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Juho-Matti Renko, Susanne Bäck, Merja H Voutilainen, T Petteri Piepponen, Ilkka Reenilä, Mart Saarma, Raimo K Tuominen
Neurotrophic factors (NTFs) hold potential as disease-modifying therapies for neurodegenerative disorders like Parkinson's disease. Glial cell line-derived neurotrophic factor (GDNF), cerebral dopamine neurotrophic factor (CDNF), and mesencephalic astrocyte-derived neurotrophic factor (MANF) have shown neuroprotective and restorative effects on nigral dopaminergic neurons in various animal models of Parkinson's disease. To date, however, their effects on brain neurochemistry have not been compared using in vivo microdialysis...
January 18, 2018: Molecular Neurobiology
Avinash C Tripathi, Savita Upadhyay, Sarvesh Paliwal, Shailendra K Saraf
This review aims to be a comprehensive, authoritative, critical, and readable review of general interest to the medicinal chemistry community because it focuses on the pharmacological, chemical, structural and computational aspects of diverse chemical categories as monoamine oxidase inhibitors (MAOIs). Monoamine oxidases (MAOs), namely MAO-A and MAO-B represent an enormously valuable class of neuronal enzymes embodying neurobiological origin and functions, serving as potential therapeutic target in neuronal pharmacotherapy, and hence we have coined the term "Neurozymes" which is being introduced for the first time ever...
January 4, 2018: European Journal of Medicinal Chemistry
Simone Carradori, Daniela Secci, Jacques P Petzer
Monoamine oxidase (MAO) inhibitors, after the initial "golden age", are currently used as third-line antidepressants (selective MAO-A inhibitors) or clinically enrolled as co-adjuvants for neurodegenerative diseases (selective MAO-B inhibitors). However, the research within this field is always increasing due to their pivotal role in modulating synaptic functions and monoamines metabolism. Areas covered: In this paper, MAO inhibitors (2015-2017) are disclosed ordering all the patents according to their chemical scaffold...
January 11, 2018: Expert Opinion on Therapeutic Patents
Maciej Gawlik, Jakub Trawiński, Robert Skibiński
The imitation of phase I metabolism of moclobemide and toloxatone, two monoamine oxidase type A (MAO-A) inhibitors, was performed with the use of titanium dioxide photocatalytic process. Ultra high pressure liquid chromatography system coupled with an accurate hybrid ESI-Q-TOF mass spectrometer was used for the evaluation of metabolic profiles, structural elucidation of the identified transformation products and quantitative analysis of the process. Based on high resolution MS and MS/MS data, eleven transformation products were characterized in photocatalytic experiments for moclobemide and seven products for toloxatone...
January 8, 2018: European Journal of Pharmaceutical Sciences
Gülhan Turan-Zitouni, Weiam Hussein, Begüm Nurpelin Sağlık, Aouatef Tabbi, Büşra Korkut
A new series of N-pyridyl-hydrazone derivatives was synthesized by using a simple and efficient method. The final compounds obtained were screened for their inhibitory potency against monoamine oxidase (MAO) A and B. The newly synthesized compounds 2a-2n specifically inhibited monoamine oxidases, displaying notably low IC50 values. Compounds 2i and 2j, with a CF₃ and OH group on the 4-position of the phenyl ring, respectively, showed considerable MAO-A and MAO-B inhibitory activities. Compounds 2k, 2l and 2n, with N-methylpyrrole, furan and pyridine moieties instead of the phenyl ring, were the most powerful and specific inhibitors of MAO-A, with IC50 values of 6...
January 8, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Derya Osmaniye, Serkan Levent, Ulviye Acar Çevik, Abdullah Burak Karaduman, Yusuf Özkay, Zafer Asım Kaplancıklı
Twenty-six novel thiosemicarbazone derivative B1-B26 were synthesized via condensation reactions between the corresponding thiosemicarbazides and aldehydes. The chemical characterization of the compounds was carried out by infrared (IR), mass (MS), proton and carbon nuclear magnetic resonance (¹H- and 13C-NMR) spectroscopic analyses. The compounds were investigated for their monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) inhibitory activity and most of them were more potent against MAO-A enzyme when compared with MAO-B enzyme...
December 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Makoto Naoi, Wakako Maruyama, Masayo Shamoto-Nagai
Type A and B monoamine oxidases (MAO-A, -B) mediate and modulate intracellular signal pathways for survival or death of neuronal cells. MAO-A is associated with development of neuronal architecture, synaptic activity, and onset of psychiatric disorders, including depression, and antisocial aggressive impulsive behaviors. MAO-B produces hydrogen peroxide and plays a vital role in neuronal loss of neurodegenerative disorders, such as Parkinson's and Alzheimer's diseases. This review presents a novel role of MAO-A and B, their substrates and inhibitors, and hydrogen peroxide in brain function and neuronal survival and death...
December 26, 2017: Journal of Neural Transmission
Woo Young Sun, Junjeong Choi, Yoon Jin Cha, Ja Seung Koo
We aimed to evaluate the expression of amine oxidase proteins in breast cancer and their clinical implications. We performed immunohistochemical staining of amine oxidase proteins (LOX, lysyl oxidase, AOC3, amine oxidase, MAOA, monoamine oxidase A, MAOB, monoamine oxidase B). Based on their hormone receptors, such as estrogen receptor (ER) and progesterone receptor (PR), human epidermal growth factor receptor 2 (HER-2), and Ki-67 immunohistochemical staining, breast cancer was divided into four molecular subtypes: luminal A, luminal B, HER-2 type, and triple-negative breast cancer (TNBC)...
December 20, 2017: International Journal of Molecular Sciences
Johannes Schulz-Fincke, Mirjam Hau, Jessica Barth, Dina Robaa, Dominica Willmann, Andreas Kürner, Julian Haas, Gabriele Greve, Tinka Haydn, Simone Fulda, Michael Lübbert, Steffen Lüdeke, Tobias Berg, Wolfgang Sippl, Roland Schüle, Manfred Jung
FAD-dependent lysine-specific demethylase 1 (LSD1) is overexpressed or deregulated in many cancers such as AML and prostate cancer and hence is a promising anticancer target with first inhibitors in clinical trials. Clinical candidates are N-substituted derivatives of the dual LSD1-/monoamine oxidase-inhibitor tranylcypromine (2-PCPA) with a basic amine function in the N-substituent. These derivatives are selective over monoamine oxidases. So far, only very limited information on structure-activity studies about this important class of LSD1 inhibitors is published in peer reviewed journals...
December 6, 2017: European Journal of Medicinal Chemistry
Seul Ki Yeon, Ji Won Choi, Jong-Hyun Park, Ye Rim Lee, Hyeon Jeong Kim, Su Jeong Shin, Bo Ko Jang, Siwon Kim, Yong-Sun Bahn, Gyoonhee Han, Yong Sup Lee, Ae Nim Pae, Ki Duk Park
Benzyloxyphenyl moiety is a common structure of highly potent, selective and reversible inhibitors of monoamine oxidase B (MAO-B), safinamide and sembragiline. We synthesized 4-(benzyloxy)phenyl and biphenyl-4-yl derivatives including halogen substituents on the terminal aryl unit. In addition, we modified the carbon linker between amine group and the biaryl linked unit. Among synthesized compounds, 12c exhibited the most potent and selective MAO-B inhibitory effect (hMAO-B IC50: 8.9 nM; >10,000-fold selectivity over MAO-A) as a competitive inhibitor...
November 24, 2017: Bioorganic & Medicinal Chemistry
Jerad Suresh, Seung Cheol Baek, Surya Parakkot Ramakrishnan, Hoon Kim, Bijo Mathew
A series of twelve furanochalcones (F1-F12) was synthesized and investigated for their human monoamine oxidase inhibitory activities. Among the series, compound (2E, 4E)-1-(furan-2-yl)-5-phenylpenta-2, 4-dien-1-one (F1), which was analyzed by single-crystal X-ray diffraction, showed potent and selective MAO-B inhibitory activity with an inhibition constant (Ki) value of 0.0041μM and selectivity index of (SI) 172.4, and exhibited competitive inhibition. Introduction of a cinnamyl group to the furanochalcone significantly increased the inhibitory activity...
November 28, 2017: International Journal of Biological Macromolecules
Christiane Ziegler, Christiane Wolf, Miriam A Schiele, Elma Feric Bojic, Sabina Kucukalic, Emina Sabic Dzananovic, Aferdita Goci Uka, Blerina Hoxha, Valdete Haxhibeqiri, Shpend Haxhibeqiri, Nermina Kravic, Mirnesa Muminovic Umihanic, Ana Cima Franc, Nenad Jaksic, Romana Babic, Marko Pavlovic, Bodo Warrings, Alma Bravo Mehmedbasic, Dusko Rudan, Branka Aukst-Margetic, Abdulah Kucukalic, Damir Marjanovic, Dragan Babic, Nada Bozina, Miro Jakovljevic, Osman Sinanovic, Esmina Avdibegovic, Ferid Agani, Alma Dzubur-Kulenovic, Jürgen Deckert, Katharina Domschke
Background: Posttraumatic Stress Disorder (PTSD) is characterized by an overactive noradrenergic system conferring core PTSD symptoms such as hyperarousal and re-experiencing. Monoamine oxidase A (MAO-A) is one of the key enzymes mediating the turnover of noradrenaline. Here, DNA methylation of the MAOA gene exonI/intronI region was investigated for the first time in regards to its role in PTSD risk and severity. Methods: MAOA methylation was analyzed via direct sequencing of sodium bisulfite treated DNA extracted from blood cells in a total sample of N=652 (m=441) patients with current PTSD, patients with remitted PTSD and healthy probands (comparison group) recruited at five centres in Bosnia-Herzegovina, Croatia, and the Republic of Kosovo...
November 23, 2017: International Journal of Neuropsychopharmacology
L Wen, A Mao, F Jiao, D Zhang, J Xie, K He
Outbreaks of trembling and shaking were reported among pigs at two pig farms in Jiangsu Province, China. Serum and tissue samples tested positive for porcine circovirus-like virus P1 and negative for classical swine fever virus, porcine circovirus type 2, astrovirus and porcine pestivirus using PCR/RT-PCR and immunohistochemical techniques. High P1 viral genome loads were identified in sera, brain and lymph node tissue samples by qPCR. In addition, one of the most notable pathological changes was dissolution of the nucleus in Purkinje cells...
November 27, 2017: Transboundary and Emerging Diseases
Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Yusuf Özkay, Beril İnci, Zafer Asım Kaplancıklı
A new series of thirteen 2-[(4-fluorophenyl)(4-nitrobenzyl)amino]-2-oxoethyl-1-substituted-carbodithioate derivatives (4a-4m) were synthesized and tested for their human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitory potential by an in vitro fluorometric method. Most of the compounds have found to be selective towards MAO-B than MAO-A. Compound 4j that carrying 4-nitrophenyl piperazine moiety, was detected as the most active agent amongst all compounds with the IC50 value of 0.097 ± 0.003 µM for MAO-B while that of selegiline was 0...
November 20, 2017: Bioorganic Chemistry
Yi-Xiang Xu, Huan Wang, Xiao-Kang Li, Sheng-Nan Dong, Wen-Wen Liu, Qi Gong, Tian-Duan-Yi Wang, Yun Tang, Jin Zhu, Jian Li, Hai-Yan Zhang, Fei Mao
A series of novel propargylamine-modified pyrimidinylthiourea derivatives (1-3) were designed and synthesized as multifunctional agents for Alzheimer's disease (AD) therapy, and their potential was evaluated through various biological experiments. Among these derivatives, compound 1b displayed good selective inhibitory activity against AChE (vs BuChE, IC50 = 0.324 μM, SI > 123) and MAO-B (vs MAO-A, IC50 = 1.427 μM, SI > 35). Molecular docking study showed that the pyrimidinylthiourea moiety of 1b could bind to the catalytic active site (CAS) of AChE, and the propargylamine moiety interacted directly with the flavin adenine dinucleotide (FAD) of MAO-B...
January 1, 2018: European Journal of Medicinal Chemistry
Yuki Higuchi, Tomoko Soga, Ishwar S Parhar
Social stress has a high impact on many biological systems in the brain, including serotonergic (5-HT) system-a major drug target in the current treatment for depression. Hyperactivity of hypothalamic-pituitary-adrenal (HPA) axis and monoamine oxidase A (MAO-A) are well-known stress responses, which are involved in the central 5-HT system. Although, many MAO-A inhibitors have been developed and used in the therapeutics of depression, effective management of depression by modulating the activity of MAO-A has not been achieved...
2017: Frontiers in Neuroscience
Narayan D Chaurasiya, Francisco León, Yuanqing Ding, Isabel Gómez-Betancur, Dora Benjumea, Larry A Walker, Stephen J Cutler, Babu L Tekwani
Renealmia alpinia (Zingiberaceae), a medicinal plant of tropical rainforests, is used to treat snakebites and other injuries and also as a febrifuge, analgesic, antiemetic, antiulcer, and anticonvulsant. The dichloromethane extract of R. alpinia leaves showed potent inhibition of human monoamine oxidases- (MAOs-) A and B. Phytochemical studies yielded six known compounds, including pinostrobin 1, 4'-methyl ether sakuranetin 2, sakuranetin 3, pinostrobin chalcone 4, yashabushidiol A 5, and desmethoxyyangonin 6...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
Simone Carradori, Francesco Ortuso, Anél Petzer, Donatella Bagetta, Celeste De Monte, Daniela Secci, Daniela De Vita, Paolo Guglielmi, Gokhan Zengin, Abdurrahman Aktumsek, Stefano Alcaro, Jacobus P Petzer
New 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of neurodegenerative disorders such as Parkinson's disease. Rational molecular design, target recognition and predicted pharmacokinetic properties have been evaluated by means of molecular modelling. Based on these properties, compounds were synthesized and evaluated in vitro as MAO-B and AChE inhibitors, and compared to the activities at their corresponding isozymes, monoamine oxidase A (MAO-A) and butyrylcholinesterase (BuChE), respectively...
October 19, 2017: European Journal of Medicinal Chemistry
Furqan Ahmad Saddique, Sumera Zaib, Saquib Jalil, Sana Aslam, Matloob Ahmad, Sadia Sultan, Humera Naz, Mazhar Iqbal, Jamshed Iqbal
Three series of 4-hydroxy-N(')-[benzylidene/1-phenylethylidene]-2-H/methyl/benzyl-1,2-benzothiazine-3-carbohydrazide 1,1-dioxides (9-11)a-l were synthesized and unraveled to be highly potent dual inhibitors of monoamine oxidases (MAO-A and MAO-B). All the examined compounds demonstrated IC50 values in lower micro-molar range for both MAO-A as well as MAO-B. The most active MAO-A inhibitor was 4-hydroxy-N'-(1-phenylethylidene)-2H-benzo[e][1,2]thiazine-3-carbohydrazide 1,1-dioxide (9i) with an IC50 value of 0...
October 19, 2017: European Journal of Medicinal Chemistry
Koichi Takao, Kazuhiro Toda, Takayuki Saito, Yoshiaki Sugita
A series of cinnamic acid derivatives, amides (1-12) and esters (13-22), were synthesized, and structure-activity relationships for antioxidant activity, and monoamine oxidases (MAO) A and B, acetylcholinesterase, and butyrylcholinesterase (BChE) inhibitory activities were analyzed. Among the synthesized compounds, compounds 1-10, 12-18, and rosmarinic acid (23), which contained catechol, o-methoxyphenol or 5-hydroxyindole moieties, showed potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity...
2017: Chemical & Pharmaceutical Bulletin
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