104842-73-1Relevant articles and documents
DIKETO-PIPERAZINE AND PIPERIDINE DERIVATIVES AS ANTIVIRAL AGENTS
-
Page/Page column 43, (2008/06/13)
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor
Tran, Joe A.,Pontillo, Joseph,Fleck, Beth A.,Marinkovic, Dragan,Arellano, Melissa,Tucci, Fabio C.,Lanier, Marion,Saunders, John,Jiang, Wanlong,Chen, Caroline W.,Foster, Alan C.,Chen, Chen
, p. 3693 - 3696 (2008/09/21)
A series of 2-pyridinylpiperazines derived from β-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki = 6.5 nM) possessed high potency.
Atypical Antipsychotic Agents: Patterns of Activity in a Series of 3-Substituted 2-Pyridinyl-1-piperazine Derivatives
New, James S.,Yevich, Joseph P.,Temple, Davis L.,New, Kimberly B.,Gross, Sharon M.,et al.
, p. 618 - 624 (2007/10/02)
A series of 3-substituted 2-pyridinyl-1-piperazine derivaties have been appended to cyclic imide groups and evaluated for their potential antipsochotic activity.The dopamine receptor affinities of these target molecules, as well as their ability to block apomorphine-induced stereotypy or reverse neuroleptic-induced catalepsy, was dependent on the lipophilic and electronic characteristics of the substituent situated on the pyridine ring.Groups with +? and -? values were most consistent with the desired biological profile of the target molecules, the cyano moiety being the optimum choice.Evaluation of compound 12 in a monkey model of amphetamine psychosis, and the regional selectivity it expresses for the A10 dopaminergic cell bodies in electrophysiological experiments, suggest this compound would be an atypical antipsychotic agent with few side effects.
ANTIPSYCHOTIC CYCLIC IMIDE DERIVATIVES OF 2-(4-BUTYLPIPERAZIN-1-YL) PYRIDINES, COMPOSITIONS AND USE
-
, (2008/06/13)
Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a substituted pyridin-2-yl ring and the second substituent is a butylene chain attached to cyclic imide heterocycles such as azaspiro 4.5!decanedione, dialkylglutarimide, thiazolidinedione, spirocyclopentylthiazolidinedione, or morpholine-2,6-dione. The compounds have psychotropic properties and 2-4-4-(2,4-dioxo-1-thia-3-azaspiro 4. 5!nonane-3-yl)butyl!-1-piperazinyl!-pyridine-3-carboxaldehyde is a typical embodiment having selective antipsychotic activity.
ANTIPSYCHOTIC CYCLIC IMIDE DERIVATIVES OF 2-(4-BUTYLPIPERAZIN-1-YL)PYRIDINES, COMPOSITIONS AND USE
-
, (2008/06/13)
Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a substituted pyridin-2-yl ring and the second substituent is a butylene chain attached to cyclic imide heterocycles such as azaspiro 4.5!decanedione, dialkylglutarimide, thiazolidinedione, spirocyclopentylthiazolidinedione, or morpholine-2,6-dione. The compounds have psychotropic properties and 2-4-4-(2,4-dioxo-1-thia-3-azaspiro 4. 5!nonane-3-yl)butyl!-1-piperazinyl!pyridine-3-carboxaldehyde is a typical embodiment having selective antipsychotic activity.