N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT6 receptor antagonists

Nirogi, Ramakrishna; Konda, Jagadishu Babu; Kambhampati, Ramasastry; Shinde, Anil; Bandyala, Thrinath Reddy; Gudla, Parandhama; Kandukuri, Kiran Kumar; Jayarajan, Pradeep; Kandikere, Vishwottam; Dubey, P. K.

doi:10.1016/j.bmcl.2012.06.002

Cited by 13 publications

(3 citation statements)

References 33 publications

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“…The medicinal chemistry was described [492]. The effects to ameliorate scopolamine-induced memory deficits in object recognition and object location tasks in Wistar rats were reported [493] Novel chemical classes of 5-HT 6 receptor antagonists, i.e., aryl aminosulfonamide derivatives with a K b of 0.02 nM were reported by medicinal chemists at Suven, as were N 1 -arylsulfonyl-3-piperazinyl indole derivatives with a K i of 3.4 nM [494][495][496][497][498][499][500][501].…”

Section: -Ht 6 Receptor Antagonistsmentioning

confidence: 99%

Cognitive Enhancers (Nootropics). Part 1: Drugs Interacting with Receptors

Froestl

Muhs

Pfeifer

2012

JAD

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Cognitive enhancers (nootropics) are drugs to treat cognition deficits in patients suffering from Alzheimer's disease, schizophrenia, stroke, attention deficit hyperactivity disorder, or aging. Cognition refers to a capacity for information processing, applying knowledge, and changing preferences. It involves memory, attention, executive functions, perception, language, and psychomotor functions. The term nootropics was coined in 1972 when memory enhancing properties of piracetam were observed in clinical trials. In the meantime, hundreds of drugs have been evaluated in clinical trials or in preclinical experiments. To classify the compounds, a concept is proposed assigning drugs to 18 categories according to their mechanism(s) of action, in particular drugs interacting with receptors, enzymes, ion channels, nerve growth factors, re-uptake transporters, antioxidants, metal chelators, and disease-modifying drugs meaning small molecules, vaccines, and monoclonal antibodies interacting with amyloid-β and tau. For drugs, whose mechanism of action is not known, they are either classified according to structure, e.g., peptides, or their origin, e.g., natural products. The review covers the evolution of research in this field over the last 25 years.

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Section: -Ht 6 Receptor Antagonistsmentioning

confidence: 99%

Cognitive Enhancers (Nootropics). Part 1: Drugs Interacting with Receptors

Froestl

Muhs

Pfeifer

2012

JAD

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“…[36][37][38] Moreover, some studies indicated that the presence of hydroxyl units in the proximity of imine linkage improves the anticancer activity, by a synergistic antioxidant activity. 39,40 Bringing all this information together, the idea of binding betulin with imine units towards achieving new anticancer agents appears to be very promising. In this light, the present study focuses on the synthesis of new betulin imine derivatives, by reacting betulinic aldehyde with different aliphatic amines.…”

Section: Introductionmentioning

confidence: 99%

“…36–38 Moreover, some studies indicated that the presence of hydroxyl units in the proximity of imine linkage improves the anticancer activity, by a synergistic antioxidant activity. 39,40…”

Section: Introductionmentioning

confidence: 99%