Synthesis of some novel substituted phenylisoxazol phenoxy 2-methylpropanoic acids and there in vivo hypolipidemic activity

Mokale, Santosh N.; Dube, Pritam N.; Nevase, Manjusha C.; Sakle, Nikhil S.; Shelke, Vishakha R.; Bhavale, Swati A.; Begum, Afreen

doi:10.1007/s00044-015-1498-2

Cited by 2 publications

(2 citation statements)

References 11 publications

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“…These new compounds have the potential to complex the zinc atom of FTase, but presented only a modest activity as FTase inhibitors and as anticancer agents . It is known that 3,5‐diarylisoxazoles display pharmaceutical properties as interleukin‐8 receptor antagonists or hypolipidemic agents, and weak anticancer activity . We are now interested in the synthesis of arylisoxazoles substituted by a dimethoxytriazine group, with the general structure 3 .…”

Section: Introductionmentioning

confidence: 99%

Exploring isoxazoles and pyrrolidinones decorated with the 4,6‐dimethoxy‐1,3,5‐triazine unit as human farnesyltransferase inhibitors

Lucescu

Ghinet

Shova³

et al. 2019

Archiv der Pharmazie

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Unprecedented triazinyl‐isoxazoles were afforded via an effective cycloaddition reaction between nitrile oxides and the scarcely described 2‐ethynyl‐4,6‐dimethoxy‐1,3,5‐triazine as dipolarophile. The biological evaluation of the newly synthesized compounds showed that the inhibition of human farnesyltransferase by zinc complexation could be improved with triazine‐isoxazole moieties. The replacement of the isoxazole unit by a pyrrolidin‐2‐one was detrimental to the inhibitory activity while the pyrrolidin‐2‐thione derivatives conserved the biological potential. The potential of selected compounds to disrupt protein farnesylation in Chinese hamster ovary (CHO) cells transfected with pEGFP‐CAAX was also evaluated.

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Section: Introductionmentioning

confidence: 99%

Exploring isoxazoles and pyrrolidinones decorated with the 4,6‐dimethoxy‐1,3,5‐triazine unit as human farnesyltransferase inhibitors

Lucescu

Ghinet

Shova³

et al. 2019

Archiv der Pharmazie

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“…The synthesis of polycyclic isoxazole analogues 17a and 17b was depicted in Scheme . SeO 2 -mediated oxidation transformed 4-hydroxyphenylethanone 12 to 2-oxo-2-phenylacetic acid 13 . , After the chlorination, the α-alkylation of benzoxepin-5-one proceeded, followed by hydroxylamine participated annulations. Deoxydation and subsequent hydrolysis reactions provided compounds 17a and 17b , ultimately.…”

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confidence: 99%

Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis

Jiang

Liu

Yuan

et al. 2019

ACS Med. Chem. Lett.

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A novel peroxisome proliferator-activated receptor (PPAR) α/δ dual agonist 5c was developed with an EC 50 of 8 nM for PPARα, 5 nM for PPARδ, and >300-fold selectivity against PPARγ (EC 50 = 2939 nM), respectively. Further ADME and pharmacokinetic studies indicated 5c possessed distinguished in vitro and in vivo profiles. The excellent in vivo efficacy of compound 5c was demonstrated by the rat primary biliary cirrhosis (PBC) model.

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Synthesis of some novel substituted phenylisoxazol phenoxy 2-methylpropanoic acids and there in vivo hypolipidemic activity

Cited by 2 publications

References 11 publications

Exploring isoxazoles and pyrrolidinones decorated with the 4,6‐dimethoxy‐1,3,5‐triazine unit as human farnesyltransferase inhibitors

Exploring isoxazoles and pyrrolidinones decorated with the 4,6‐dimethoxy‐1,3,5‐triazine unit as human farnesyltransferase inhibitors

Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis

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