2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D-3 receptor

被引：15

作者：

Bolton, D ^{[1
]}

Boyfield, I ^{[1
]}

Coldwell, MC ^{[1
]}

Hadley, MS ^{[1
]}

Johns, A ^{[1
]}

Johnson, CN ^{[1
]}

Markwell, RE ^{[1
]}

Nash, DJ ^{[1
]}

Riley, GJ ^{[1
]}

Scott, EE ^{[1
]}

Smith, SA ^{[1
]}

Stemp, G ^{[1
]}

Wadsworth, HJ ^{[1
]}

Watts, EA ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT, HARLOW CM19 5AW, ESSEX, ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(97)00045-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles (8 - 15) has been prepared to investigate the effect on affinity and selectivity for the dopamine Dg receptor of modifying the substituent in the phenyl ring at the 2-position of the pyrrole. Sulfonate 7 and sulfonamides 12, 14, 15 were shown to have high affinities (pKi's 8.0 - 8.7) and selectivities (100 - 150-fold) for the D-3 over the D-2 receptor. (C) 1997, Elsevier Science Ltd.

引用

页码：485 / 488

页数：4

共 50 条

[41] Methyl 2-{1-[(Z)-3-methyl-5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-4-ylidene]ethylamino}-3-phenylpropanoate
Zhu, Hualing
Shi, Jun
Wei, Zhen
Dai, Ronghua
Zhang, Xin
ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O1352 - U938
[42] 2-[4-(dimethylamino)phenyl]-1-{[4-(dimethylamino)phenyl]methyl}-1H-benzimidazole
Yang, Shu-Ping
Han, Li-Jun
Wang, Da-Qi
Ding, Tie-Zhu
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2007, 63 : O365 - O367
[43] 1-(2-Methyl-5-phenyl-3-thienyl)2-(3-methyl-5-phenyl-2-thienyl)-3,3,4,4,5,5-hexafluorocyclopent-1-ene: a novel photochromic hybrid diarylethene
Pu, SZ
Liu, G
Chen, B
Wang, RJ
ACTA CRYSTALLOGRAPHICA SECTION C-STRUCTURAL CHEMISTRY, 2005, 61 (10): : O599 - O601
[44] 5-{2-(4-Chlorophenyl)-1-[2-(4-chloro-phenyl)-1-(3,4,5-trimethoxyphenyl)-ethoxy]ethyl}-1,2,3-trimethoxybenzene
Fu, Ying
Yuan, Mu
Hu, Xuemei
Yang, Yanshou
Hou, Hongxia
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2012, 68 : O1007 - +
[45] Synthesis and properties of 1-[(2-methyl-5-phenyl)-3-thienyl]-2-[(2-methyl-5-acetylenyl)-3-thienyl] perfluorocyclopentene
Zhang, C. C.
Hu, S. H.
Fan, C. B.
Pu, S. Z.
2015 2ND INTERNATIONAL CONFERENCE ON MATERIAL ENGINEERING AND APPLICATION (ICMEA 2015), 2015, : 289 - 294
[46] Transformations of methyl 2-[(E)-2-(dimethylamino)-1-(methoxycarbonyl)ethenyl]-1-methyl-1H-indole-3-carboxylate
Bevk, David
Groselj, Uros
Meden, Anton
Svete, Jurij
Stanovnik, Branko
HELVETICA CHIMICA ACTA, 2006, 89 (11) : 2774 - 2782
[47] 2-{5-[(1H-1,2,4-triazol-1-yl) methyl]-1,3,4-oxadiazol-2-ylthio}-1-(2,4-dichlorophenyl)-ethanone
Xu, LZ
Yu, GP
Yin, SM
Zhou, K
Yang, SH
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2005, 61 : O3375 - O3376
[48] Synthesis and Properties of a New Unsymmetrical Diarylethene 1-{2-methyl-[5-(4-trifluoromethyl)phenyl-3-thienyl]}-2-{[2-methyl-5-(3-chlorine)phenyl]-3-thienyl} Perfluorocyclopentene
Li, Shuying
Lu, Ruiming
Zhang, Daobin
Pu, Shouzhi
PROCEEDINGS OF THE 2015 INTERNATIONAL CONFERENCE ON MATERIALS CHEMISTRY AND ENVIRONMENTAL PROTECTION (MEEP-15), 2016, 4
[49] 1-(3-cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1,3-dihydroimidazol-2-one:: A selective high-affinity antagonist for the human dopamine D4 receptor with excellent selectivity over ion channels
Carling, RW
Moore, KW
Moyes, CR
Jones, EA
Bonner, K
Emms, F
Marwood, R
Patel, S
Patel, S
Fletcher, AE
Beer, M
Sohal, B
Pike, A
Leeson, PD
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (14) : 2706 - 2715
[50] SYNTHESIS AND ANTI-INFLAMMATORY ACTIVITY OF 2-{[5-(2-CHLOROPHENYL)-4H-1,2,4-TRIAZOL-3-YL]SULFANYL}-1-(SUBSTITUTED PHENYL)ETHANONES
Karande, N. A.
Rathi, L. G.
PHARMACEUTICAL CHEMISTRY JOURNAL, 2017, 51 (07) : 558 - 563

← 1 2 3 4 5 →