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Synthesis and in vitro bio-activity evaluation of N4-benzyl substituted 5-chloroisatin-3-thiosemicarbazones as urease and glycation inhibitors
- Source :
- Acta Chimica Slovenica, Vol 65, Iss 1, Pp 108-118 (2018)
- Publication Year :
- 2018
- Publisher :
- Slovenian Chemical Society, 2018.
-
Abstract
- A series of fifteen N4-benzyl substituted 5-chloroisatin-3-thiosemicarbazones 5a–o were synthesized and screened mainly for their antiurease and antiglycation effects. Lemna aequinocitalis growth and Artemia salina assays were carried out to determine their phytotoxicity and cytotoxicity potential. All the compounds proved to be extremely effective urease inhibitors, demonstrating enzyme inhibition much better than the reference inhibitor, thiourea (IC50 values 1.31 ± 0.06 to 3.24 ± 0.15 vs. 22.3 ± 1.12 μM). On the other hand, eight out of fifteen compounds tested, i.e. 5b, 5c, 5h–k, 5m and 5n were found to be potent glycation inhibitors. Of these, five viz. 5c, 5h–j and 5n proved to be exceedingly efficient, displaying glycation inhibition greater than the reference inhibitor, rutin (IC50 values 114.51 ± 1.08 to 229.94 ± 3.40 vs. 294.5 ± 1.5 μM).
Details
- Language :
- English
- ISSN :
- 13180207 and 15803155
- Volume :
- 65
- Issue :
- 1
- Database :
- Directory of Open Access Journals
- Journal :
- Acta Chimica Slovenica
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.7fe69c52abcf4eed96d4fd372248f940
- Document Type :
- article
- Full Text :
- https://doi.org/10.17344/acsi.2017.3649