Výsledky vyhledávání - "Jonathan A. Covel"

A calcineurin antifungal strategy with analogs of FK506

Autor: Mehdi Michel Djamel Numa, Molly K. Moloney, Nambu Mitchell David, Robert R. Webb, Michael Trzoss, Mili Kapoor, Jonathan A. Covel, Quinlyn A. Soltow, Mitchell Mutz, Xiaoming Li, Peter J. Webb

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 27:2465-2471

A novel antifungal strategy targeting the inhibition of calcineurin is described. To develop a calcineurin based inhibitor of pathogenic fungi, analogs of FK506 were synthesized that were able to permeate mammalian but not fungal cells. Antagonists i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e21264582bc6932ed420f6836aaa6ac4
https://doi.org/10.1016/j.bmcl.2017.04.004

Zobrazit plný text záznamu

Synthesis of analogs of the Gwt1 inhibitor manogepix (APX001A) and in vitro evaluation against Cryptococcus spp

Autor: Mili Kapoor, Quinlyn A. Soltow, Michael Trzoss, Molly K. Moloney, Jonathan A. Covel, Peter J. Webb, Karen Joy Shaw

Publikováno v: Bioorg Med Chem Lett

Fosmanogepix (APX001) is a first-in-class prodrug molecule that is currently in Phase 2 clinical trials for invasive fungal infections. The active moiety manogepix (APX001A) inhibits the novel fungal protein Gwt1. Gwt1 catalyzes an early step in the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b8755e5c3c69d6cf0c5a88586a4b7a1
https://doi.org/10.1016/j.bmcl.2019.126713

Zobrazit plný text záznamu

Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:71-75

The design of a new clinical candidate histamine-H(3) receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by replac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5d0d99a5060605090b0ee3524c5cbb2d
https://doi.org/10.1016/j.bmcl.2011.11.075

Zobrazit plný text záznamu

Total Synthesis of Bryostatin 1

Autor: Arnab Rudra, Yam B. Poudel, Thomas Cummins, Jonathan A. Covel, Gary E. Keck

Publikováno v: Journal of the American Chemical Society. 133:744-747

Bryostatin 1 is a marine natural product that is a very promising lead compound because of the potent biological activity it displays against a variety of human disease states. We describe herein the first total synthesis of this agent. The synthetic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d52d65f5db6b203bb73dede048ca9014
https://doi.org/10.1021/ja110198y

Zobrazit plný text záznamu

Design and Evaluation of Novel Biphenyl Sulfonamide Derivatives with Potent Histamine H3 Receptor Inverse Agonist Activity

Publikováno v: Journal of Medicinal Chemistry. 52:5603-5611

Antagonism of the histamine-H(3) receptor is one tactic being explored to increase wakefulness for the treatment of disorders such as excessive daytime sleepiness (EDS) as well as other sleep or cognitive disorders. Phenethyl-R-2-methylpyrrolidine co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91140b3031229283d3f2a52afb1585eb
https://doi.org/10.1021/jm900857n

Zobrazit plný text záznamu

Novel H3 receptor antagonists with improved pharmacokinetic profiles

Autor: Andrew J. Grottick, Michelle D. Pulley, Rena Hayashi, Jonathan A. Covel, Brian J. Hofilena, Guilherme Pereira, William Thomsen, Vincent J. Santora, Marissa Suarez, Jeff Edwards, Albert S. Ren, Jodie Lorea, Michael I. Weinhouse, Graeme Semple, Erin K. Hauser, John Frazer, Jason B. Ibarra

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:4133-4136

A new series of H 3 antagonists derived from the natural product Conessine are presented. Several compounds from these new series retain the potency and selectivity of earlier diamine based analogs while exhibiting improved PK characteristics. One co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a3e31fcd35211c56f91ff3a94e95619
https://doi.org/10.1016/j.bmcl.2008.05.086

Zobrazit plný text záznamu

Pyran Annulation: Asymmetric Synthesis of 2,6-Disubstituted-4-methylene Tetrahydropyrans

Autor: Gary E. Keck, Tobias Schiff, Tao Yu, Jonathan A. Covel

Publikováno v: Organic Letters. 4:1189-1192

[reaction: see text] A reaction process for the asymmetric construction of a variety of cis or trans disubstituted pyrans is described. This sequences allows for the asymmetric convergent union of two aldehydes with silyl-stannane reagent 1 in a two-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78ceb6a40f27910446ff257edd7285ff
https://doi.org/10.1021/ol025645d

Zobrazit plný text záznamu

Asymmetric Total Synthesis of Rhizoxin D

Autor: Jonathan A. Covel, Travis T. Wager, Dhileepkumar Krishnamurthy, Mark D. McLaws, Gary E. Keck, Victor J. Cee, Kenneth A. Savin, Carrie A. Wager

Publikováno v: Angewandte Chemie. 113:237-240

We describe herein the synthesisof rhizoxin D by an approach utilizing catalytic asymmetricallylation as a key strategic element.The overall approach to this synthesis is illustrated inScheme 1 and relied upon disconnections at the C9yC10 andC20yC21

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c13749c7fb380e63974263f8a60c5679
https://doi.org/10.1002/1521-3757(20010105)113:1<237::aid-ange237>3.0.co

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání