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Dive into the research topics where Jeffrey J. Letourneau is active.

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Featured researches published by Jeffrey J. Letourneau.


Bioorganic & Medicinal Chemistry Letters | 2009

2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.

Andrew G. Cole; Adolph C. Bohnstedt; Vidyadhar M. Paradkar; Celia Kingsbury; Jorge Quintero; Haengsoon Park; Yingchun Lu; Ming You; Irina Neagu; David J. Diller; Jeffrey J. Letourneau; Yuefei Shao; Ray Anthony James; Christopher Mark Riviello; Koc-Kan Ho; Tsung H. Lin; Bojing Wang; Kenneth C. Appell; Matthew A. Sills; Elizabeth Quadros; Earl F. Kimble; Michael Ohlmeyer; Maria L. Webb

A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was identified incorporating a chroman-based functional group. Compound 24 shows excellent kinase activity, good oral bioavailability and demonstrates efficacy in an acute mechanistic mouse model through inhibition of interleukin-2 (IL-2) induced interferon-gamma (INF-gamma) production.


Bioorganic & Medicinal Chemistry Letters | 2009

Synthesis and initial evaluation of novel, non-peptidic antagonists of the αv-integrins αvβ3 and αvβ5

Jeffrey J. Letourneau; Jinqi Liu; Michael Ohlmeyer; Chris Riviello; Yajing Rong; Hong Li; Kenneth C. Appell; Shalini Bansal; Biji Jacob; Angela Wong; Maria L. Webb

The discovery, synthesis and preliminary SAR of a novel class of non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5) is described. High-throughput screening of an extensive series of ECLiPStrade mark compound libraries led to the identification of compound 1 as a dual inhibitor of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5). Optimization of compound 1 involving, in part, introduction of two novel constraints led to the discovery of compounds 15a and 15b with reduced PSA and much improved potency for both the alpha(v)beta(3) and alpha(v)beta(5) integrins. Compounds 15a and 15b were shown to have promising activity in functional cellular assays and compound 15a also exhibited a promising Caco-2 permeability profile.


Bioorganic & Medicinal Chemistry Letters | 2011

Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.

Susan Elizabeth Napier; Jeffrey J. Letourneau; Nasrin Ansari; Douglas S. Auld; James R. Baker; Stuart Best; Leigh Campbell-Wan; Ray Jui-Hsiang Chan; Mark Craighead; Hema Desai; Koc-Kan Ho; Cliona P. MacSweeney; Rachel Milne; J. Richard Morphy; Irina Neagu; Michael Ohlmeyer; Jack Pick; Jeremy Presland; Chris Riviello; Heather A. Zanetakos; Jiuqiao Zhao; Maria L. Webb

Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and OT. Optimised compound 16 shows a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.


Bioorganic & Medicinal Chemistry Letters | 2011

Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists

Susan Elizabeth Napier; Jeffrey J. Letourneau; Nasrin Ansari; Douglas S. Auld; James R. Baker; Stuart Best; Leigh Campbell-Wan; Jui-Hsiang Chan; Mark Craighead; Hema Desai; Katharine A. Goan; Koc-Kan Ho; Ellen G.J. Hulskotte; Cliona P. MacSweeney; Rachel Milne; J. Richard Morphy; Irina Neagu; Michael Ohlmeyer; Ard W.M.M. Peeters; Jeremy Presland; Chris Riviello; Ge S.F. Ruigt; Fiona J. Thomson; Heather A. Zanetakos; Jiuqiao Zhao; Maria L. Webb

Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) (V(3)) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and oxytocin (OT). Optimised compound 12j demonstrates a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.


Bioorganic & Medicinal Chemistry Letters | 2010

Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists

Jeffrey J. Letourneau; Christopher Mark Riviello; Hong Li; Andrew G. Cole; Koc-Kan Ho; Heather A. Zanetakos; Hema Desai; Jiuqiao Zhao; Douglas S. Auld; Susan Elizabeth Napier; Fiona J. Thomson; Katharine A. Goan; J. Richard Morphy; Michael Ohlmeyer; Maria L. Webb

The discovery, synthesis, and preliminary structure-activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse, three million-member compound collection, prepared using ECLiPS technology, had good activity in a V3 binding assay (IC50=0.20 microM), but less than desirable physicochemical properties. Optimization of compound 1 yielded potent analogs 19 (IC50=0.31 microM) and 24 (IC50=0.12 microM) with improved drug-like characteristics.


Bioorganic & Medicinal Chemistry Letters | 2018

Identification and initial optimization of inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB)

Jeffrey J. Letourneau; Ilana L. Stroke; David W. Hilbert; Laurie J. Sturzenbecker; Brett A. Marinelli; Jorge Quintero; Joan Eileen Sabalski; Linh Ma; David J. Diller; Philip D. Stein; Maria L. Webb

The discovery, synthesis and preliminary structure-activity relationship (SAR) of a novel class of inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB) is described. A high throughput screening (HTS) campaign resulted in the identification of moderately active screening hits 1-5 the most potent of which was compound 1 (IC50 = 0.77 µM). In silico docking of an early analog offered suggestions for structural modification which resulted in the design and synthesis of highly potent analogs 13j(IC50 = 1 nM) and 13 l(IC50 = 7 nM) which were chosen as leads for further optimization.


Archive | 2002

N-heterocyclic inhibitors of tnf-alpha expression

Kevin Joseph Moriarty; Yvonne Shimshock; Gulzar Ahmed; Junjun Wu; James Wen; Wei Li; Shawn D. Erickson; Jeffrey J. Letourneau; Edward Mcdonald; Katerina Leftheris; Stephen T. Wrobleski


Archive | 2002

Pyrimidine and triazine kinase inhibitors

Shawn David Erickson; James Inglese; Jeffrey J. Letourneau; Christopher Mark Riviello


Journal of Medicinal Chemistry | 2004

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Katerina Leftheris; Gulzar Ahmed; Ran Chan; Alaric J. Dyckman; Zahid Hussain; Kan Ho; John Hynes; Jeffrey J. Letourneau; Wei Li; Shuqun Lin; Axel Metzger; Kevin Joseph Moriarty; Chris Riviello; Yvonne Shimshock; James Wen; John Wityak; Stephen T. Wrobleski; Hong Wu; Junjun Wu; Madhuri Desai; Kathleen M. Gillooly; Tsung H. Lin; Derek Loo; Kim W. McIntyre; Sidney Pitt; Ding Ren Shen; David J. Shuster; Rosemary Zhang; David J. Diller; Arthur M. Doweyko


Archive | 2006

Azinone and diazinone V3 inhibitors for depression and stress disorders

Jeffrey J. Letourneau; Koc-Kan Ho; Michael J. Ohlmeyer; Patrick Jokiel; Christopher Mark Riviello

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