Synthesis of aminopyrrolo[1,2-a]thieno[3,2-e]pyrazine derivatives as serotoninergic 5-HT7 ligands

被引:3
|
作者
Pave, Gregoire [1 ]
Lazar, Said [2 ]
Lesnard, Aurelien [3 ]
Rault, Sylvain [3 ]
Guillaumet, Gerald [1 ]
机构
[1] Univ Orleans, CNRS, Inst Chim Organ & Analyt, UMR 6005, BP 6759, F-45067 Orleans, France
[2] Univ Hassan II Mohammedia, Lab Biochim Environm & Agroalimentaire, URAC 36, Mohammadia 20800, Morocco
[3] Univ Caen, FR CNRS 3038, CERMN EA 4258, F-14032 Caen, France
关键词
Serotonin; 5-HT(7)Rs ligands; affinity; aminopyrrolothienopyrazines; RECEPTOR ANTAGONIST SB-269970; POTENTIAL ANXIOLYTIC AGENTS; 3,4-DIHYDRO-3-AMINO-2H-1-BENZOPYRAN DERIVATIVES; HIGH-AFFINITY; PHARMACOPHORES; RELAXATION; EXPRESSION; AGONISTS; CLONING;
D O I
10.3998/ark.5550190.0011.a11
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of piperazinopyrrolo[1,2-a]thieno[3,2-e]pyrazine derivatives were prepared and evaluated to determine their affinity for the 5-HT7 receptor. Various substitutions on piperazine were explored as well as replacement of the piperazine by other amines.
引用
收藏
页码:116 / 131
页数:16
相关论文
共 50 条
  • [31] Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands
    Ofori, Edward
    Zhu, Xue Y.
    Etukala, Jagan R.
    Peprah, Kwakye
    Jordan, Kamanski R.
    Adkins, Adia A.
    Bricker, Barbara A.
    Kang, Hye J.
    Huang, Xi-Ping
    Roth, Bryan L.
    Ablordeppey, Seth Y.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2016, 24 (16) : 3464 - 3471
  • [32] Synthesis of New Serotonin 5-HT7 Receptor Ligands. Determinants of 5-HT7/5-HT1A Receptor Selectivity
    Medina, Rocio A.
    Sallander, Jessica
    Benhamu, Bellinda
    Porras, Esther
    Campillo, Mercedes
    Pardo, Leonardo
    Lopez-Rodriguez, Maria L.
    JOURNAL OF MEDICINAL CHEMISTRY, 2009, 52 (08) : 2384 - 2392
  • [33] A new synthesis of pyrido[1,2-a]thieno[3,2-d]pyrimidines
    Briel, D
    PHARMAZIE, 2003, 58 (11): : 836 - 837
  • [34] New fused pyrazines.: Synthesis of pyrido[3′,2′:4,5]thieno[2,3-e]pyrrolo[1,2-a]pyrazine derivatives
    El-Kashef, HS
    El-Dean, AMK
    Geies, AA
    Lancelot, JC
    Dallemagne, P
    Rault, S
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2000, 37 (06) : 1521 - 1526
  • [35] NEW 5H-[1,3]THIAZOLO[3,2-A]PYRIDO[3,2-E]PYRIMIDIN-5-ONE DERIVATIVES AS DIURETICS
    MONGE, A
    MARTINEZMERINO, V
    SIMON, MA
    SANMARTIN, C
    ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH, 1995, 45-1 (03): : 306 - 310
  • [36] Synthesis and rearrangement of cycloalkyl[1,2-e]oxazolo[3,2-a]pyrimidin-8/9-ones:: an access to cycloalkyl[1,2-d]oxazolo[3,2-a]pyrimidin-5-ones
    Adetchessi, OS
    Léger, JM
    Guillon, J
    Forfar-Bares, I
    Bosc, JJ
    Jarry, C
    TETRAHEDRON, 2005, 61 (18) : 4453 - 4460
  • [37] 2-Aminothiophenes as building blocks in heterocyclic synthesis: Synthesis and antimicrobial evaluation of a new class of pyrido[1,2-a]thieno[3,2-e]pyrimidine, quinoline and pyridin-2-one derivatives
    Behbehani, Haider
    Ibrahim, Hamada Mohamed
    Makhseed, Saad
    Elnagdi, Mohamed H.
    Mahmoud, Huda
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2012, 52 : 51 - 65
  • [38] STUDIES IN HETEROCYCLICS .10. SYNTHESIS OF IIH-NAPHTHO[1,2-E]THIAZOLO[3,2-A]PYRIMIDINES
    SONDHI, SM
    RALHAN, NK
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1977, 15 (08): : 697 - 699
  • [39] Synthetic route to 4,5-dihydro-9H-pyrido[1,2-a] thieno[3,2-e]pyrimidine derivatives through 1,3-dipolar cycloaddition
    Santagati, A
    Granata, G
    Santagati, M
    JOURNAL OF CHEMICAL RESEARCH-S, 2001, (08): : 304 - 306
  • [40] SYNTHESIS OF 1-ARYL-6,7,8,9-TETRAHYDRO[1]BENZOTHIENO[3,2-E]THIAZOLO[3,2-A]PYRIMIDIN-5(H)-ONES
    GAKHAR, HK
    MADAN, A
    KUMAR, N
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1980, 19 (04): : 250 - 252