Výsledky vyhledávání - "Frank Taplin"

Oxazole phosphonic acids as fructose 1,6-bisphosphatase inhibitors with potent glucose-lowering activity

Autor: Scott C. Potter, Srinivas Rao Kasibthatla, Qun Dang, Frank Taplin, Paul D. van Poelje, Tony Gibson, Mark D. Erion, Tao Jiang

Publikováno v: MedChemComm. 2:287-290

To discover an alternative heterocyclic scaffold to the thiazole series of FBPase inhibitors such as thiazole 1, oxazoles were investigated to see if replacing the sulfur of the thiazole scaffold with an oxygen is tolerated. Numerous oxazoles with a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e742e99d9c44f6af40d2d3fe13f63937
https://doi.org/10.1039/c0md00269k

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Fructose-1,6-bisphosphatase Inhibitors. 2. Design, Synthesis, and Structure−Activity Relationship of a Series of Phosphonic Acid Containing Benzimidazoles that Function as 5′-Adenosinemonophosphate (AMP) Mimics

Autor: Jay DaRe, Qun Dang, Mark D. Erion, Tony Gibson, Frank Taplin, Paul D. van Poelje, Yan Liu, Scott C. Potter, Srinivras Rao Kasibhatla, K. Raja Reddy, Wei Xiao, Gerard R. Scarlato

Publikováno v: Journal of Medicinal Chemistry. 53:441-451

Efforts to enhance the inhibitory potency of the initial purine series of fructose-1,6-bisphosphatase (FBPase) inhibitors led to the discovery of a series of benzimidazole analogues with human FBPase IC(50)s < 100 nM. Inhibitor 4.4 emerged as a lead

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99b77507b9a9519ff4310d803b2ebc1e
https://doi.org/10.1021/jm901420x

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Discovery of Phosphonic Diamide Prodrugs and Their Use for the Oral Delivery of a Series of Fructose 1,6-Bisphosphatase Inhibitors

Autor: Tao Jiang, James M. Fujitaki, Daniel K. Cashion, Srinivas Rao Kasibhatla, Yan Liu, K. Raja Reddy, Paul D. van Poelje, Scott C. Potter, Frank Taplin, William G. Schulz, Kevin Fan, Mark D. Erion, Qun Dang

Publikováno v: Journal of Medicinal Chemistry. 51:4331-4339

Like most phosphonic acids, the recently discovered potent and selective thiazole phosphonic acid inhibitors of fructose 1,6-bisphosphatase (FBPase) exhibited low oral bioavailability (OBAV) and therefore required a prodrug to achieve oral efficacy.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65bfa7ac815f2145b3a778cc523215b4
https://doi.org/10.1021/jm8001235

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Discovery of a series of phosphonic acid-containing thiazoles and orally bioavailable diamide prodrugs that lower glucose in diabetic animals through inhibition of fructose-1,6-bisphosphatase

Autor: Jay DaRe, Tao Jiang, Scott C. Potter, Tony Gibson, Qun Dang, Frank Taplin, Yan Liu, Mark D. Erion, Daniel K. Cashion, Haiqing Li, Zhili Sun, Jason D. Jacintho, Paul D. van Poelje, Srinivas Rao Kasibhatla, Yi Fan, Lemus Robert Huerta, Feng Tian, Wenyu Li

Publikováno v: Journal of medicinal chemistry. 54(1)

Oral delivery of previously disclosed purine and benzimidazole fructose-1,6-bisphosphatase (FBPase) inhibitors via prodrugs failed, which was likely due to their high molecular weight (>600). Therefore, a smaller scaffold was desired, and a series of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7227453a1b09fd9029c96cde2a01f99
https://pubmed.ncbi.nlm.nih.gov/21126019

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Discovery of Phosphonic Acid-Containing Desaminobenzimidazoles as Fructose 1,6-Bisphosphatase Inhibitors that are Suitable for Oral Delivery via Prodrugs

Autor: M. Rami Reddy, Paul D. van Poelje, Srinivas Rao Kasibthatla, Tony Gibson, Qun Dang, Scott C. Potter, Frank Taplin, Mark D. Erion, Tao Jiang, K. Raja Reddy

Publikováno v: Journal of Diabetes & Metabolism.

To discover an alternative series of fructose 1,6-bisphosphatase (FBPase) inhibitors that is suitable for oral delivery via prodrugs, the 4-amino group was removed from the initial 4-aminobenzimidazole lead series, since the number of hydrogen bond d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fddc0fae1017c6af81721bcf2583d864
https://doi.org/10.4172/2155-6156.1000105

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Akademický článek

Discovery of a Series of Phosphonic Acid-Containing Thiazoles and Orally Bioavailable Diamide Prodrugs That Lower Glucose in Diabetic Animals Through Inhibition of Fructose-1,6-Bisphosphatase.

Autor: Qun Dang, Yan Liu, Daniel K. Cashion, Srinivas Rao Kasibhatla, Tao Jiang, Frank Taplin, Jason D. Jacintho, Haiqing Li, Zhili Sun, Yi Fan, Jay DaRe, Feng Tian, Wenyu Li, Tony Gibson, Robert Lemus, Paul D. van Poelje, Scott C. Potter, Mark D. Erion

Publikováno v: Journal of Medicinal Chemistry; Jan2011, Vol. 54 Issue 1, p153-165, 13p

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Akademický článek

Autor: Qun Dang, Srinivas Rao Kasibhatla, Wei Xiao, Yan Liu, Jay DaRe, Frank Taplin, K. Raja Reddy, Gerard R. Scarlato, Tony Gibson, Paul D. van Poelje, Scott C. Potter, Mark D. Erion

Publikováno v: Journal of Medicinal Chemistry; Jan2010, Vol. 53 Issue 1, p441-451, 11p

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Akademický článek

Discovery of Phosphonic Diamide Prodrugs and Their Use for the Oral Delivery of a Series of Fructose 1,6-Bisphosphatase Inhibitors.

Autor: Qun Dang, Srinivas Rao Kasibhatla, Tao Jiang, Kevin Fan, Yan Liu, Frank Taplin, William Schulz, Daniel K. Cashion, K. Raja Reddy, Paul D. van Poelje, James M. Fujitaki, Scott C. Potter, Mark D. Erion

Publikováno v: Journal of Medicinal Chemistry; Jun2008, Vol. 51 Issue 14, p4331-4339, 9p

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