A QSAR study on 2-(4-methylpiperazin-1-yl)quinoxalines as human histamine H<sub>4</sub> receptor ligands

Sharma, B. K.; Pilania, Pradeep; Singh, Prithvi; Prabhakar, Yenamandra S.

doi:10.3109/14756366.2010.519702

Cited by 5 publications

(1 citation statement)

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“…. In this work, Sharma and colleagues presented a total of eight QSAR models using two, three, and four descriptors to explain the structural requirements of this series to achieve adequate H 4 R affinity. The descriptors were from topological, steric, electronic, and hydrophobic nature, and BELm1 descriptor was present in all models, indicating its importance in H 4 R affinity.…”

Section: Sar E Qsar Studiesmentioning

confidence: 99%

Histamine H₄ Receptor Ligands: Future Applications and State of Art

Corrêa

Fernandes

2014

Chem Biol Drug Des

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Histamine is a chemical transmitter found practically in whole organism and exerts its effects through the interaction with H1 to H4 histaminergic receptors. Specifically, H4 receptors are found mainly in immune cells and blood-forming tissues, thus are involved in inflammatory and immune processes, as well as some actions in central nervous system. Therefore, H4 receptor ligands can have applications in the treatment of chronic inflammatory and immune diseases and may be novel therapeutic option in these conditions. Several H4 receptor ligands have been described from early 2000's until nowadays, being imidazole, indolecarboxamide, 2-aminopyrimidine, quinazoline, and quinoxaline scaffolds the most explored and discussed in this review. Moreover, several studies of molecular modeling using homology models of H4 receptor and QSAR data of the ligands are summarized. The increasing and promising therapeutic applications are leading these compounds to clinical trials, which probably will be part of the next generation of blockbuster drugs.

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Section: Sar E Qsar Studiesmentioning

confidence: 99%