Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
omega-(2-Naphthyloxy) amino alkanes, obtained as major by-product during course of synthesis of carbamate esters from omega-(2-naphthyloxy) alkyl halides and amines, showed significant anti-hyperglycemic and lipid lowering activities in various test models as a novel class of compounds. Compounds were tested in rat GLM, SLM, STZ, and STZ-S models at 100mg/kg dose. Of these compound 13 was found to be the most active which caused lowering of sugar by 33.6%, 31.0%, 28.5%, and 73.8% in GLM, SLM, STZ, STZ-S, and db/db mice models, respectively. It also significantly effected lowering of LDL in rat model and also in Hamster model without reducing HDL. Most of the compounds showing anti-diabetic and lipid lowering activity have shown promising PPAR-alpha/gamma/delta-activity. Compounds 6, 13, and 19 have shown very good PPAR-alpha/gamma/delta activity.
Chaturvedi
Devdutt
D
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
Ray
Suprabhat
S
Srivastava
Arvind K
AK
Chander
Ramesh
R
D000473:Alkanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000145:classification / Q000494:pharmacology*; D000478:Alkylation; D000586:Amination; D000818:Animals; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000145:classification / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000145:classification / Q000494:pharmacology*; D050356:Lipid Metabolism / Q000187:drug effects; D008297:Male; D015394:Molecular Structure; D009281:Naphthalenes / Q000737:chemistry*; D047495:PPAR gamma / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
D000473:Alkanes; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D009281:Naphthalenes; D047495:PPAR gamma