title: Synthesis and antihyperlipidemic activity of some novel 4-(substitutedamino)-5-substituted-3-mercapto- (4H)-1,2,4-triazoles.
abstract: Hyperlipidemia is considered one of the key factors for cardiovascular diseases. Based on earlier work on a series of 5-alkyl-4-aryl-3-mercapto-(4H)-1,2,4-triazoles, for further lead modification, a series of 4-(substituted)amino-5-substituted-3-mercapto-(4H)-1,2,4-triazoles was designed. Target compounds were synthesized by the well known Hoggarth synthesis of substituted 1,2,4-triazoles. Synthesized compounds were screened for lipid lowering activity using the "Poloxamer 407 induced hyperlipidemia in rats" model at a dose of 100 mg/kg p.o. Compounds were found to alter serum lipid levels significantly. Most of the compounds significantly reduced serum cholesterol and triglyceride levels. Some of the compounds were found to reduce triglycerides and elevate high density lipoprotein (HDL) levels more than the standard drug atorvastatin (CAS 134523-03-8). Compounds with chloro substitution on aryl rings were found more active in reducing serum lipid levels than other substitutions.
authors.affiliation: Department of Pharmaceutical Chemistry, L. M. College of Pharmacy, Navrangpura, Ahmedabad, Gujarat, India. mahesh.chhabria@rediffmail.com
authors.forename: Mahesh T
authors.initials: MT
authors.lastname: Chhabria
authors.forename: Bhanubhai N
authors.initials: BN
authors.lastname: Suhagia
authors.forename: Pathik S
authors.initials: PS
authors.lastname: Brahmkshatriya
authors.forename: Priyesha M
authors.initials: PM
authors.lastname: Raval
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002784:Cholesterol / Q000097:blood; D008076:Cholesterol, HDL / Q000097:blood; D002855:Chromatography, Thin Layer; D015195:Drug Design; D005260:Female; D006949:Hyperlipidemias / Q000097:blood / Q000139:chemically induced / Q000188:drug therapy; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D008055:Lipids / Q000097:blood; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D020442:Poloxamer; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D013055:Spectrophotometry, Infrared; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014280:Triglycerides / Q000097:blood
chemical_list: D000924:Anticholesteremic Agents; D008076:Cholesterol, HDL; D000960:Hypolipidemic Agents; D007202:Indicators and Reagents; D008055:Lipids; D013438:Sulfhydryl Compounds; D014230:Triazoles; D014280:Triglycerides; D020442:Poloxamer; D002784:Cholesterol