Results 41 to 50 of about 43,876 (205)

Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity [PDF]

, 2019
A series of benzo[b]thiophen-3-ols were synthesised and investigated as potential human monoamine oxidase (hMAO) inhibitors in vitro as well as ex vivo in rat cortex synaptosomes by means of evaluation of 3,4-dihydroxyphenylacetic acid/dopamine (DOPAC/DA)
Alcaro, Stefano, Bagetta, Donatella, Carradori, Simone, Chimenti, Paola, Ferrante, Claudio, Guglielmi, Paolo, Leone, Sheila, Ortuso, Francesco, Petzer, Anél, Petzer, Jacobus P, Recinella, Lucia, Rotondi, Giulia, Secci, Daniela, Zengin, Gokhan   +13 more
core   +1 more source

Stereoselective Biotransformation: Transfer of Learning to Advance Drug Metabolism and Biocatalysis

Angewandte Chemie, EarlyView.
Understanding stereoselective biotransformations has implications for predicting drug disposition and response and may also inspire novel biocatalytic and biomimetic strategies to address challenges in metabolite and API synthesis. ABSTRACT Chirality is an important determinant of drug action, as enantiomers can exhibit markedly different ...
Grace A. Okunlola, Godwin A. Aleku
wiley   +2 more sources

Design, synthesis, docking studies and monoamine oxidase inhibition of a small library of 1-acetyl- and 1-thiocarbamoyl-3,5-diphenyl-4,5-dihydro-(1h)-pyrazoles [PDF]

, 2019
New N-acetyl/N-thiocarbamoylpyrazoline derivatives were designed and synthesized in high yields to assess their inhibitory activity and selectivity against human monoamine oxidase A and B.
Carradori, Simone, Chimenti, Paola, Cirilli, Roberto, Guglielmi, Paolo, Petzer, Anél, Petzer, Jacobus P., Poli, Giulio, Rotondi, Giulia, Secci, Daniela   +8 more
core   +2 more sources

Fluoxetine: a case history of its discovery and preclinical development [PDF]

, 2014
Introduction: Depression is a multifactorial mood disorder with a high prevalence worldwide. Until now, treatments for depression have focused on the inhibition of monoaminergic reuptake sites, which augment the bioavailability of monoamines in the CNS ...
Bel N, Bergstrom RF, Bravo L, Bremner JD, Burrows GD, Chouinard G, Datla KP, Esther Berrocoso, Juan Antonio Mico, Kreiss DS, Laura Perez-Caballero, Lemberger L, Li Q, Lidia Bravo, Maj J, Nibuya M, Owens MJ, Rutter JJ, Sonia Torres-Sanchez, Stevens JC, Wong DT   +20 more
core   +2 more sources

Structure-Activity Relationship Analysis of 3-Phenylcoumarin-Based Monoamine Oxidase B Inhibitors

Frontiers in Chemistry, 2018
Monoamine oxidase B (MAO-B) catalyzes deamination of monoamines such as neurotransmitters dopamine and norepinephrine. Accordingly, small-molecule MAO-B inhibitors potentially alleviate the symptoms of dopamine-linked neuropathologies such as depression ...
Sanna Rauhamäki, Pekka A. Postila, Sanna Niinivehmas, Sami Kortet, Sami Kortet, Emmi Schildt, Emmi Schildt, Mira Pasanen, Elangovan Manivannan, Elangovan Manivannan, Mira Ahinko, Pasi Koskimies, Niina Nyberg, Pasi Huuskonen, Elina Multamäki, Markku Pasanen, Risto O. Juvonen, Hannu Raunio, Juhani Huuskonen, Olli T. Pentikäinen, Olli T. Pentikäinen   +20 more
doaj   +1 more source

A meta-analysis of pharmacotherapy for social anxiety disorder: an examination of efficacy, moderators, and mediators [PDF]

, 2017
INTRODUCTION: Social anxiety disorder (SAD) is among the most prevalent mental disorders, associated with impaired functioning and poor quality of life. Pharmacotherapy is the most widely utilized treatment option.
Borenstein M, Hofmann SG, Jasper Smits, Joshua Curtiss, Leigh Andrews, Lipsey MW, Michelle Davis, Stefan G. Hofmann, Stein MB   +8 more
core   +2 more sources

N-methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor [PDF]

, 2014
On the basis of N-((5-(3-(1-benzylpiperidin-4-yl)propoxy)-1-methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (II, ASS234) and QSAR predictions, in this work we have designed, synthesized, and evaluated a number of new indole derivatives from which ...
Agbaba, D., Alcaro, S., Bautista-Aguilera, O.M., Chioua, M., De Andrés, L., Filipic, S., Marco-Contelles, J., Nikolic, K., Ortuso, F., Ramsay, R.R., Rodríguez-Franco, M.I., Samadi, A., Soriano, E., Yañez, M.   +13 more
core   +3 more sources

Design and Synthesis of Novel and Potent Monoamine Oxidase Inhibitors

CHIMIA, 1995
Reversible and selective monoamine oxidase-A inhibitors (RIMA's) like moclobemide (Aurorix®) have rehabilitated the use of MAO inhibitors as drugs of choice in depression.
Quirico Branca, Roland Jakob-Røtne, Rolf Kettler, Stephan Röver, Michelangelo Scalone   +4 more
doaj   +2 more sources

Concentration of norepinephrine, serotonin, and histamine, and of amine-metabolizing enzymes in mammalian adipose tissue

Journal of Lipid Research, 1963
The norepinephrine content of adipose tissue is shown to be very different in various animal species and different sites of origin, ranging from 0.03-1.4 μg/g. Adipose tissue also contains considerable amounts of serotonin (0.01-1.04 μg/g) and histamine (
K. Stock, E.O. Westermann
doaj   +1 more source

Reactive oxygen-related diseases: therapeutic targets and emerging clinical indications [PDF]

, 2015
SIGNIFICANCE Enhanced levels of reactive oxygen species (ROS) have been associated with different disease states. Most attempts to validate and exploit these associations by chronic antioxidant therapies have provided disappointing results. Hence, the
Ana I. Casas, Andreas Daiber, Antonio Cuadrado, Brunner HG, Fabio Di Lisa, Ghassan J. Maghzal, Hampton MB, Harald H.H.W. Schmidt, Hou YC, Karl H. Krause, Klebanoff SJ., Liu VW, Manuela G. López, Nina Kaludercic, Pietro Ghezzi, Roland Stocker, Sandler M, Savenkova ML, Sonia Leach, Tamara Seredenina, V. Thao-Vi Dao, Vincent Jaquet   +21 more
core   +3 more sources