D-(R)- and L-(S)-3-Alkylaminopyrrolidino-substituted dihydrodibenzo[b,f]- and -[b,e]thiepins, xanthenes, and diphenylmethanes

Witiak, Donald T.; Hsu, Song Y.; Ollmann, James E.; Griffith, Robert K.; Seth, Shiv K.; Gerald, Michael C.

doi:10.1021/jm00253a007

Cited by 8 publications

(5 citation statements)

References 10 publications

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“…Triton WR-1339-induced hyperlipidemic rat model (7). Methods were identical to those previously reported (4). Hyperlipidemia was induced by IP injection of Triton WR-1339 (oxyethylated tert-octylphenolformaldehyde polymer, Ruger Chemical Co., Philadelphia, PA).…”

Section: Biological Methodsmentioning

confidence: 99%

“…Preparation of microsomes. The homogenization of livers and preparation of microsomes were done as described previously (4,11).…”

Section: Biological Methodsmentioning

confidence: 99%

“…The assay from mevalonic acid formation from D,L-3-hydroxy-3-methylglutaryl-3-[14C]-CoA was carried out by procedures identical to those described previously (4). Ethylmorphine N-demethylase assay.…”

Section: Biological Methodsmentioning

confidence: 99%

“…To further explore the effect of structural modification at the 4-position on antilipidemic properties, ethyl-cis-6-chloro-4-hydroxy-chroman-2-carboxylate (IV) and its tricyclic lactone, 6-chloro-4-hydroxychroman-2-carboxylic acid lactone (V), were synthesized and their pharmacological profiles examined in 2 hyperlipidemic rat models and in normal animals. Lactone V was of interest since other clofibrate-related lactones (1,4,5) have been found to possess some of the antilipidemic and metabolic properties associated with the parent compound, clofibrate. In this paper, the comparative biolog- ical profiles of I-V ( Fig.…”

Section: Introductionmentioning

confidence: 99%

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Antilipidemic activity of 4‐oxo‐functionalized ethyl 6‐chlorochroman‐2‐carboxylate analogs and a related tricyclic lactone in three rat models

Cavestri

Minatelli

Baldwin

et al. 1981

Lipids

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The synthesis of ethyl cis-6-chloro-4-hydroxychroman-2-carboxylate (IV) and 6-chloro-4-hydroxy-chroman-2-carboxylic acid lactone (V) are reported. The antilipidemic properties of these compounds in 3 rat models were compared to the activity obtained for the previously synthesized related analogs ethyl 6-chlorochroman-2-carboxylate (II), ethyl 6-chlorochromanone-2-carboxylate (III) and clofibrate (I). The biologically most interesting analog, ethyl 6-chlorochroman-2-carboyxlate (II) like clofibrate (I), was an effective antitriglyceridemic and anticholesterolemic agent in Triton WR-1339 hyperlipidemic rats, sucrose-fed hyperlipidemic rats and chow-fed normolipemic rats. Ethyl 6-chlorochromanone-2-carboxylate (III) was found to be active after 7 days of administration to sucrose-fed rats. In sucrose-fed, male Sprague-Dawley rats, the comparative effects of these analogs on various hepatic drug parameters also were carried out. Consistent with previous findings, results obtained with these compounds provide evidence showing that changes in hepatic HMG-CoA reductase activity bear no relationship to serum cholesterol lowering in the sucrose-fed model.

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Section: Biological Methodsmentioning

confidence: 99%

“…Preparation of microsomes. The homogenization of livers and preparation of microsomes were done as described previously (4,11).…”

Section: Biological Methodsmentioning

confidence: 99%

Section: Biological Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Antilipidemic activity of 4‐oxo‐functionalized ethyl 6‐chlorochroman‐2‐carboxylate analogs and a related tricyclic lactone in three rat models

Cavestri

Minatelli

Baldwin

et al. 1981

Lipids

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“…Coverslips were mounted, dried, dipped in a 1 :2 dilution of liquid emulsion (Kodak NTB-2) and left in the dark at 4°C for 3 days. Slides were developed in Kodak D19 developer and fixed in Kodak fixer, Nuclei were stained with hematoxin-eosin and at least 50 nuclei selected at random were counted using an Artex counter connected to a Zeiss AUS JENA research microscope (400 x magnification) as described previously (Witiak et al, 1977).…”

Section: Unscheduled D N a Synthesismentioning

confidence: 99%

Differing Levels of Excision Repair in Human Fetal Dermis and Brain Cells

Gibson

D’Ambrosio

1982

Photochem & Photobiology

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Abstract— The levels of DNA excision repair, as measured by unscheduled DNA synthesis (UDS) and the UV‐endonuclease sensitive site assay, were compared in cells derived from human fetal brain and dermal tissues. The level of UDS induced following ultraviolet (UV) irradiation was found to be lower (approx. 60%) in the fetal brain cells than in fetal dermal cells. It was determined, using the UV‐endonuclease sensitive site assay to confirm the UDS observation, that 50% of the dimers induced by UV in fetal dermal cells were repaired in 8h, while only 15% were removed in the fetal brain cells during the same period of time. Even after 24 h, only 44% of the dimers induced by UV in the fetal brain cells were repaired, while 65% were removed in the dermal cells. These data suggest that cultured human fetal brain cells exhibit lower levels of excision repair compared to cultured human fetal dermal cells.

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ChemInform Abstract: D‐(R)‐ AND L‐(S)‐3‐ALKYLAMINOPYRROLIDINO‐SUBSTITUTED DIHYDRODIBENZO(B,F)‐ AND ‐(B,E)THIEPINS, XANTHENES, AND DIPHENYLMETHANES

Witiak¹,

Hsu²,

Ollmann³

et al. 1974

Chemischer Informationsdienst

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D-(R)- and L-(S)-3-Alkylaminopyrrolidino-substituted dihydrodibenzo[b,f]- and -[b,e]thiepins, xanthenes, and diphenylmethanes

Cited by 8 publications

References 10 publications

Antilipidemic activity of 4‐oxo‐functionalized ethyl 6‐chlorochroman‐2‐carboxylate analogs and a related tricyclic lactone in three rat models

Antilipidemic activity of 4‐oxo‐functionalized ethyl 6‐chlorochroman‐2‐carboxylate analogs and a related tricyclic lactone in three rat models

Differing Levels of Excision Repair in Human Fetal Dermis and Brain Cells

ChemInform Abstract: D‐(R)‐ AND L‐(S)‐3‐ALKYLAMINOPYRROLIDINO‐SUBSTITUTED DIHYDRODIBENZO(B,F)‐ AND ‐(B,E)THIEPINS, XANTHENES, AND DIPHENYLMETHANES

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