5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists

Liu, Kevin G.; Robichaud, Albert J.; Bernotas, Ronald C.; Yan, Yuli; Lo, Jennifer R.; Zhang, Meiyi; Hughes, Zoë A.; Huselton, Christine; Zhang, Guo Ming; Zhang, Jean Y.; Kowal, Dianne; Smith, Deborah L.; Schechter, Lee E.; Comery, Thomas A.

doi:10.1021/jm1007825

Cited by 60 publications

(18 citation statements)

References 24 publications

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“…nor the 5-HT 6 antagonist WAY-255315 at 1 mg/kg, p.o. (test compound A or SAM-315 according to (Liu et al, 2010)) alone enhanced retention for the familiar objects in the ORT (48-hour interval, time delay -induced deficit). However, the combination of the two compounds produced a significant retention of the memory as evident by the significant difference between the mean time exploring the novel and familiar objects.…”

Section: Discussionmentioning

confidence: 99%

The selective 5-HT 6 receptor antagonist SLV has putative cognitive- and social interaction enhancing properties in rodent models of cognitive impairment

Bruin

Loevezijn

Wicke

et al. 2016

Neurobiology of Learning and Memory

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Section: Discussionmentioning

confidence: 99%

The selective 5-HT 6 receptor antagonist SLV has putative cognitive- and social interaction enhancing properties in rodent models of cognitive impairment

Bruin

Loevezijn

Wicke

et al. 2016

Neurobiology of Learning and Memory

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“…3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (57) had emerged as the most potent 5-hydroxytryptamine antagonist (Liu et al, 2010).…”

Section: -Hydroxytryptamine Antagonistmentioning

confidence: 99%

Indazole: a medicinally important heterocyclic moiety

et al. 2011

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This article reveals the various biological activities of the heterocyclic compound, indazole, including anti-inflammatory, antimicrobial, antiHIV, anticancer, hypoglycemic, antiprotozoal, antihypertensive, and other activities. From the observed biological activities of the indazole moiety, it is concluded that the medicinal properties of indazole have to be explored in the near future for the treatment of various pathological conditions.

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“…1 They constitute key skeletal framework of many natural products as well as pharmaceuticals and have attracted considerable attention because of their important biological properties. 2 A few medicinally privileged compounds containing sulfone as the structural motif are shown in Fig. 1.…”

Section: Introductionmentioning

confidence: 99%

Biocatalytic Oxidation of Sulfides to Sulfones

Dhiman¹

2021

Orient. J. Chem

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This paper describes a method for the biocatalytic oxidation of sulfides. During the screening of microorganisms using pure cultures of Bacteria and Fungi for the oxidation of sulfides, it was observed that a number of strains of microorganisms, were able to oxidize various sulfides (1-4), but the desired sulfoxide was either not obtained or obtained only as a minor product. A close observation of the reaction showed complete oxidation and thus sulfone (5-8) formation had occurred in these cases.Sulfones are used to stabilize intermediates like α-radicals, α-anionsetc. and also used as cationic synthons in many known reactions.This prompted us to explore the sulfone synthesis by biocatalytic route.Approximately 20% of the strains tested (400 bacterial and 200 fungal) showed the formation of sulfone with conversion rate varying from 3 to 100% based on TLC analysis. There were two strains of fungi, Aspergillus ochraceus MTCC 5245 and Penicillium Funiculosum MTCC 5246 which showed excellent biocatalytic activity for oxidation sulfides to corresponding sulfones in high yield. In all these strains, the product was different from corresponding standard sulfoxide prepared by oxidation with m-chloroperbenzoic acid but well corresponded with the standard sample of sulfone prepared by oxidation of the corresponding sulfides with oxone®. The identity of sulfones in all cases was confirmed by 1H NMR.

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5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists

Cited by 60 publications

References 24 publications

The selective 5-HT 6 receptor antagonist SLV has putative cognitive- and social interaction enhancing properties in rodent models of cognitive impairment

The selective 5-HT 6 receptor antagonist SLV has putative cognitive- and social interaction enhancing properties in rodent models of cognitive impairment

Indazole: a medicinally important heterocyclic moiety

Biocatalytic Oxidation of Sulfides to Sulfones

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