61895-53-2Relevant academic research and scientific papers
New arylpiperazines with flexible versus partly constrained linker as serotonin 5-HT1A/5-HT7 receptor ligands
Kowalski, Piotr,Mitka, Katarzyna,Jaskowska, Jolanta,Duszynska, Beata,Bojarski, Andrzej J.
, p. 339 - 348 (2013/07/19)
A series of new long-chain arylpiperazine (LCAP) derivatives with flexible and partly constrained alkyl linker were synthesized and investigated in vitro as potential serotonin 5-HT1A and 5-HT7 receptor ligands. The compounds were prepared by a two-step procedure using naphthalimide and 2H-1,3-benzoxazine-2,4(3H)-dione as imides, and 1-(2-methoxyphenyl)piperazine (o-OMe-PhP) and 1,2,3,4-tetrahydroisoquinoline (THIQ) as amine pharmacophores. Modifications of the spacer structure included introduction of flexible penta- and hexamethylene chains as well as partly constrained m- and p-xylyl moieties. In general, the new compounds were more active at the 5-HT1A than at the 5-HT7 receptor, and the o-OMe-PhP derivatives displayed higher affinities than their respective THIQ analogs. The spacer modifications had little effect on the observed in vitro activities. Within the o-OMe-PhP series, except for a small binding reduction for ligands containing the m-xylyl moiety, there was no substantial change in the compounds' potency at both receptors, while for the THIQ derivatives a clear structure-activity relationship was visible only for the interaction of the compounds with the 5-HT7 receptor, which strongly favored flexible analogs. New LCAP derivatives with flexible and partly constrained alkyl linker were tested as potential serotonin 5-HT1A and 5-HT7 receptor ligands. The spacer structure was modified by introduction of flexible penta- and hexamethylene chains and partly constrained m- and p-xylyl moieties. The new compounds were more active at the 5-HT1A than at the 5-HT7 receptor. o-OMe-PhP derivatives displayed higher affinities than their respective THIQ analogs. The spacer modifications had little effect on the observed in vitro activities. Copyright
Traceless approach for the synthesis of 3,5-disubstituted thiohydantoins on functionalized ionic-liquid support
Yao, Chao,Zhang, Yandong,Zhang, Guolin,Chen, Wenteng,Yu, Yongping,Houghten, Richard A.
experimental part, p. 717 - 724 (2011/03/19)
A traceless approach for the synthesis of 3,5-disubstituted thiohydantoins on a novel functionalized ionic-liquid support, 5, is described. Acylation of benzylamine functionalized ionic-liquid support with amino acids yielded ionic-liquid-supported amino acids, which reacted with isothiocyanates to afford ionic-liquid-supported thioureas. Following intramolecular cyclization cleavage from the ionic-liquid support by trifluoroacetic acid (TFA), the desired 3,5-disubstituted thiohydantoins were obtained in good yields and purities. The efficiency of this ionic-liquid-phase strategy facilitated isolation and analysis of intermediates and removal of excess reagents and by-products during the reaction process.
S-adenosyl methionine decarboxylase inhibitors
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, (2008/06/13)
The adenosine derivatives represented by the following formula: STR1 and the pharmaceutically acceptable salts thereof wherein R is H or C1 -C7 alkyl, Q is the moiety of the formula STR2 wherein V is H or --COOH X is H, F, Cl, Br, and Z is H, F, Cl, or Br. These compounds are inhibitors of S-adenosylmethione decarboxylase and are useful for treating parasitic infections.
5'-amine substituted adenosine analogs as immunosuppressants
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, (2008/06/13)
The present invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of certain 5'-amine substituted adenosine analogs.
