Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase

Thalji, Reema K.; McAtee, J. Jeffrey; Belyanskaya, Svetlana; Brandt, Martín; Brown, G. K.; Costell, Melissa H.; Ding, Yun; Dodson, Jason W.; Eisennagel, Steve H.; Fries, Rusty E.; Gross, Janet L.; Harpel, Mark R.; Holt, Dennis A.; Israel, David I.; Jolivette, Larry J.; Krosky, Daniel J.; Li, Hu; Lu, Quinn; Mandichak, Tracy; Roethke, Theresa J.; Schnackenberg, Christine G.; Schwartz, Benjamin; Shewchuk, Lisa M.; Xie, Wensheng; Behm, David J.; Douglas, Stephen A.; Shaw, Ami L.; Marino, Joseph P.

doi:10.1016/j.bmcl.2013.04.019

Cited by 57 publications

(44 citation statements)

References 25 publications

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“…The platform features two major benefits, access to a broad set of chemotypes with vast structural diversity and use of negligible amounts of target protein. Since its inception, ELT has successfully identified tractable hit series for diverse targets (33,34,40). Purified PDE12 was immobilized, and selections were performed to screen a three-cycle library.…”

Section: Effects Of Pde12 Gene Inactivation On Viral Infection-thementioning

confidence: 99%

The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors

Wood

Bledsoe

Chai

et al. 2015

Journal of Biological Chemistry

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Background: PDE12 degrades 2Ј,5Ј-oligoadenylate, a second messenger involved in the antiviral action of interferon. Results: Inactivation of the PDE12 gene and novel inhibitors of the enzyme render cells resistant to more than one virus. Conclusion: PDE12 negatively regulates the innate immune response, and inhibitors of PDE12 have antiviral activity. Significance: PDE12 inhibitors have the potential to be broadly acting antiviral medicines.

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Section: Effects Of Pde12 Gene Inactivation On Viral Infection-thementioning

confidence: 99%

The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors

Wood

Bledsoe

Chai

et al. 2015

Journal of Biological Chemistry

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“…Compared to its urea analog 32 , 2a is 13-fold less potent. The molecular docking of 2a (Fig 3) suggests that it is twisted upside down, unlike 2b and 2c (fig.…”

mentioning

confidence: 94%

Adamantyl thioureas as soluble epoxide hydrolase inhibitors

Burmistrov

Morisseau

Pitushkin

et al. 2018

Bioorganic & Medicinal Chemistry Letters

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A series of inhibitors of the soluble epoxide hydrolase (sEH) containing one or two thiourea groups has been developed. Inhibition potency of the described compounds ranges from 50 μM to 7.2 nM. 1,7-(Heptamethylene)bis[(adamant-1-yl)thiourea] (6f) was found to be the most potent sEH inhibitor, among the thioureas tested. The inhibitory activity of the thioureas against the human sEH is closer to the value of activity against rat sEH rather than murine sEH. While being less active, thioureas are up to 7-fold more soluble than ureas, which makes them more bioavailable and thus promising as sEH inhibitors.

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“…al [142]. has identified 1-(1,3,5-triazin-yl)piperidine-4-carboxamide as inhibitor of soluble epoxide hydrolase.…”

mentioning

confidence: 98%

Triazine as a promising scaffold for its versatile biological behavior

Singla

Luxami

Paul

2015

European Journal of Medicinal Chemistry

114

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Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase

Cited by 57 publications

References 25 publications

The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors

The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors

Adamantyl thioureas as soluble epoxide hydrolase inhibitors

Triazine as a promising scaffold for its versatile biological behavior

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