Recent advances with 5‐HT3 modulators for neuropsychiatric and gastrointestinal disorders

R Juza, P Vlcek, E Mezeiova, K Musilek… - Medicinal research …, 2020 - Wiley Online Library
Abstract Serotonin (5‐hydroxytryptophan [5‐HT]) is a biologically active amine expressed in
platelets, in gastrointestinal (GI) cells and, to a lesser extent, in the central nervous system …

Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors

BA Sparling, EF DiMauro - Bioorganic & Medicinal Chemistry Letters, 2017 - Elsevier
The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of
nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT 3 R), γ-aminobutyric acid (GABA …

New quinoxaline derivatives as dual Pim-1/2 kinase inhibitors: Design, synthesis and biological evaluation

B Oyallon, M Brachet-Botineau, C Logé, T Robert… - Molecules, 2021 - mdpi.com
Proviral integration site for Moloney murine leukemia virus (Pim)-1/2 kinase overexpression
has been identified in a variety of hematologic (eg, multiple myeloma or acute myeloid …

Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors

B Oyallon, M Brachet-Botineau, C Logé… - European Journal of …, 2018 - Elsevier
We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human
proviral integration site for Moloney murine leukemia virus-1 (Hs Pim-1) kinase. Seventeen …

Antidepressant-like effects of a novel 5-HT3 receptor antagonist 6z in acute and chronic murine models of depression

D Gupta, M Radhakrishnan, Y Kurhe… - Acta Pharmacologica …, 2014 - nature.com
Aim: To investigate the antidepressant-like effects of a novel 5-HT 3 receptor antagonist N-
(benzo [d] thiazol-2-yl)-3-methoxyquinoxalin-2-carboxamide (6z) in acute and chronic …

Anxiolytic-like effect of (4-benzylpiperazin-1-yl)(3-methoxyquinoxalin-2-yl) methanone (6g) in experimental mouse models of anxiety

S Bhatt, R Mahesh, T Devadoss… - Indian Journal of …, 2013 - journals.lww.com
Aim: The present study was designed to investigate the anxiolytic activity of 6g, a novel
serotonin type-3 receptor (5-HT 3) receptor antagonist in experimental mouse models of …

Piperazine Analogs of Naphthyridine‐3‐carboxamides and Indole‐2‐carboxamides: Novel 5‐HT3 Receptor Antagonists with Antidepressant‐Like Activity

AK Dhar, R Mahesh, A Jindal, S Bhatt - Archiv der Pharmazie, 2015 - Wiley Online Library
Abstract Series of piperazine analogs of naphthyridine‐3‐carboxamides and indole‐2‐
carboxamides were designed using a ligand‐based approach with consideration of the …

Design, Synthesis and Evaluation of Antidepressant Activity of Novel 2‐Methoxy 1, 8 Naphthyridine 3‐Carboxamides as 5‐HT3 Receptor Antagonists

R Mahesh, AK Dhar, A Jindal… - Chemical Biology & Drug …, 2014 - Wiley Online Library
A series of novel 1, 8‐naphthyridine‐3‐carboxamides as 5‐HT 3 receptor antagonists were
synthesized with an intention to explore the antidepressant activity of these compounds. The …

Antidepressant & anxiolytic activities of N-(pyridin-3-yl) quinoxalin-2-carboxamide: A novel serotonin type 3 receptor antagonist in behavioural animal models

DK Pandey, T Devadoss, N Modak… - Indian Journal of …, 2016 - journals.lww.com
Methods: Antidepressant activity was evaluated in preliminary tests such as forced swim and
tail suspension tests (FST & TST). Anti-anxiety effect of QCF-21 was investigated by …

Potassium 6-Oxo-7,13,16,22-tetraazatetracyclo[12.6.2.18,12.017,21]tricosa-1(20),8(23),9,11,14,16,18,21-octaen-2-yne-15-carboxylate

C Blouet, S Letast, T Robert, S Bach, N Pinaud… - Molbank, 2023 - mdpi.com
Potassium 6-oxo-7, 13, 16, 22-tetraazatetracyclo [12.6. 2.18, 12.017, 21] tricosa-1 (20), 8
(23), 9, 11, 14, 16, 18, 21-octaen-2-yne-15-carboxylate was synthesized through a multi-step …