Synthesis crystal structure of 2-methoxybenzoylhydrazones and evaluation of their α-glucosidase and urease inhibition potential

• Published in: Medicinal Chemistry Research
• Main Author: Taha M.; Ismail N.H.; Baharudin M.S.; Lalani S.; Mehboob S.; Khan K.M.; Yousuf S.; Siddiqui S.; Rahim F.; Choudhary M.I.
• Format: Article
• Language: English
• Published: Birkhauser Boston 2015
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84934852218&doi=10.1007%2fs00044-014-1213-8&partnerID=40&md5=f9766e8be167226cebc66a658178de74
• ISSN: 10542523
• DOI: 10.1007/s00044-014-1213-8

Compounds 1-30 showed varying degree of α-glucosidase inhibition with IC50 values ranging between 187 and 420 μM. Compounds 1, 2, 3, 6, 8, 12, and 4 (IC50 = 187.7 ± 3.05, 203.4 ± 4.0, 240.7 ± 1.9, 252.9 ± 3.9, 285.2 ± 6.3, 399.07 ± 1.2, and 420.36 ± 5.6 μM, respectively) were found to be more active than standard acarbose (IC50 = 906 ± 6.3 μM). The synthetic compounds were also tested for urease inhibition. Compounds 5 (IC50 = 19.6 ± 1.0 μM) and 1 (IC50 = 21.6 ± 0.6 μM) showed better activity than standard drug thiourea (IC50 = 21.8 ± 1.6 μM). The crystal structures of compounds 15 and 16 are also reported. Graphical Abstract: Compounds 1-30 synthesized and evaulated for Alpha-glucosidase as well as Ureas inhibition. The crystal structures of compounds 15 and 16 are also reported[Figure not available: see fulltext.] © 2014 Springer Science+Business Media New York.