PMID- 23074549 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20121018 LR - 20211021 IS - 2070-5204 (Electronic) IS - 1999-768X (Print) IS - 1999-768X (Linking) VI - 27 IP - 5 DP - 2012 Sep TI - Synthesis and Anti-hyperlipidemic Activity of 3H-benzo [4, 5] thieno [2, 3-d] [1, 2, 3] triazin-4-ones: Possible Mechanism of Altered Lipid Metabolism. PG - 388-95 LID - 10.5001/omj.2012.96 [doi] AB - OBJECTIVES: The present study was aimed to evaluate the anti-hyperlipidemic activity of newly synthesized tricyclic benzothieno 1, 2, 3-triazine derivatives namely CP-1 (3-(methyl)- 5,6,7,8-tetrahydro,3H-benzo[4,5] thieno [2,3-d][1,2,3] triazin-4-one), CP-2 (3-(ethyl)- 5,6,7,8-tetrahydro,3H-benzo[4,5] thieno [2,3-d][1,2,3] triazin-4-one) and CP-6 (3-(2-chloro phenyl)-5,6,7,8-tetrahydro,3H-benzo[4,5] thieno [2,3-d][1,2,3] triazin-4-one) against dexamethasone and Triton WR-1339-induced hyper-lipidemia in rats. METHODS: Anti-hyperlipidemic activity of the test compounds were evaluated against dexamethasone (10 mg/kg, subcutaneous [s.c.]) and Triton WR-1339 (200 mg/kg, intraperitoneal [i.p]) induced hyperlipidemia in rats. RESULTS: Administration of single dose of Triton WR-1339 (200 mg/kg i.p) and dexamethasone (10 mg/kg s.c.) for 8 consecutive days to adult wistar rats caused severe hyperlipidemia characterized by marked increase in serum cholesterol, LDL-C, VLDL-C and triglyceride levels along with an increase in atherogenic index. Serum HDL-C levels were decreased significantly compared to normal control. Pretreatment with Atorvastatin (10 mg/kg, p.o.), CP-1 (25 and 50 mg/kg), CP-2 (25 and 50 mg/kg) and CP-6 (25 and 50 mg/kg) showed significant and dose-dependent protection against dexamethasone and Triton WR-1339-induced hyperlipidemia in rats by maintaining serum total cholesterol, LDL-C, VLDL-C and HDL-C levels within the normal range. Also, a significant decrease in atherogenic index was observed. The anti-hyperlipidemic effect of CP-6 was comparable with reference standard Atorvastatin. Furthermore, CP-6 was found to be more potent than CP-1 and CP-2. CONCLUSION: These findings suggest that CP-1, CP-2 and CP-6 possess significant anti-hyperlipidemic activity against experimental animal models of hyperlipidemia. FAU - Viswanatha, Gollapalle L AU - Viswanatha GL AD - Department of Pharmacology, PES College of Pharmacy, Bangalore-560050. CN - Janaki Priyadarshini B FAU - Hanumanthappa, Shylaja AU - Hanumanthappa S FAU - Rangappa, Srinath AU - Rangappa S FAU - Janardhanan, Saravanan AU - Janardhanan S LA - eng PT - Journal Article PL - Oman TA - Oman Med J JT - Oman medical journal JID - 101526350 PMC - PMC3472570 OTO - NOTNLM OT - 1, 2, 3-Triazine-4-ones OT - Dexamethasone OT - Diazotization OT - Gewald reaction OT - Hyperlipidemia OT - Thiophenes OT - Triton WR-1339 EDAT- 2012/10/18 06:00 MHDA- 2012/10/18 06:01 PMCR- 2012/09/01 CRDT- 2012/10/18 06:00 PHST- 2012/04/02 00:00 [received] PHST- 2012/06/25 00:00 [accepted] PHST- 2012/10/18 06:00 [entrez] PHST- 2012/10/18 06:00 [pubmed] PHST- 2012/10/18 06:01 [medline] PHST- 2012/09/01 00:00 [pmc-release] AID - OMJ-D-12-00025 [pii] AID - 10.5001/omj.2012.96 [doi] PST - ppublish SO - Oman Med J. 2012 Sep;27(5):388-95. doi: 10.5001/omj.2012.96.