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Volumn 20, Issue 10, 2010, Pages 3065-3069

Synthesis of novel benzocoumarin derivatives as lipid lowering agents

Author keywords

Anti dyslipidemia; Antioxidant; Benzocoumarins; Cholesterol lowering; Synthesis

Indexed keywords

(4 METHYL 2 OXO 2H BENZO[H]CHROMEN 7 YLOXY)ACETIC ACID ETHYL ESTER; 4 METHYL 7 (1 PHENYLETHOXY)BENZO[H]CHROMEN 2 ONE; 4 METHYL 7 OXIRANYLMETHOXY BENZO[H]CHROMEN 2 ONE; 7 (2 HYDROXY 3 PHENYLAMINOPROPOXY) 4 METHYL BENZO[H]CHROMEN 2 ONE; 7 (2 HYDROXY 3'4 TOLYLAMINOPROPOXY) 4 METHYL BENZO[H]CHROMEN 2 ONE; 7 (3 CHLORO 2 HYDROXYPROPOXY) 4 METHYL BENZO[H]CHROMEN 2 ONE; 7 [2 HYDROXY 3 (4 METHOXYPHENYLAMINO)PROPOXY] 4 METHYL BENZO[H]CHROMEN 2 ONE; 7 [3 (4 FLUOROPHENYLAMINO) 2 HYDROXYPROPOXY] 4 METHYL BENZO[H]CHROMEN 2 ONE; 7 BENZYLOXY 4 METHYL BENZO[H]CHROMEN 2 ONE; ALLOPURINOL; ALPHA TOCOPHEROL; ANSECULIN; ANTILIPEMIC AGENT; BENZOCOUMARIN DERIVATIVE; CALANOLIDE A; CHOLESTEROL; COUMARIN DERIVATIVE; GEIPARVARIN; GEMFIBROZIL; HYDROXYL RADICAL; LIPID; MANNITOL; NOVOBIOCIN; PHOSPHOLIPID; PSORALEN; SUPEROXIDE; TRIACYLGLYCEROL; TYLOXAPOL; UNCLASSIFIED DRUG; UNINDEXED DRUG; WARFARIN;

EID: 77952290793     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.103     Document Type: Article
Times cited : (52)

References (26)
  • 12
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  • 18
    • 77952288375 scopus 로고    scopus 로고
    • note
    • 4. Column chromatography over silica gel (100-200 mesh) and elution with 50% chloroform in hexane furnished the final product 8.This was obtained in 75% yield as white solid.
  • 23
    • 77952287695 scopus 로고    scopus 로고
    • note
    • Lipid lowering activity: Adult male Charles Foster rats (200-225 g) bred in the animal house of the institute were used for the lipid lowering activity. Rats were divided in control, triton induced, triton plus compounds and Gemfibrozil (100 mg/kg) treated groups containing six rats in each. Hyperlipidemia was developed by administration of Triton WR-1339 (Sigma chemical Co., St. Louis, USA) at a dose of 400 mg/kg body wt. intraperitoneally to animals of all groups except the control. Compounds 3-13 were macerated with gum acacia (0.2% w/v), suspended in water and fed simultaneously with triton at a dose of 100 mg/kg po to the animals of treated groups. Animals of the control and triton group without treatment with test compounds were given same amount of gum acacia suspension (vehicle). After 18 h of treatment (50 mg/kg body wt.) 1.0 mL blood was withdrawn from retro-orbital sinus using glass capillary in EDTA coated eppendorf tube (3.0 mg/mL blood). The blood was centrifuged (at 2500g) at 4 °C for 10 min and the plasma was separated. Plasma was diluted with normal saline (ratio 1:3) and used for analysis of total cholesterol (TC), phospholipids (PL), triglycerides (Tg) and post heparin lipolytic activity (PHLA) using spectrophotometer, Beckmann auto-analyzer and standard kits purchased from Beckmann Coulter International, USA.
  • 24
    • 77952290740 scopus 로고    scopus 로고
    • note
    • 4 buffer (pH 7.4) to a final volume of 2.5 mL. The above reaction mixtures in the absence or presence of test compounds (100 μg/mL and 200 μg/mL) were incubated at 37 °C for 90 min. The test compounds were also studied for their inhibitory action against microsomal lipid peroxidation in vitro by non-enzymatic inducer. Reference tubes and reagents blanks were also run simultaneously. Malondialdehyde (MDA) contents in both experimental and reference tubes were estimated spectrophotometrically by thiobarbituric acid as mentioned above. Allopurinol, mannitol and α-tocopherol were used as standard drugs for superoxide, hydroxylations and microsomal lipid peroxidation. All experimental data were analyzed using Student's t-test. Oxidized LDL was compared with the test compounds treated oxidized LDL. The generation of oxygen free radicals was compared in the presence and absence of test compounds. The hyperlipidemic group was compared with control and hyperlipidemic plus drug treated groups P <0.05 was considered to be significant.


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