of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives were synthesized and optimized by introducing a functional 3,5-disubstituted-1H-pyrazole moiety int...
A series of 4-aminoquinazolines derivatives containing hydrophilic group were designed and identified as potent Pan-PI3K inhibitors in this study. The results of antiproliferative assays in vitro showed that this series of compounds had strong inhibition of tumor growth, especially compound 7b f...
A series of tin(IV) and organotin(IV) hydridotris(4-bromo-1H-pyrazol-1-yl)borates has been prepared. The compounds of general formula RnSnCl4−n−1[HB(4-Br-pz)3] (where R = Me or Ph, n = 0, 1, 2, or 3) are rigid in solution and contain a six-coordinate tin(IV) site with a tridentate ligand. They w...
A total of 13 new co-ordination solids have been prepared of composition [Co(HBTC)(PHEN)(H2O)] (12), [Mn3(BTC)2(PHEN)3] (13), [Mn(HBTC)(6)(H2O)] (14), [Mn(HBTC)(7)(H2O)] (15), [Zn3(BTC)2(6)3(H2O)3]·4H2O (16), [Zn(HBTC)(6)(H2O)] (17), [Zn(H2BTC)2(6)] (18), [Zn(HBTC)(7)(H2O)] (19), [Zn(HBTC)(8)(H...
A series of metal complexes M[HB(4-Brpz)3]2 [HB(4-Brpz)3 = hydridotris(4-bromo-1H-pyrazol-1-yl)borate and M = Mn, Fe, Co, Ni, Cu, Zn, Cd, Pb] were obtained from reaction of K[HB(4-Brpz)3] and the appropriate metal salt in aqueous solution. These air-stable complexes are sparingly soluble in most...