title: Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice.
abstract: A series of propiophenone derivatives (6-23) have been synthesized and evaluated for their in vivo antihyperglycemic activities in sucrose loaded model (SLM), sucrose challenged streptozotocin (STZ-S) induced diabetic rat model and C57BL/KsJ db/db diabetic mice model. Compound 15 and 16 were emerged as potent antihyperglycemics and lipid lowering agents. These compounds (15, 16) further validate the potency by reducing body weight and food intake in db/db mice model. Possible mechanism of action for the propiophenone derivatives was established by the evaluation in various in vitro models. Interestingly some of the compounds were efficiently inhibiting PTP-1B.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Council of Scientific and Industrial Research, Lucknow 226 001, India. dratulsax@gmail.com
authors.forename: Atul
authors.initials: A
authors.lastname: Kumar
authors.forename: Siddharth
authors.initials: S
authors.lastname: Sharma
authors.forename: Lalit Prakash
authors.initials: LP
authors.lastname: Gupta
authors.forename: Pervez
authors.initials: P
authors.lastname: Ahmad
authors.forename: Swayam Prakash
authors.initials: SP
authors.lastname: Srivastava
authors.forename: Neha
authors.initials: N
authors.lastname: Rahuja
authors.forename: A K
authors.initials: AK
authors.lastname: Tamrakar
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism; D004435:Eating / Q000187:drug effects; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D008055:Lipids / Q000097:blood; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D011427:Propiophenones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D013311:Streptozocin; D015431:Weight Loss / Q000187:drug effects*
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D008055:Lipids; D011427:Propiophenones; D013311:Streptozocin; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1