N-acylated benzyl carbamate with 86% yield was achieved in 20 min of time. Then we examined the reaction conditions in presence of anhydrous cerium Chloride with the same substrates, observed that the reaction learn more was completed within 6 min of time with 95% yield ( Scheme. 2, Entry-1 in Table 2) and decided to go with anhydrous cerium chloride to explore the substrate scope in this case as well. These reaction conditions were success
full while exploring the possibilities with structurally diversed acid anhydrides like propionic, pivalic and benzoic anhydrides. We have examined the same reaction conditions to find out the applicability in case of secondary carbamates like amino acid carbamates and amine carbamates and found positive results. All the results regarding the N-acylation of carbamates were mentioned in Table 2. Synthesized compounds were screened check details for their antifungal activity by anti Malassezia in vitro liquid broth culture in high-throughput assay format for anti-dandruff activity testing against two virulent organisms M. furfur and M. pachydermatis MF-ATCC44338 MP-ATCC42757 were the corresponding strains. The compounds were tested in four replicates in the concentration range of 200 uM, 180 uM, 160 uM, 140 uM, 120 uM, 100 uM, 75 uM, 50 uM,
25 uM, 10 uM and 1 uM by incubating them for stipulated time period of 72 h and taking their growth observations in the form of optical density at 600 nm wavelength at different time intervals. The growth in the treated wells was compared with the growth in the untreated wells. Ketoconazole was used as control, among heptaminol the compounds
screened 2a, 2i and 4a showed activity than the standard antifungal drug i.e. Ketoconazole, corresponding results were mentioned in Table 3. We have developed a novel and efficient method for of N-acylation of sulfonamides and carbamates with carboxylic acid anhydrides under solvent free and mild reaction conditions in presence of cerium (III) chloride. Synthesized compounds were evaluated for their antifungal activity against M. furfur and M. pachydermatis. Three compounds 2a, 2i, and 4a showed very good activity against both the organisms, for the first time N-acyl sulfonamides and carbamates class was evaluated as potential anti-Malassezia agents. This outcome indicates that there is a good scope for evaluation of this class of compounds as potential leads towards anti Malassezia activity. All authors have none to declare. “
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