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High potent and selective arylpiperazine derivatives as ligands for the 5-HT 1A receptor
- Source :
- Bioorganic & Medicinal Chemistry Letters. 10:1089-1092
- Publication Year :
- 2000
- Publisher :
- Elsevier BV, 2000.
-
Abstract
- This paper reports the synthesis and affinities on the 5-HT1A versus the α1A receptors of new arylpiperazinylalkylthiothienopyrimidine and thiadiazole derivatives 16–24 Download : Download high-res image (79KB) Download : Download full-size image Scheme 1 . Reagents and conditions: (i) CSCl2, CHCl3/H2O, NaHCO3, room temperature; (ii) N2H4.H2O, CHCl3, room temperature; (iii) KOH, EtOH, reflux; (iv) HCl, H2O, room temperature; (v) 1-(3-chloropropyl)-4-(2-methoxyphenyl, 2-nitrophenyl or 2-pyrimidinyl)piperazine, EtOH, reflux. . Arylpiperazines 16–23 show affinities values in the nanomolar range for the 5-HT1A receptor. The compound 16 is highly potent (Ki 0.26 nM, selectivity 28), the derivatives 20 and 21 are less potent, but highly selective (Ki 9.40 and 5.06 nM, selectivity 207 and 73, respectively).
- Subjects :
- Serotonin
Clinical Biochemistry
Pharmaceutical Science
Pyrimidinones
Thiophenes
Ligands
Biochemistry
Piperazines
Structure-Activity Relationship
chemistry.chemical_compound
Receptors, Adrenergic, alpha-1
Drug Discovery
Animals
Receptor
Piperazine
Molecular Biology
Arylpiperazine derivatives
5-HT receptor
Binding Sites
Chemistry
Organic Chemistry
Highly selective
Affinities
Combinatorial chemistry
Rats
Receptors, Serotonin
Reagent
Molecular Medicine
Selectivity
Receptors, Serotonin, 5-HT1
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 10
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....df3dd9cac658887b8cf92158c1956706