A number of (aminoalkyl)-l,2-closo-dodecaboranes have been synthcsized to provide arborants with a functional group for covalent incorporation into structures of potential use in the treatment of cancer by boron neutron capture therapy (BNCT). acetylenes reacted with decaborane to give the corresponding carboranes; removal of the phthalimido group under mild conditions using sodium borohydride in 2-propanol furnished the (aminoalky1)carborancs which were isolated as their hydrochloride salts. An alternative approach involved the conversion of an (iodoalky1)or a ((tosy1oxy)alkyl)carborane to the azido derivative which gave the amine on hydrogenation. An effective way of attaching a carborane moiety to thiouracil, which is selectively taken up in melanoma cells, is illustrated by the acylation of two of these amines with thiouracil-5-carboxylic acid.
Synthesis of novel nonionic surfactants has attracted attention of synthetic chemists due to the issues of the currently used commercial surfactants. The synthesis of three biocompatible triazole‐based nonionic surfactants is reported for nanovesicular drug loading. The surfactants were synthesized in a three‐step reaction and characterized using 1HNMR and mass spectroscopy techniques. They were investigated for their critical micelle concentration (CMC) using a UV–Visible spectrophotometer. Their biocompatibility was investigated against cell culture and in blood. All the synthesized nonionic surfactants were further explored for their nanovesicular drug loading using clarithromycin as a model hydrophobic drug. Nonionic surfactants revealed lower CMC in 35–45 μM and were less hemolytic and cytotoxic. They were capable of self‐assembling in nanosize niosomal vesicles encapsulating increased amounts of drug. The results suggest the synthesized nonionic surfactants as biocompatible nanotechnology‐based drug‐delivery vehicles.
In this research work Semicarbazide, thiosemicarbazide derivatives 3 to 25 were synthesized by conventional methods with high percentage yield and reaction rate. 1H-NMR and EIMS spectroscopic techniques were used to elucidate the structure of the synthesized compounds. The effect of thiosemicarbazide and semicarbazide derivatives as an antioxidant agents were studied by DPPH free radical scavenging, ferric ion reducing, ferrous ion chelating assays. Higher DDPH radical scavenging activity exhibited by most of the compounds as compared to standard vitamin C. Excellent ferric ion reducing activity was indicated by compounds of theseriesas compared to standard vitamin C. However most of the compounds generally showed average ferrous ion chelating activity than standard EDTA.
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Current study is focused to synthesize 4-Bromobenzohydrzide detivatives (1-29) and were examined for α-amylase enzyme inhibitory potential at various concentrations. 4-Bromobenzoic acid hydrzide detivatives (1-29) were synthesized via three stpers reaction from 4-bromobenzoic acid. Esterification was done by refluxing in MeOH for 2 hr in the presence of of concentrated H2SO4 till dissolution. In second step methyl 4-bromobenzoate and hydrazine hydrate in excess (1:5) was refluxed in methanol. 4-Bromobenzohydrazide hydrazones were synthesized by the condensation reaction of substituted aryl aldehydes and 4-bromobenzohydrazide in the presence of ethanol and glacial acetic acid. All synthesized derivatives demonstrated good inhibitory activities in the range of IC50= 0.217±0.012-5.5±0.019 as compared to standard Acarbose having IC50 = 1. 34 ± 0. 019. Out of twenty nine (29) derivatives, only five (05) compounds 23 8, 24, 9, and 13 showed less activity than the standard. Results of the enzyme inhibition its self showed that the activity of this library is due to the core structure. The slightly changes in activity is might be due to the different substitutions and position of the substitution. Furthermore; molecular docking study was performed in order to explore the possible binding mode of the synthesized compounds against α-amylase enzyme.
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