Dariusz Wodka
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Explore the profile of Dariusz Wodka including associated specialties, affiliations and a list of published articles.
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14
Citations
39
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Recent Articles
1.
Lan P, Romero F, Wodka D, Kassick A, Dang Q, Gibson T, et al.
J Med Chem
. 2017 Oct;
60(21):9040-9052.
PMID: 29035567
AMP-activated protein kinase (AMPK) plays an essential role as a cellular energy sensor and master regulator of metabolism in eukaryotes. Dysregulated lipid and carbohydrate metabolism resulting from insulin resistance leads...
2.
Judd A, Souers A, Wodka D, Zhao G, Mulhern M, Iyengar R, et al.
Bioorg Med Chem Lett
. 2007 Mar;
17(8):2365-71.
PMID: 17350253
A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated analogs were...
3.
Iyengar R, Lynch J, Mulhern M, Judd A, Freeman J, Gao J, et al.
Bioorg Med Chem Lett
. 2007 Jan;
17(4):874-8.
PMID: 17234405
The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety led to the discovery of 19, a...
4.
Rohde J, Pliushchev M, Sorensen B, Wodka D, Shuai Q, Wang J, et al.
J Med Chem
. 2007 Jan;
50(1):149-64.
PMID: 17201418
Starting from a rapidly metabolized adamantane 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor 22a, a series of E-5-hydroxy-2-adamantamine inhibitors, exemplified by 22d and (+/-)-22f, was discovered. Many of these compounds are...
5.
Souers A, Iyengar R, Judd A, Beno D, Gao J, Zhao G, et al.
Bioorg Med Chem Lett
. 2006 Dec;
17(4):884-9.
PMID: 17188866
The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the identification of a series of chiral racemic compounds that displayed good to...
6.
Lynch J, Freeman J, Judd A, Iyengar R, Mulhern M, Zhao G, et al.
J Med Chem
. 2006 Oct;
49(22):6569-84.
PMID: 17064075
Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to the identification of a chromone-2-carboxamide series as having excellent...
7.
Kym P, Souers A, Campbell T, Lynch J, Judd A, Iyengar R, et al.
J Med Chem
. 2006 Mar;
49(7):2339-52.
PMID: 16570930
An inactin-anesthetized rat cardiovascular (CV) assay was employed in a screening mode to triage multiple classes of melanin-concentrating hormone receptor 1 (MCHr1) antagonists. Lead identification was based on a compound...
8.
Kym P, Iyengar R, Souers A, Lynch J, Judd A, Gao J, et al.
J Med Chem
. 2005 Sep;
48(19):5888-91.
PMID: 16161992
4-(1-Benzo[1,3]dioxol-5-ylmethylpiperidine-4-ylmethyl)-6-chlorochromen-2-one (7) is a potent, orally bioavailable melanin concentrating hormone receptor 1 (MCHr1) antagonist that causes dose-dependent weight loss in diet-induced obese mice. Further evaluation of 7 in an anesthetized...
9.
Souers A, Gao J, Wodka D, Judd A, Mulhern M, Napier J, et al.
Bioorg Med Chem Lett
. 2005 May;
15(11):2752-7.
PMID: 15911251
A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism in both binding and functional assays. Several compounds that acted as MCHr1 antagonists were...
10.
Souers A, Gao J, Brune M, Bush E, Wodka D, Vasudevan A, et al.
J Med Chem
. 2005 Mar;
48(5):1318-21.
PMID: 15743174
Optimization of a high-throughput screening hit against melanin-concentrating hormone receptor 1 (MCHr1) led to the discovery of 2-(4-benzyloxy-phenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide (7a). This compound was found to be a high-affinity ligand for MCHr1...