John V. Duncia
Wilmington University
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Featured researches published by John V. Duncia.
Bioorganic & Medicinal Chemistry Letters | 1998
John V. Duncia; Joseph B. Santella; C. Anne Higley; William John Pitts; John Wityak; William E. Frietze; F.Wayne Rankin; Jung-Hui Sun; Richard A. Earl; A.Christine Tabaka; Christopher A. Teleha; Karl F. Blom; Margaret F. Favata; Elizabeth J. Manos; Andrea J. Daulerio; Deborah A. Stradley; Kurumi Y. Horiuchi; Robert A. Copeland; Peggy Scherle; James M. Trzaskos; Ronald L. Magolda; George L. Trainor; Ruth R. Wexler; Frank W. Hobbs; Richard E. Olson
In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with an IC50 of 0.07 microM for MEK 1 and 0.06 microM for MEK 2. U0126 can undergo isomerization and cyclization reactions to form a variety of products, both chemically and in vivo, all of which exhibit less affinity for MEK and lower inhibition of AP-1 activity than parent, U0126.
Bioorganic & Medicinal Chemistry Letters | 1998
John V. Duncia; Joseph B. Santella; C. Anne Higley; Mary K. VanAtten; Patricia C. Weber; Richard S. Alexander; Charles A. Kettner; James Russell Pruitt; Anne Y. Liauw; Mimi L. Quan; Robert M. Knabb; Ruth R. Wexler
Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors.
Bioorganic & Medicinal Chemistry Letters | 1997
Mimi L. Quan; John Wityak; Celia Dominguez; John V. Duncia; Charles A. Kettner; Christopher D. Ellis; A.Y. Liauw; Jeongsook M. Park; Joseph B. Santella; Robert M. Knabb; Martin Thoolen; Patricia C. Weber; Ruth R. Wexler
Abstract Thrombin is a serine protease that plays an important role in the blood coagulation cascade, and is a target enzyme for new therapeutic agents. Ac-(D)-Phe-Pro-boroArg-OH (DuP 714) was found to be a highly effective thrombin inhibitor. In order to reduce the peptidic nature of DuP 714, we have designed a series of novel biaryl substituted alkylboronate esters as potent thrombin inhibitors. The most potent compounds have subnanomolar affinity for thrombin.
Bioorganic & Medicinal Chemistry Letters | 1994
Joseph B. Santella; John V. Duncia; Carol L. Ensinger; Mary K. VanAtten; David J. Carini; Ruth R. Wexler; Andrew T. Chiu; Pancras C. Wong; Pieter B.M.W.M. Timmermans
Abstract We wish to report on a series of substituted methyl esters and amides of DMP 811, which bind to both the AT 1 and AT 2 receptor subtypes. Some of the esters bind well to both receptor subtypes in the subnanomolar range when the optimal acid isostere is present together with an ortho-fluorine substituent on the biphenylmethyl group.
European Journal of Pharmacology | 1994
Pancras C. Wong; John V. Duncia; Joseph B. Santella; Ronald D. Smith; Ruth R. Wexler; Pieter B.M.W.M. Timmermans; Andrew T. Chiu
AT1 and AT2 are the two major receptor subtypes for angiotensin II that have been pharmacologically defined by using the selective ligands losartan and PD123177, respectively. EXP597 (4-[(5-(2-benzoyl)benzyloxycarbonyl-4-ethyl-2-n-propylimidazole-1- yl)methyl]-3-fluoro-2-isoamyloxycarbonylaminosulfonyl-[1,1]-biph enyl, potassium salt) is a nonpeptide angiotensin II receptor ligand which in the rat adrenal exhibits binding affinities (IC50) of 0.5 and 0.7 nM for angiotensin AT1 and AT2 receptor subtypes, respectively. Further, EXP597 is an insurmountable angiotensin II receptor antagonist in the isolated rabbit aorta and lowers blood pressure in renal hypertensive rats with i.v. and p.o. ED30 values of 0.05 and 0.9 mg/kg, respectively.
Bioorganic & Medicinal Chemistry Letters | 1995
John V. Duncia; Joseph B. Santella; Andrew T. Chiu; Pancras C. Wong; Ruth R. Wexler
Abstract Most angiotensin II antagonists in the literature contain the biphenyltetrazole moiety. We now wish to report a new, more rigidized biphenyl replacement, namely the dibenzobicyclo[2.2.2.]octane scaffold. It was designed on the basis of the three-dimensional conformation of the biphenyltetrazole moiety of losartan, the prototypic angiotensin II antagonist. This biphenyltetrazole replacement fixes both the imidazole and the negatively charged (at physiological pH) tetrazole in the same areas of space where they are located in losartan. Other scaffolds such as a fluorene and Rebeks Cleft are also discussed.
Medicinal Research Reviews | 1992
John V. Duncia; David J. Carini; Andrew T. Chiu; Alexander L. Johnson; William A. Price; Pancras C. Wong; Ruth R. Wexler; Pieter B.M.W.M. Timmermans
Archive | 2000
John V. Duncia; Daniel S. Gardner; Joseph B. Santella
Archive | 1990
David John Carini; John V. Duncia
Archive | 1990
David John Carini; John V. Duncia