keyword
https://read.qxmd.com/read/38267058/synthesis-and-biological-evaluation-of-2-azolylmethylene-3-2h-benzofuranone-derivatives-as-potent-monoamine-oxidases-inhibitors
#21
JOURNAL ARTICLE
Koichi Takao, Yuka Kubota, Kota Kurosaki, Hitoshi Kamauchi, Yoshihiro Uesawa, Yoshiaki Sugita
A series of 2-azolylmethylene-3-(2H)-benzofuranone derivatives, 2-indolylmethylene-3-(2H)-benzofuranone and 2-pyrrolylmethylene-3-(2H)-benzofuranone derivatives, were synthesized, and their monoamine oxidase (MAO) A and B inhibitory activities were evaluated. Compounds 1b, 3b, 6b, 7b, and 10b showed strong inhibitory activity against MAO-A, and compound 3b showed the highest potency and selectivity, with an IC50 value of 21 nM and a MAO-A selectivity index of 48. Compounds 3c, 4c, 9a, 9c, 10c, 11a, and 11c showed strong inhibitory activity against MAO-B, and compound 4c showed the highest potency and selectivity, with an IC50 value of 16 nM and a MAO-B selectivity index of >1100...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38230273/monoamine-oxidase-a-mao-a-inhibitors-screened-from-the-autodisplayed-fv-antibody-library
#22
JOURNAL ARTICLE
Jeong Soo Sung, Seunghwan Kim, Jaeyong Jung, Tae-Hun Kim, Soonil Kwon, Hyung Eun Bae, Min-Jung Kang, Joachim Jose, Misu Lee, Jae-Chul Pyun
Serotonin-like mimotopes were screened from the Fv-antibody library to be used as inhibitors against monoamine oxidase A (MAO-A). The Fv-antibody [corresponding to the VH region of immunoglobulin G (IgG)] consists of three complementarity-determining regions and four frame regions. The Fv-antibody library was prepared by site-directed mutagenesis of CDR3, which consists of 11 amino acid residues. Three target clones were screened from the Fv-antibody library, and the binding affinity of the screened clones to the monoclonal anti-serotonin antibody was analyzed using fluorescence-activated cell sorting...
January 12, 2024: ACS Pharmacology & Translational Science
https://read.qxmd.com/read/38218887/isatin-tethered-halogen-containing-acylhydrazone-derivatives-as-monoamine-oxidase-inhibitor-with-neuroprotective-effect
#23
JOURNAL ARTICLE
Sunil Kumar, Jong Min Oh, Prabitha Prabhakaran, Abhimanyu Awasti, Hoon Kim, Bijo Mathew
Sixteen isatin-based hydrazone derivatives (IS1-IS16) were synthesized and assessed for their ability to inhibit monoamine oxidases (MAOs). All the molecules showed improved inhibitory MAO-B activity compared to MAO-A. Compound IS7 most potently inhibited MAO-B with an IC50 value of 0.082 μM, followed by IS13 and IS6 (IC50  = 0.104 and 0.124 μM, respectively). Compound IS15 most potently inhibited MAO-A with an IC50 value of 1.852 μM, followed by IS3 (IC50  = 2...
January 13, 2024: Scientific Reports
https://read.qxmd.com/read/38211551/challenging-the-anticolorectal-cancer-capacity-of-quinoxaline-based-scaffold-via-triazole-ligation-unveiled-new-efficient-dual-vegfr-2-mao-b-inhibitors
#24
JOURNAL ARTICLE
Mohammed Salah Ayoup, Ahmed Ammar, Hamida Abdel-Hamid, Adel Amer, Marwa M Abu-Serie, Samah A Nasr, Doaa A Ghareeb, Mohamed Teleb, Gina N Tageldin
Monoamine oxidases (MAOs) and vascular endothelial growth factor receptor-2 (VEGFR-2) are promoters of colorectal cancer (CRC) and central signaling nodes in epithelial-mesenchymal transition (EMT) induced by activating hypoxia-inducible factors (HIFs). Herein, a novel series of rationally designed triazole-tethered quinoxalines were synthesized and evaluated against HCT-116 CRC cells. The tailored scaffolds combine the pharmacophoric themes of both VEGFR-2 inhibitors and MAO inhibitors. All the synthesized derivatives were screened utilizing the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay for their possible cytotoxic effects on normal human colonocytes, then evaluated for their anticancer activities against HCT-116 cells overexpressing MAOs...
January 6, 2024: Bioorganic Chemistry
https://read.qxmd.com/read/38198753/cardiac-mao-a-inhibition-protects-against-catecholamine-induced-ventricular-arrhythmias-via-enhanced-diastolic-calcium-control
#25
JOURNAL ARTICLE
Qian Shi, Hamza Malik, Rachel M Crawford, Jennifer Streeter, Jinxi Wang, Ran Huo, Jean C Shih, Biyi Chen, Duane Hall, E Dale Abel, Long-Sheng Song, Ethan J Anderson
AIMS: A mechanistic link between depression and risk of arrhythmias could be attributed to altered catecholamine metabolism in the heart. Monoamine oxidase-A (MAO-A), a key enzyme involved in catecholamine metabolism and longstanding antidepressant target, is highly expressed in the myocardium. The present study aimed to elucidate the functional significance and underlying mechanisms of cardiac MAO-A in arrhythmogenesis. METHODS AND RESULTS: Analysis of TriNetX database revealed that depressed patients treated with MAO inhibitors had a lower risk of arrhythmias compared to those treated with selective serotonin reuptake inhibitors...
January 10, 2024: Cardiovascular Research
https://read.qxmd.com/read/38194480/near-infrared-fluorescence-probe-for-monoamine-oxidase-a-with-a-large-stokes-shift-for-intraoperative-navigation
#26
JOURNAL ARTICLE
Linhao Zhang, Rong Zhang, Xinyue Cong, Maomao He, Xin Zhao, Jiangli Fan, Xiaojun Peng, Jingnan Cui, Wen Sun
Monoamine oxidase A (MAO-A) is a dimeric flavoprotein that is found in the mitochondrial membrane. Currently, there is a lack of near-infrared fluorescent probes (NIR-FPs) with good specificity and high sensitivity for detecting MAO-A, making it difficult to accurately recognize and image cells in vitro and in vivo. In this study, the NIR-FP DDM-NH 2 was designed and synthesized in order to detect MAO-A specifically in live biological systems. The probe comprised two functional components: dicyanoisophosphone as an NIR dye precursor and alanine as a recognition moiety...
January 9, 2024: ACS Applied Bio Materials
https://read.qxmd.com/read/38172401/identification-of-genes-regulated-by-trait-sensitivity-to-negative-feedback-and-prolonged-alcohol-consumption-in-rats
#27
JOURNAL ARTICLE
Agata Cieslik-Starkiewicz, Karolina Noworyta, Joanna Solich, Agata Korlatowicz, Agata Faron-Górecka, Rafal Rygula
BACKGROUND: The results of our previous studies demonstrated that low sensitivity to negative feedback (NF) is associated with increased vulnerability to the development of compulsive alcohol-seeking in rats. In the present study, we investigated the molecular underpinnings of this relationship. METHODS: Using TaqMan Gene Expression Array Cards, we analyzed the expression of the genes related to NF sensitivity and alcohol metabolism in three cortical regions (medial prefrontal cortex [mPFC], anterior cingulate cortex [ACC], orbitofrontal cortex [OFC]) and two subcortical regions (nucleus accumbens [Nacc], amygdala [Amy])...
January 3, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38171905/synthesis-of-2-8-dioxabicyclo-3-3-1-nonane-derivatives-and-their-neuroprotective-activities
#28
JOURNAL ARTICLE
Hitoshi Kamauchi, Akifumi Takanashi, Mitsuaki Suzuki, Kouki Izumi, Koichi Takao, Yoshiaki Sugita
Twenty natural-product-like 2,8-dioxabicyclo[3.3.1]nonane derivatives were synthesized and their neuroprotective activities were tested using human monoamine oxidases (MAO) A and B and acetyl and butyryl cholinesterases (ChE). Compound 1s showed inhibitory activity for MAO-A, MAO-B and acetylcholinesterase (AChE) (IC50 values 34.0, 2.3 and 11.0 µM, respectively). The inhibition mode of (-)-1s for MAO-B was investigated. Chiral HPLC of (±)-1s separated the enantiomers and (-)-1s showed MAO-B inhibitory activity...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38144071/development-of-a-new-class-of-monoamine-oxidase-b-inhibitors-by-fine-tuning-the-halogens-on-the-acylhydrazones
#29
JOURNAL ARTICLE
Jayalakshmi Jayan, Jiseong Lee, Sunil Kumar, Amritha Manoharan, Anishma Payyappilliparambil Narayanan, Reenoo Jauhari, Mohamed A Abdelgawad, Mohammed M Ghoneim, Hasnaa Ali Ebrahim, Subin Mary Zachariah, Hoon Kim, Bijo Mathew
A total of 14 acyl hydrazine derivatives ( ACH1-ACH14 ) were developed and examined for their ability to block monoamine oxidase (MAO). Thirteen analogues showed stronger inhibition potency against MAO-B than MAO-A. With a half-maximum inhibitory concentration of 0.14 μM, ACH10 demonstrated the strongest inhibitory activity against MAO-B, followed by ACH14 , ACH13 , ACH8 , and ACH3 (IC50 = 0.15, 0.18, 0.20, and 0.22 μM, respectively). Structure-activity relationships suggested that the inhibition effect on MAO-B resulted from the combination of halogen substituents of the A- and/or B-rings...
December 19, 2023: ACS Omega
https://read.qxmd.com/read/38136164/a-multitarget-approach-against-neuroinflammation-alkyl-substituted-coumarins-as-inhibitors-of-enzymes-involved-in-neurodegeneration
#30
JOURNAL ARTICLE
Emanuela Berrino, Simone Carradori, Fabrizio Carta, Francesco Melfi, Marialucia Gallorini, Giulio Poli, Tiziano Tuccinardi, José G Fernández-Bolaños, Óscar López, Jacobus P Petzer, Anél Petzer, Paolo Guglielmi, Daniela Secci, Claudiu T Supuran
Neurodegenerative disorders (NDs) include a large range of diseases characterized by neural dysfunction with a multifactorial etiology. The most common NDs are Alzheimer's disease and Parkinson's disease, in which cholinergic and dopaminergic systems are impaired, respectively. Despite different brain regions being affected, oxidative stress and inflammation were found to be common triggers in the pathogenesis and progression of both diseases. By taking advantage of a multi-target approach, in this work we explored alkyl substituted coumarins as neuroprotective agents, capable to reduce oxidative stress and inflammation by inhibiting enzymes involved in neurodegeneration, among which are Carbonic Anhydrases (CAs), Monoamine Oxidases (MAOs), and Cholinesterases (ChEs)...
November 25, 2023: Antioxidants (Basel, Switzerland)
https://read.qxmd.com/read/38132450/-ginkgo-biloba-antioxidant-activity-and-in-silico-central-nervous-system-potential
#31
JOURNAL ARTICLE
Eduardo Suárez-González, Jesús Sandoval-Ramírez, Jorge Flores-Hernández, Alan Carrasco-Carballo
Ginkgo biloba (GB) extracts have been used in clinical studies as an alternative therapy for Alzheimer's disease (AD), but the exact bioaction mechanism has not yet been elucidated. In this work, an in silico study on GB metabolites was carried out using SwissTargetPrediction to determine the proteins associated with AD. The resulting proteins, AChE, MAO-A, MAO-B, β-secretase and γ-secretase, were studied by molecular docking, resulting in the finding that kaempferol, quercetin, and luteolin have multitarget potential against AD...
December 1, 2023: Current Issues in Molecular Biology
https://read.qxmd.com/read/38116435/repurposing-azoles-to-resolve-serotogenic-toxicity-associated-with-linezolid-to-combat-multidrug-resistant-tuberculosis
#32
JOURNAL ARTICLE
Rukaiyya T Girase, Iqrar Ahmad, Jong Min Oh, Hoon Kim, Bijo Mathew, Siva K Vagolu, Tone Tønjum, Nisheeth C Desai, Dharmarajan Sriram, Jyothi Kumari, Harun M Patel
Serotogenic toxicity is a major hurdle associated with Linezolid in the treatment of drug-resistant tuberculosis (TB) due to the inhibition of monoamine oxidase (MAO) enzymes. Azole compounds demonstrate structural similarities to the recognized anti-TB drug Linezolid, making them intriguing candidates for repurposing. Therefore, we have repurposed azoles (Posaconazole, Itraconazole, Miconazole, and Clotrimazole) for the treatment of drug-resistant TB with the anticipation of their selectivity in sparing the MAO enzyme...
December 14, 2023: ACS Medicinal Chemistry Letters
https://read.qxmd.com/read/38095566/queuine-as-a-potential-multi-target-drug-for-alzheimer-s-disease-insights-from-protein-dynamics
#33
JOURNAL ARTICLE
Münteha Girgin, Nigar Kantarci-Carsibasi
Alzheimer's disease (AD) is a neurodegenerative disorder with a complex pathogenesis. One promising approach to treating AD is simultaneously targeting multiple aspects of the disease using a multi-target drug (MTD). In this study, multi-target drug (MTD) potential of the nutraceutical molecule Queuine was explored using molecular docking and molecular dynamics (MD) simulations with five different protein targets engaged in AD: AChE, beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), N-methyl-D-aspartate receptor (NMDAR), monoamine oxidase A (MAO-A), and Synapsin III...
December 14, 2023: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38084656/supplementing-clinical-lactation-studies-with-pbpk-modeling-to-inform-drug-therapy-in-lactating-mothers-prediction-of-primaquine-exposure-as-a-case-example
#34
JOURNAL ARTICLE
Xian Pan, Khaled Abduljalil, Lisa M Almond, Amita Pansari, Karen Rowland Yeo
Evaluating the safety of primaquine (PQ) during breastfeeding requires an understanding of its pharmacokinetics (PKs) in breast milk and its exposure in the breastfed infant. Physiologically-based PK (PBPK) modeling is primed to assess the complex interplay of factors affecting the exposure of PQ in both the mother and the nursing infant. A published PBPK model for PQ describing the metabolism by monoamine oxidase A (MAO-A; 90% contribution) and cytochrome P450 2D6 (CYP2D6; 10%) in adults was applied to predict the exposure of PQ in mothers and their breastfeeding infants...
December 12, 2023: CPT: Pharmacometrics & Systems Pharmacology
https://read.qxmd.com/read/38066695/the-intracellular-monoamine-oxidase-a-inhibitory-activity-and-the-protective-effect-of-small-hairtail-related-peptides-in-nerve-cells-sh-sy5y
#35
JOURNAL ARTICLE
Aiyuan Zhang, Xiaoxue Yang, Keying Su, Jintao Xie, Xuewu Zhang
This study was to investigate the inhibitory activity of small hairtail-related peptides (VFEVFW, LPNSLYQQ, LPNSLYQK and FADAME) on intracellular monoamine oxidase-A (MAO-A) and their protective effects in a cell model. Specifically, the inhibition activity in SH-SY5Y cells indicated that VFEVFW and LPNSLYQK reduced about 50% of MAO-A activity in cells, at 0.5 mM. The survival experiment demonstrated that the toxic effect of dexamethasone (DEX) on cells can be significantly alleviated in the presence of peptides, and these peptides can restore (>20%) the mitochondrial membrane potential of SH-SY5Y cells reduced by DEX...
December 8, 2023: Bioscience, Biotechnology, and Biochemistry
https://read.qxmd.com/read/38064100/cardioprotective-effect-of-2-ethyl-3-hydroxy-6-methylpyridinium-2-nitroxysuccinate-against-adrenaline-hydrocortisone-induced-myocardial-ischemia-in-mice-modulation-of-free-radical-processes-in-biomembranes-and-monoamine-oxidase-a-activity
#36
JOURNAL ARTICLE
Irina I Faingold, Anastasia V Smolina, Yulia V Soldatova, Darya A Poletaeva, Anastasia A Balakina, Tatyana E Sashenkova, Uguljan Yu Allayarova, Tatyana R Prikhodchenko, Svetlana V Blokhina, Lyudmila A Makartseva, David A Areshidze, Vladislav N Varfolomeev, Denis V Mishchenko, Raisa A Kotelnikova
Oxidative stress (OS) plays a key role in the development of cardiovascular diseases (CVD) in three major ways: reactive oxygen species (ROS)-induced reduction of nitric oxide (NO) bioavailability, ROS-induced inflammation and ROS-induced mitochondrial dysfunction. Oxidation of lipid molecules under the action of ROS leads to damage to membrane structures, changes the functioning of membrane-bound enzymes, and impairs membrane permeability and stability. An increase in OS results in the occurrence of endothelial dysfunction and drug tolerance, side effects, requiring discontinuation of drugs...
December 8, 2023: Cell Biochemistry and Biophysics
https://read.qxmd.com/read/38061181/synthesis-in-vitro-and-in-silico-studies-of-new-derivatives-of-diphenylpiperazine-scaffold-a-key-substructure-for-mao-inhibition
#37
JOURNAL ARTICLE
Lamiaa O El-Halaby, Walaa M El-Husseiny, Shahenda M El-Messery, Fatma E Goda
Fifteen new diphenylpiperazine hybrids were designed, synthesized and in vitro biologically evaluated against hMAOs enzymes via fluorometric method. All of our new compounds displayed strong inhibitory activities against both two isoforms of hMAOs with IC50 range of 0.091-16.32 µM. According to selectivity index values, all hybrids showed higher selectivity against hMAO-A over hMAO-B. Compound 8 exhibited the best hMAO-A inhibition activity (IC50 value = 91 nM, SI = 19.55)...
December 3, 2023: Bioorganic Chemistry
https://read.qxmd.com/read/38053684/isatin-based-benzyloxybenzene-derivatives-as-monoamine-oxidase-inhibitors-with-neuroprotective-effect-targeting-neurogenerative-disease-treatment
#38
JOURNAL ARTICLE
Feba Benny, Jong Min Oh, Sunil Kumar, Mohamed A Abdelgawad, Mohammed M Ghoneim, Mohamed Sadek Abdel-Bakky, Neelima Kukerti, Jobin Jose, Hoon Kim, Bijo Mathew
Eighteen isatin-based benzyloxybenzaldehyde derivatives from three subseries, ISB, ISFB, and ISBB, were synthesized and their ability to inhibit monoamine oxidase (MAO) was evaluated. The inhibitory activity of all synthesized compounds was found to be more profound against MAO-B than MAO-A. Compound ISB1 most potently inhibited MAO-B with an IC50 of 0.124 ± 0.007 μM, ensued by ISFB1 (IC50 = 0.135 ± 0.002 μM). Compound ISFB1 most potently inhibited MAO-A with an IC50 of 0.678 ± 0...
November 30, 2023: RSC Advances
https://read.qxmd.com/read/38049514/protective-effects-of-niacin-following-high-fat-rich-diet-an-in-vivo-and-in-silico-study
#39
JOURNAL ARTICLE
Noreen Samad, Natasha Manzoor, Ammara Batool, Aqsa Noor, Saima Khaliq, Sana Aurangzeb, Sheraz Ahmed Bhatti, Imran Imran
Niacin had long been understood as an antioxidant. There were reports that high fat diet (HFD) may cause psychological and physical impairments. The present study was aimed to experience the effect of Niacin on % growth rate, cumulative food intake, motor activity and anxiety profile, redox status, 5-HT metabolism and brain histopathology in rats. Rats were administered with Niacin at a dose of 50 mg/ml/kg body weight for 4 weeks following normal diet (ND) and HFD. Behavioral tests were performed after 4 weeks...
December 1, 2023: Scientific Reports
https://read.qxmd.com/read/38004136/antidepressant-like-effect-of-oroxylum-indicum-seed-extract-in-mice-model-of-unpredictable-chronic-mild-stress
#40
JOURNAL ARTICLE
Chorpeth Chalermwongkul, Charinya Khamphukdee, Juthamart Maneenet, Supawadee Daodee, Orawan Monthakantirat, Chantana Boonyarat, Yutthana Chotritthirong, Suresh Awale, Anake Kijjoa, Yaowared Chulikhit
Major depressive disorder (MDD) is one life-threatening disorder that is prevalent worldwide. The evident etiology of this disease is still poorly understood. Currently, herbal medicine is gaining more interest as an alternative antidepressant. Oroxylum indicum , which is used in traditional medicine and contains a potential antidepressive compound, baicalein, could have an antidepressive property. An in vitro monoamine oxidase-A (MAO-A) inhibitory assay was used to preliminarily screening for the antidepressant effect of O...
November 10, 2023: Nutrients
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