| Literature DB >> 30034597 |
Renjitha Jalaja1,2, Shyni G Leela3, Praveen K Valmiki1,2, Chettiyan Thodi F Salfeena1,2, Kizhakkan T Ashitha1,2, Venkata Rao D Krishna Rao4, Mangalam S Nair1, Raghu K Gopalan3,2, Sasidhar B Somappa1,2.
Abstract
Obesity contributes to the genesis of many metabolic disorders including dyslipidemia, coronary heart disease (CHD), nonalcoholic fatty liver, type 2 diabetes, etc. Pancreatic lipase plays a vital role in food fat digestion and absorption. Therefore, to control obesity, inhibition of pancreatic lipase is the active therapy. Thus, novel natural product derived labdane appended triazoles with pancreatic lipase inhibition potential were designed and synthesized. Among these hybrids, 6b and 6f exhibited excellent inhibitory activity (IC50 0.75 ± 0.02 μM and 0.77 ± 0.01 μM), slightly better than that of the positive control Orlistat (IC50 0.8 ± 0.03 μM). Compounds 6c, 6e, and 6g-j inhibited the PL comparable to that of positive control. Interestingly none of the compounds showed cytotoxicity (Hep G2) in the concentration range from 0.5 to 100 μM. Overall results reveal the potential of labdane appended triazoles as antiobesity agents.Entities:
Year: 2018 PMID： 30034597 PMCID： PMC6047173 DOI： 10.1021/acsmedchemlett.8b00109
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345