Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs

Zaręba, Przemysław; Drabczyk, Anna K.; Jaśkowska, Jolanta; Satała, Grzegorz

doi:10.1016/j.bmc.2020.115459

Cited by 13 publications

(1 citation statement)

References 34 publications

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“…The study is focused to increase affinity towards 5‐HT 6 R and reduce towards 5‐HT 7 R. In group 1 compound 73a showed the highest affinity towards 5‐HT 6 R (IC 50 value: 486 ± 86) and a small decrease in the affinity towards 5‐HT 1A and 5‐HT 7 receptor while compounds 74c and 74d are the most active compounds in group 2 (IC 50 value: 52 ± 7 and 57 ± 4). Structure–activity relationship of compounds 73 and 74 is shown in Figure 2 (Zaręba et al., 2020).…”

Section: Biological Activity and Structure–activity Relationship Of P...mentioning

confidence: 99%

The medicinal chemistry of piperazines: A review

Faizan,

Kumar,

Mazumder

et al. 2024

Chem Biol Drug Des

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The versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six‐membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability, and ADME characteristics, as well as improved target affinity and specificity. Various synthetic protocols have been reported for piperazine and its derivatives. In this review, we focused on recently published synthetic protocols for the synthesis of the piperazine and its derivatives. The structure–activity relationship concerning different biological activities of various piperazine‐containing drugs has also been highlighted to provide a good understanding to researchers for future research on piperazines.

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Section: Biological Activity and Structure–activity Relationship Of P...mentioning

confidence: 99%

The medicinal chemistry of piperazines: A review

Faizan,

Kumar,

Mazumder

et al. 2024

Chem Biol Drug Des

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Unraveling the Potential of Cyclic N‐Sulfonyl Ketimines in the MCR Universe

Fragkiadakis,

Fotopoulou,

Froudas

et al. 2024

Eur J Org Chem

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Cyclic N‐sulfonyl ketimines constitute an accessible class of lead‐like heterocycles with a vast application in both synthetic organic and medicinal chemistry. In this context, we harness the capabilities of these heterocycles in four different isocyanide‐based multicomponent reactions. Our goal was to create libraries of compounds with functional groups and vectors that are compatible for structural elaboration and optimization of their physical properties. We synthesized 15 unprecedented compounds with high diversity and complexity, whereas we have obtained four single crystal structures of each scaffold, unraveling their geometrical features and potential employment in drug discovery.

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Advances in drug design and therapeutic potential of selective or multitarget 5‐HT1A receptor ligands

Giorgioni,

Bonifazi,

Botticelli

et al. 2024

Medicinal Research Reviews

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Abstract5‐HT1A receptor (5‐HT1A‐R) is a serotoninergic G‐protein coupled receptor subtype which contributes to several physiological processes in both central nervous system and periphery. Despite being the first 5‐HT‐R identified, cloned and studied, it still represents a very attractive target in drug discovery and continues to be the focus of a myriad of drug discovery campaigns due to its involvement in numerous neuropsychiatric disorders. The structure‐activity relationship studies (SAR) performed over the last years have been devoted to three main goals: (i) design and synthesis of 5‐HT1A‐R selective/preferential ligands; (ii) identification of 5‐HT1A‐R biased agonists, differentiating pre‐ versus post‐synaptic agonism and signaling cellular mechanisms; (iii) development of multitarget compounds endowed with well‐defined poly‐pharmacological profiles targeting 5‐HT1A‐R along with other serotonin receptors, serotonin transporter (SERT), D2‐like receptors and/or enzymes, such as acetylcholinesterase and phosphodiesterase, as a promising strategy for the management of complex psychiatric and neurodegenerative disorders. In this review, medicinal chemistry aspects of ligands acting as selective/preferential or multitarget 5‐HT1A‐R agonists and antagonists belonging to different chemotypes and developed in the last 7 years (2017–2023) have been discussed. The development of chemical and pharmacological 5‐HT1A‐R tools for molecular imaging have also been described. Finally, the pharmacological interest of 5‐HT1A‐R and the therapeutic potential of ligands targeting this receptor have been considered.

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Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs

Cited by 13 publications

References 34 publications

The medicinal chemistry of piperazines: A review

The medicinal chemistry of piperazines: A review

Unraveling the Potential of Cyclic N‐Sulfonyl Ketimines in the MCR Universe

Advances in drug design and therapeutic potential of selective or multitarget 5‐HT1A receptor ligands

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