David G Washburn
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Explore the profile of David G Washburn including associated specialties, affiliations and a list of published articles.
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101
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Recent Articles
1.
Vantourout J, Mason A, Yuen J, Simpson G, Evindar G, Kuai L, et al.
Bioconjug Chem
. 2021 Feb;
32(2):279-289.
PMID: 33523652
Reducing the required frequence of drug dosing can improve the adherence of patients to chronic treatments. Hence, drugs with longer half-lives are highly desirable. One of the most promising approaches...
2.
Washburn D, Holt D, Dodson J, McAtee J, Terrell L, Barton L, et al.
Bioorg Med Chem Lett
. 2013 Jul;
23(17):4979-84.
PMID: 23886683
Lead optimization of piperidine amide HTS hits, based on an anilino-thiazole core, led to the identification of analogs which displayed low nanomolar blocking activity at the canonical transient receptor channels...
3.
Kallander L, Washburn D, Hoang T, Frazee J, Stoy P, Johnson L, et al.
Bioorg Med Chem Lett
. 2009 Nov;
20(1):371-4.
PMID: 19926282
The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The...
4.
Washburn D, Hoang T, Frazee J, Johnson L, Hammond M, Manns S, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4664-8.
PMID: 19616429
We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency...
5.
Thompson S, Washburn D, Frazee J, Madauss K, Hoang T, Lapinski L, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4777-80.
PMID: 19595590
Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring...
6.
Hammond M, Washburn D, Hoang H, Manns S, Frazee J, Nakamura H, et al.
Bioorg Med Chem Lett
. 2009 Jun;
19(15):4441-5.
PMID: 19497745
The lead serum and glucocorticoid-related kinase 1 (SGK1) inhibitors 4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid (1) and {4-[5-(2-naphthalenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]phenyl}acetic acid (2) suffer from low DNAUC values in rat, due in part to formation and excretion...
7.
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists
Hammond M, Patterson J, Manns S, Hoang T, Washburn D, Trizna W, et al.
Bioorg Med Chem Lett
. 2009 Apr;
19(10):2637-41.
PMID: 19376703
Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands...
8.
Washburn D, Hoang T, Campobasso N, Smallwood A, Parks D, Webb C, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(4):1097-100.
PMID: 19167885
A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of...
9.
Washburn D, Heidebrecht Jr R, Martin S
Org Lett
. 2003 Sep;
5(19):3523-5.
PMID: 12967315
[reaction: see text] A synthesis of the 6-aza[3.2.1]bicyclooctene (-)-2 has been completed by a short sequence of reactions that required only six operations from (S)-malic acid and featured a novel...
10.
Crimmins M, Katz J, Washburn D, Allwein S, McAtee L
J Am Chem Soc
. 2002 May;
124(20):5661-3.
PMID: 12010038
The total synthesis of spongistatin 1 (1) and spongistatin 2 (2) has been achieved through an advanced-stage intermediate. The synthesis is highlighted by a highly convergent assembly of the four...