The reaction of 2-(4-bromo phenyl) methyl cyanide (1a) with ethylchloroformate in the presence of n-butyl lithium gave ethyl-2-(4-bromo phenyl)-2-cyano acetate (2a). 2a on reduction with sodium borohydride yields 3-amino-2-(4-bromo phenyl) propan-1-ol (3a). Compound 3a on further reaction with tert butyloxy anhydride in presence of triethylamine afford tert-butyl-2-(4-bromo phenyl)-3hydroxy propyl carbamate (4a). 4a on treatment with tosyl chloride gave 2-(4-bromo phenyl)-3-(tertiarybutyloxy carbonyl amino)-propan-1-ol-(4-toluene sulphonate) (5a). Compound 5a on cyclization followed by hydrolysis gave 3-(4-bromo phenyl) azetidine (7a). Compounds 2b-2e, 3b-3e, 4b-4e, 5b-5e, 6b-6e and 7b-e were synthesized by a similar method. The compounds are characterized by elemental analysis, IR, 1 H NMR and Mass spectral analysis and screened for antimicrobial activity.
). -Compounds (IIId-f) and (VIf) exhibit moderate to good antibacterial activities against S. aureus and E. coli. -(NAGARAJU, V.; SRINIVASULU, R.; DORASWAMY, K.; RAMANA*, P. V.; J.
The 2-methacryloxyacetophenone (MAP) was prepared and subjected to suspension polymerization with divinylbenzene (DVB). The differently sulfonated MAP-DVB cross-linked copolymer cationic exchange resins were prepared by sulfonation with a fixed volume of concentrated sulfuric acid in an oil bath at 70 o C. Several characteristics of the prepared resins were evaluated, i.e. Fourier transform infrared spectra, the ion-exchange capacity, and microscopic morphology. The resin characteristics were altered with degree of sulfonation, providing that differently sulfonated resins could be prepared. The behavior of Fexofenadine hydrochloride loading and in vitro release in the USP stimulated gastric and intestinal fluids of the obtained resins were evaluated. The drug loaded in the resin increased with increasing degree of sulfonic group and hence the drug binding site in resin employed. The drug release was lower from the resins with higher degree of sulfonic group due to the increase in the diffusive path depth. The drug release was a little lower in stimulated gastric fluid (SGF) than stimulated intestinal fluids. The basic group, ionized to a little greater extent in SGF and preferred binding with the resin rather than releasing. Hence, the differently sulfonated resins could be utilized as novel carriers for drug delivery.
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