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David D Christ

Explore the profile of David D Christ including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 18
Citations 138
Followers 0
Related Specialties
Biochemistry
Pharmacology
Chemistry
Top 10 Co-Authors
Mingxin Qian
Robert C Newton
Rui-Qin Liu
Maryanne B Covington
Carl P Decicco
James J-W Duan
James M Trzaskos
Krishna Vaddi
Zhonghui Lu
Zelda R Wasserman
Published In
Bioorg Med Chem Lett
J Med Chem
Drug Metab Dispos
Pharm Res
J Pharm Sci
Affiliations
Soon will be listed here.
Recent Articles
1.
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859)
Le Bourdonnec B, Windh R, Ajello C, Leister L, Gu M, Chu G, et al.
J Med Chem . 2008 Sep; 51(19):5893-6. PMID: 18788723
Selective delta opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening....
2.
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents
Lu Z, Ott G, Anand R, Liu R, Covington M, Vaddi K, et al.
Bioorg Med Chem Lett . 2008 Feb; 18(6):1958-62. PMID: 18282708
Potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered with several new heterocyclic P1' groups in conjunction with cyclic beta-amino hydroxamic acid scaffolds. Among them, the...
3.
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents
Ott G, Asakawa N, Lu Z, Anand R, Liu R, Covington M, et al.
Bioorg Med Chem Lett . 2008 Feb; 18(5):1577-82. PMID: 18242982
Novel ((2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamides were found to be excellent P1' substituents in conjunction with unique constrained beta-amino hydroxamic acid scaffolds for the discovery of potent selective inhibitors of TNF-alpha Converting Enzyme (TACE)....
4.
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE)
Ott G, Asakawa N, Liu R, Covington M, Qian M, Vaddi K, et al.
Bioorg Med Chem Lett . 2008 Feb; 18(4):1288-92. PMID: 18234496
Two novel oxaspiro[4.4]nonane beta-benzamido hydroxamic scaffolds have been synthesized in enantio- and diasteriomerically pure form. These templates proved to be exceptional platforms that have led to the discovery of potent...
5.
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE)
Ott G, Asakawa N, Lu Z, Liu R, Covington M, Vaddi K, et al.
Bioorg Med Chem Lett . 2007 Dec; 18(2):694-9. PMID: 18061445
Selective inhibitors of TNF-alpha Converting Enzyme (TACE) based on (1R,2S)-cyclopentyl, (3S,4S)-pyrrolidinyl, and (3R,4S)-tetrahydrofuranyl beta-benzamido hydroxamic acids have been synthesized and evaluated. This study has led to the discovery of novel...
6.
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors
Duan J, Chen L, Lu Z, Xue C, Liu R, Covington M, et al.
Bioorg Med Chem Lett . 2007 Nov; 18(1):241-6. PMID: 18032037
Beta-benzamido hydroxamic acids were discovered as potent TACE inhibitors. A computer model was constructed to help understanding the binding activities and guiding SAR study. SAR optimization led to the discovery...
7.
N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations
He K, Qian M, Wong H, Bai S, He B, Brogdon B, et al.
J Pharm Sci . 2007 Oct; 97(7):2568-80. PMID: 17914718
N-in-1 (or cassette) dosing pharmacokinetics (PK) has been used in drug discovery for rapid assessment of PK properties of new chemical entities. However, because of potential for drug-drug interactions this...
8.
Pharmacokinetics and pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a potent and selective inhibitor of tumor necrosis factor alpha-converting enzyme...
Qian M, Bai S, Brogdon B, Wu J, Liu R, Covington M, et al.
Drug Metab Dispos . 2007 Jul; 35(10):1916-25. PMID: 17656469
DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)) is a potent and selective inhibitor of tumor necrosis factor (TNF)-alpha-converting enzyme (TACE). It significantly inhibits lipopolysaccharide-induced soluble TNF-alpha production in blood from rodents, chimpanzee,...
9.
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity
Pruitt J, Batt D, Wacker D, Bostrom L, Booker S, Mclaughlin E, et al.
Bioorg Med Chem Lett . 2007 Apr; 17(11):2992-7. PMID: 17418570
DPC168, a benzylpiperidine-substituted aryl urea CCR3 antagonist evaluated in clinical trials, was a relatively potent inhibitor of the 2D6 isoform of cytochrome P-450 (CYP2D6). Replacement of the cyclohexyl central ring...
10.
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors
Chen X, Ghavimi B, Corbett R, Xue C, Liu R, Covington M, et al.
Bioorg Med Chem Lett . 2007 Feb; 17(7):1865-70. PMID: 17276676
A new P1' group for TACE inhibitors was identified by eliminating the oxygen atom in the linker of the original 4-(2-methylquinolin-4-ylmethoxy)phenyl P1' group. Incorporation of this 4-(2-methylquinolin-4-ylmethyl)phenyl group onto different...