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Items: 1 to 20 of 135

1.

Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists.

Ivachtchenko AV, Dmitriev DE, Golovina ES, Dubrovskaya ES, Kadieva MG, Koryakova AG, Kysil VM, Mitkin OD, Tkachenko SE, Okun IM, Vorobiov AA.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2133-6. doi: 10.1016/j.bmcl.2010.02.046. Epub 2010 Feb 14.

PMID:
20207539
2.

Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists.

Ivachtchenko AV, Golovina ES, Kadieva MG, Kysil VM, Mitkin OD, Tkachenko SE, Okun I.

Bioorg Med Chem. 2011 Feb 15;19(4):1482-91. doi: 10.1016/j.bmc.2010.12.055. Epub 2011 Jan 5.

PMID:
21277782
3.

Antagonists of 5-HT₆ receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines-Synthesis and 'structure-activity' relationship.

Ivachtchenko AV, Golovina ES, Kadieva MG, Kysil VM, Mitkin OD, Vorobiev AA, Okun I.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4273-80. doi: 10.1016/j.bmcl.2012.05.036. Epub 2012 May 17.

PMID:
22664127
4.

(3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.

Ivachtchenko AV, Dmitriev DE, Golovina ES, Kadieva MG, Koryakova AG, Kysil VM, Mitkin OD, Okun IM, Tkachenko SE, Vorobiev AA.

J Med Chem. 2010 Jul 22;53(14):5186-96. doi: 10.1021/jm100350r.

PMID:
20560595
5.

2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: new series of highly potent and specific serotonin 5-HT6 receptor antagonists.

Ivachtchenko AV, Golovina ES, Kadieva MG, Koryakova AG, Mitkin OD, Tkachenko SE, Kysil VM, Okun I.

Eur J Med Chem. 2011 Apr;46(4):1189-97. doi: 10.1016/j.ejmech.2011.01.038. Epub 2011 Feb 1.

PMID:
21333408
6.

Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists.

Ivachtchenko AV, Golovina ES, Kadieva MG, Koryakova AG, Kovalenko SM, Mitkin OD, Okun IM, Ravnyeyko IM, Tkachenko SE, Zaremba OV.

Bioorg Med Chem. 2010 Jul 15;18(14):5282-90. doi: 10.1016/j.bmc.2010.05.051. Epub 2010 May 24.

PMID:
20541425
7.

Synthesis and structure-activity relationship (SAR) of (5,7-disubstituted 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidin-2-yl)-methylamines as potent serotonin 5-HT(6) receptor (5-HT(6)R) antagonists.

Ivachtchenko AV, Golovina ES, Kadieva MG, Kysil VM, Mitkin OD, Tkachenko SE, Okun IM.

J Med Chem. 2011 Dec 8;54(23):8161-73. doi: 10.1021/jm201079g. Epub 2011 Nov 10.

PMID:
22029285
8.

Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives.

Bózsing D, Simonek I, Simig G, Jakóczi I, Gacsályi I, Lévay G, Tihanyi K, Schmidt E.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3097-9.

PMID:
12372510
9.

New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.

Brea J, Rodrigo J, Carrieri A, Sanz F, Cadavid MI, Enguix MJ, Villazón M, Mengod G, Caro Y, Masaguer CF, Raviña E, Centeno NB, Carotti A, Loza MI.

J Med Chem. 2002 Jan 3;45(1):54-71.

PMID:
11754579
10.

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
11.

4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.

Fletcher SR, Burkamp F, Blurton P, Cheng SK, Clarkson R, O'Connor D, Spinks D, Tudge M, van Niel MB, Patel S, Chapman K, Marwood R, Shepheard S, Bentley G, Cook GP, Bristow LJ, Castro JL, Hutson PH, MacLeod AM.

J Med Chem. 2002 Jan 17;45(2):492-503.

PMID:
11784153
12.

Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.

Wu YJ, He H, Hu S, Huang Y, Scola PM, Grant-Young K, Bertekap RL, Wu D, Gao Q, Li Y, Klakouski C, Westphal RS.

J Med Chem. 2003 Nov 6;46(23):4834-7.

PMID:
14584934
13.

Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.

Holmberg P, Sohn D, Leideborg R, Caldirola P, Zlatoidsky P, Hanson S, Mohell N, Rosqvist S, Nordvall G, Johansson AM, Johansson R.

J Med Chem. 2004 Jul 29;47(16):3927-30.

PMID:
15267230
14.

New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.

Jurczyk S, Kołaczkowski M, Maryniak E, Zajdel P, Pawłowski M, Tatarczyńska E, Kłodzińska A, Chojnacka-Wójcik E, Bojarski AJ, Charakchieva-Minol S, Duszyńska B, Nowak G, Maciag D.

J Med Chem. 2004 May 6;47(10):2659-66.

PMID:
15115407
15.

Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity.

Medina RA, Sallander J, Benhamú B, Porras E, Campillo M, Pardo L, López-Rodríguez ML.

J Med Chem. 2009 Apr 23;52(8):2384-92. doi: 10.1021/jm8014553.

PMID:
19326916
16.

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.

Bromidge SM, Bertani B, Borriello M, Bozzoli A, Faedo S, Gianotti M, Gordon LJ, Hill M, Zucchelli V, Watson JM, Zonzini L.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2338-42. doi: 10.1016/j.bmcl.2009.02.056. Epub 2009 Feb 20.

PMID:
19286377
17.

8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists.

Ivachtchenko AV, Mitkin OD, Tkachenko SE, Okun IM, Kysil VM.

Eur J Med Chem. 2010 Feb;45(2):782-9. doi: 10.1016/j.ejmech.2009.10.035. Epub 2009 Oct 31.

PMID:
19939513
18.
19.

Structure-activity relationship studies of CNS agents, Part 25. 4,6-di(heteroaryl)-2-(N-methylpiperazino)pyrimidines as new, potent 5-HT2A receptor ligands: a verification of the topographic model.

Mokrosz MJ, Strekowski L, Kozak WX, Duszyńska B, Bojarski AJ, Kłodzinska A, Czarny A, Cegła MT, Dereń-Wesoøek A, Chojnacka-Wójcik E, et al.

Arch Pharm (Weinheim). 1995 Sep;328(9):659-66.

PMID:
7487423
20.

Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.

Baraldi PG, Cacciari B, Romagnoli R, Spalluto G, Moro S, Klotz KN, Leung E, Varani K, Gessi S, Merighi S, Borea PA.

J Med Chem. 2000 Dec 14;43(25):4768-80.

PMID:
11123985
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