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» Authors » Jeffrey A Deskus

Jeffrey A Deskus

Explore the profile of Jeffrey A Deskus including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 17
Citations 56
Followers 0
Related Specialties
Biochemistry
Chemistry
Biology
Top 10 Co-Authors
Ronald J Mattson
Nicholas J Lodge
Thaddeus F Molski
Derek J Denhart
John E Macor
Jonathan L Ditta
Gail K Mattson
James R Epperson
H Dalton King
Yu-Wen Li
Published In
Bioorg Med Chem Lett
J Med Chem
Nucl Med Biol
Bioorg Med Chem
Affiliations
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Recent Articles
1.
Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors
Lodge N, Li Y, Chin F, Dischino D, Zoghbi S, Deskus J, et al.
Nucl Med Biol . 2014 May; 41(6):524-35. PMID: 24793011
Introduction: A radioligand for measuring the density of corticotropin-releasing factor subtype-1 receptors (CRF1 receptors) in living animal and human brain with positron emission tomography (PET) would be a useful tool...
2.
Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors
Ditta J, Denhart D, Deskus J, Epperson J, Meng Z, Gao Q, et al.
Bioorg Med Chem Lett . 2013 Apr; 23(10):2948-50. PMID: 23578689
Racemic 5-(trans-2-aminomethylcyclopropyl)indoles, 5-(trans-2-aminomethylcyclopentyl) indoles, and 5-(cis-2-aminomethylcyclopentyl)indoles were synthesized and evaluated as selective serotonin reuptake inhibitors. These analogs followed SAR trends similar to those previously reported for 3-cycloalkyl substituted indoles. The...
3.
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents
Deskus J, Dischino D, Mattson R, Ditta J, Parker M, Denhart D, et al.
Bioorg Med Chem Lett . 2012 Sep; 22(21):6651-5. PMID: 23010264
Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET radioligand. Compound [(18)F]10 was prepared with high radiochemical purity...
4.
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors
King H, Meng Z, Deskus J, Sloan C, Gao Q, Beno B, et al.
J Med Chem . 2010 Oct; 53(21):7564-72. PMID: 20949929
A series of conformationally restricted homotryptamines has been synthesized and shown to be potent inhibitors of hSERT. Conformational restriction of the homotryptamine side chain was attained by the insertion of...
5.
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable...
Hartz R, Ahuja V, Zhuo X, Mattson R, Denhart D, Deskus J, et al.
J Med Chem . 2009 Dec; 52(23):7653-68. PMID: 19954247
Detailed metabolic characterization of 8, an earlier lead pyrazinone-based corticotropin-releasing factor-1 (CRF(1)) receptor antagonist, revealed that this compound formed significant levels of reactive metabolites, as measured by in vivo and...
6.
Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors
Denhart D, Deskus J, Ditta J, Gao Q, King H, Kozlowski E, et al.
Bioorg Med Chem Lett . 2009 Jun; 19(15):4031-3. PMID: 19560923
A series of racemic 3-(trans-2-aminomethylcyclopentyl)indoles was synthesized and found to have potent binding to the human serotonin transporter (hSERT). The most active analog was synthesized stereospecifically and the active enantiomer...
7.
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz R, Ahuja V, Arvanitis A, Rafalski M, Yue E, Denhart D, et al.
J Med Chem . 2009 Jun; 52(14):4173-91. PMID: 19552437
Evidence suggests that corticotropin-releasing factor-1 (CRF(1)) receptor antagonists may offer therapeutic potential for the treatment of diseases associated with elevated levels of CRF such as anxiety and depression. A pyrazinone-based...
8.
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz R, Ahuja V, Rafalski M, Schmitz W, Brenner A, Denhart D, et al.
J Med Chem . 2009 Jun; 52(14):4161-72. PMID: 19552436
A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropin-releasing factor-1 (CRF(1)) receptor antagonists. Selected compounds proved efficacious in an anxiety model in rats; however, pharmacokinetic properties...
9.
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor
King H, Denhart D, Deskus J, Ditta J, Epperson J, Higgins M, et al.
Bioorg Med Chem Lett . 2007 Sep; 17(20):5647-51. PMID: 17766113
A series of hybrid molecules containing the cyclopropylmethylamino side chain found in homotryptamine (1S,2S)-2c and an isosteric heteroaryl or naphthyl core were prepared and their binding affinities for the human...
10.
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors
Deskus J, Epperson J, Sloan C, Cipollina J, Dextraze P, Qian-Cutrone J, et al.
Bioorg Med Chem Lett . 2007 Mar; 17(11):3099-104. PMID: 17391962
A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were determined. In particular, a nitrile substituent at the C5...