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Items: 27

1.

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

Chrovian CC, Soyode-Johnson A, Peterson AA, Gelin CF, Deng X, Dvorak CA, Carruthers NI, Lord B, Fraser I, Aluisio L, Coe KJ, Scott B, Koudriakova T, Schoetens F, Sepassi K, Gallacher DJ, Bhattacharya A, Letavic MA.

J Med Chem. 2018 Jan 11;61(1):207-223. doi: 10.1021/acs.jmedchem.7b01279. Epub 2017 Dec 20.

PMID:
29211470
2.

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A.

J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25.

PMID:
28493698
3.

Polypharmacology of Small-Molecule Modulators of the 5-Lipoxygenase Activating Protein (FLAP) Observed via a High-throughput Lipidomics Platform.

Song J, Liu X, Zhu J, Tootoonchi M, Keith JM, Meduna SP, Dvorak CA, Eccles W, Krawczuk PJ, Blevitt JM, Wu J, Rao NL, Lebsack AD, Milla ME.

J Biomol Screen. 2016 Feb;21(2):127-35. doi: 10.1177/1087057115607815. Epub 2015 Oct 6.

PMID:
26442913
4.

Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.

Dvorak CA, Coate H, Nepomuceno D, Wennerholm M, Kuei C, Lord B, Woody D, Bonaventure P, Liu C, Lovenberg T, Carruthers NI.

ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8. doi: 10.1021/acsmedchemlett.5b00247. eCollection 2015 Sep 10.

5.

Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.

Dvorak CA, Liu C, Shelton J, Kuei C, Sutton SW, Lovenberg TW, Carruthers NI.

ACS Med Chem Lett. 2012 Jun 11;3(8):637-9. doi: 10.1021/ml3000676. eCollection 2012 Aug 9.

6.

The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.

Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18.

PMID:
21802951
7.

Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT(7) antagonists.

Rudolph DA, Dvorak CA, Dvorak L, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):42-4. doi: 10.1016/j.bmcl.2010.11.078. Epub 2010 Nov 24.

PMID:
21159507
8.

Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.

Dvorak CA, Apodaca R, Xiao W, Jablonowski JA, Bonaventure P, Dugovic C, Shelton J, Lord B, Miller K, Dvorak LK, Lovenberg TW, Carruthers NI.

Eur J Med Chem. 2009 Oct;44(10):4098-106. doi: 10.1016/j.ejmech.2009.04.049. Epub 2009 May 13.

PMID:
19524331
9.

Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat.

Dugovic C, Shelton JE, Aluisio LE, Fraser IC, Jiang X, Sutton SW, Bonaventure P, Yun S, Li X, Lord B, Dvorak CA, Carruthers NI, Lovenberg TW.

J Pharmacol Exp Ther. 2009 Jul;330(1):142-51. doi: 10.1124/jpet.109.152009. Epub 2009 Apr 10.

PMID:
19363060
10.

Novel imidazole-based histamine H3 antagonists.

Jablonowski JA, Ly KS, Bogenstaetter M, Dvorak CA, Boggs JD, Dvorak LK, Lord B, Miller KL, Mazur C, Wilson SJ, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):903-7. doi: 10.1016/j.bmcl.2008.11.114. Epub 2008 Dec 6.

PMID:
19119007
11.

2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.

Shireman BT, Dvorak CA, Rudolph DA, Bonaventure P, Nepomuceno D, Dvorak L, Miller KL, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2103-8. doi: 10.1016/j.bmcl.2008.01.090. Epub 2008 Jan 30. Erratum in: Bioorg Med Chem Lett. 2008 Jul 15;18(14):4253.

PMID:
18282705
12.

Recent medicinal chemistry of the histamine H3 receptor.

Letavic MA, Barbier AJ, Dvorak CA, Carruthers NI.

Prog Med Chem. 2006;44:181-206. Review. No abstract available.

PMID:
16697898
13.

Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.

Venable JD, Cai H, Chai W, Dvorak CA, Grice CA, Jablonowski JA, Shah CR, Kwok AK, Ly KS, Pio B, Wei J, Desai PJ, Jiang W, Nguyen S, Ling P, Wilson SJ, Dunford PJ, Thurmond RL, Lovenberg TW, Karlsson L, Carruthers NI, Edwards JP.

J Med Chem. 2005 Dec 29;48(26):8289-98.

PMID:
16366610
14.

Palladium-catalyzed coupling of pyrazole triflates with arylboronic acids.

Dvorak CA, Rudolph DA, Ma S, Carruthers NI.

J Org Chem. 2005 May 13;70(10):4188-90.

PMID:
15876117
15.

4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.

Dvorak CA, Apodaca R, Barbier AJ, Berridge CW, Wilson SJ, Boggs JD, Xiao W, Lovenberg TW, Carruthers NI.

J Med Chem. 2005 Mar 24;48(6):2229-38.

PMID:
15771465
16.

Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.

McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK, Dvorak CA, Lovenberg TW, Carruthers NI, Jones TK.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9.

PMID:
15261275
17.

The first potent and selective non-imidazole human histamine H4 receptor antagonists.

Jablonowski JA, Grice CA, Chai W, Dvorak CA, Venable JD, Kwok AK, Ly KS, Wei J, Baker SM, Desai PJ, Jiang W, Wilson SJ, Thurmond RL, Karlsson L, Edwards JP, Lovenberg TW, Carruthers NI.

J Med Chem. 2003 Sep 11;46(19):3957-60.

PMID:
12954048
18.

A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.

Apodaca R, Dvorak CA, Xiao W, Barbier AJ, Boggs JD, Wilson SJ, Lovenberg TW, Carruthers NI.

J Med Chem. 2003 Aug 28;46(18):3938-44.

PMID:
12930154
19.

An asymmetric approach to spirocylic systems: a formal synthesis of zizaene.

Hughes RC, Dvorak CA, Meyers AI.

J Org Chem. 2001 Aug 10;66(16):5545-51.

PMID:
11485481
21.

Wavelength-dependent temporal properties of retinal horizontal cells in turtles.

Dvorak CA, Granda AM.

Vis Neurosci. 1990 May;4(5):427-35.

PMID:
2271453
22.

9-[(1,3-Dihydroxy-2-propoxy)methyl]guanine: a new potent and selective antiherpes agent.

Martin JC, Dvorak CA, Smee DF, Matthews TR, Verheyden JP.

J Med Chem. 1983 May;26(5):759-61.

PMID:
6302255
23.

Quantitative electron microscopic analysis of the optic nerve of the turtle, Pseudemys.

Geri GA, Kimsey RA, Dvorak CA.

J Comp Neurol. 1982 May 1;207(1):99-103.

PMID:
7096642
24.

Photoreceptor signals at visual threshold.

Dvorak CA, Granda AM, Maxwell JH.

Nature. 1980 Feb 28;283(5750):860-1.

PMID:
7360231
25.

Contrast sensitivity and acuity of the goldfish.

Northmore DP, Dvorak CA.

Vision Res. 1979;19(3):255-61. No abstract available.

PMID:
442550
26.

Computer analysis of spatial integration in vertebrate retinal horizontal cells.

Dvorak CA, Taylor TM.

IEEE Trans Biomed Eng. 1977 Mar;24(2):149-52. No abstract available.

PMID:
892818
27.

Methyl 5(6)-phenylsulfinyl-2-benzimidazolecarbamate, a new, potent anthelmintic.

Averkin EA, Beard CC, Dvorak CA, Edwards JA, Fried JH, Kilian JG, Kistner TP, Drudge JH, Lyons ET, Sharp ML, Corwin RM, Schiltz RA.

J Med Chem. 1975 Nov;18(11):1164-6.

PMID:
1177265

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