Multifunctional arylsulfonamide derivatives with 5-HT/5-HT receptor antagonistic activity: a structural study.

Nowadays, a search for antagonists co-acting on serotonin receptor subtypes 6 and 7 (5-HTR and 5-HTR, respectively) is of great interest due to the increasing number of patients suffering from dementia and related behavioural and psychological symptoms. The X-ray crystal structures of four promising multifunctional ligands in the hydrochloride forms were determined, namely 4-(6-fluoro-1,2-benzoxazol-3-yl)-1-[3-(3-methylbenzenesulfonamido)propyl]piperidin-1-ium chloride, CHFNOS·Cl, (I), 4-(6-fluoro-1,2-benzoxazol-3-yl)-1-[4-(5-fluoro-3-methylbenzo[b]thiophene-2-sulfonamido)butyl]piperidin-1-ium chloride, CHFNOS·Cl, (II), 4-(6-fluoro-1,2-benzoxazol-3-yl)-1-[4-(6-fluorobenzo[b]thiophene-2-sulfonamido)butyl]piperidin-1-ium chloride, CHClFNOS·Cl, (III), and 4-(6-fluoro-1,2-benzoxazol-3-yl)-1-[3-(3-chloro-4-fluorobenzenesulfonamido)propyl]piperidin-1-ium chloride, CHClFNOS·Cl, (IV). Two pharmacologically important functional groups, i.

Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent.

A series of novel spirohydantoin derivatives with arylpiperazinylbutyl moiety were synthesized and evaluated for serotonin 5-HT1A, 5-HT2A, 5-HT7 and dopamine D2 receptors. Based on these data, four compounds were selected for further binding affinity assays on dopamine D1, D3, D4, and 5-HT2C, 5-HT6 as well as adrenergic α1 and α2C receptors, which are involved in various CNS diseases such as schizophrenia, anxiety and/or depression. The compound 14, 1-{4-[4-(2-metoxyphe-nyl)piperazin-1-yl]butyl}-3',4'-dihydro-2H,2'H,5H-spiro[imidazolidine-4,1'-naphthalene]-2,5-dione, with the most promising functional profile, mixed 5-HT2A/D2 antagonist and 5-HT1A partial agonist, was selected.

7-Meth-oxy-2-phenyl-chroman-4-one.

In the title compound, C(16)H(14)O(3), the ring O atom and the two adjacent non-fused C atoms, as well as the attached phenyl ring, exhibit static disorder [occupancy ratio 0.559 (12):0.441 (12)].

Self-assembly of long-chain quaternary ammonium cations in a hybrid inorganic-organic material with one-dimensional polymeric tribromidoplumbate(II).

catena-Poly[benzyldecyldimethylammonium [plumbate(II)-tri-μ-bromido]], {(C(19)H(34)N)[PbBr(3)]}(n), crystallizes as an inorganic-organic hybrid following monoclinic space-group symmetry P2(1)/c. The structure consists of extended chains running along the [001] direction and built of [PbBr(3)](-) units. These inorganic chains are separated by interdigitated ammonium cations which form hydrophilic layers through weak C-H···Br interactions.