Results 51 to 60 of about 35,554 (229)

Synthesis and Antibacterial Evaluation of Novel Heterocyclic Compounds Containing a Sulfonamido Moiety

Molecules, 2013
Aiming for the synthesis of new heterocyclic compounds containing a sulfonamido moiety suitable for use as antibacterial agents, the precursor ethyl {[4-N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenylazo}cyanoacetate was reacted with a variety of active ...
Eman A. El-Bordany, Mohamed M. Youssef, Mohammad Emad Azab   +2 more
doaj   +1 more source

Preparation and Diagnosis of Pyrimidines Derivatives by Conventional And Microwave Ways. [PDF]

مجلة جامعة الانبار للعلوم الصرفة, 2017
This work includes synthesis and characterization of new derivatives of pyrimidine (R. or Ar. -1, 2, 3, 4-tetrahydropyrimidin-5-yl) ethan-1-one), via the reaction of acetyl acetone with different aldehydes and guanidine hydrochloride.
Waleed F. AL-Hiti, Samea J. Khammase, Bushra T. Mahdi   +2 more
doaj   +1 more source

Discovery of a Novel and Potent Kir4.1 Inhibitor as a Safe and Rapid‐Onset Antidepressant Agent in Mice

Advanced Science, EarlyView.
The preferred derivative JX3212 demonstrates strong inhibitory activity against Kir4.1 with favorable druggability and shows significant antidepressant efficacy in vivo. Abstract Major depressive disorder is a serious psychiatric disorder for which novel and fast‐acting antidepressants are required.
Sisi Wang, Xiaoyu Zhou, Mengdan Li, Chao Zhang, Haiyan Xu, Jingyi He, Li Zhan, Yueling Gu, Hao Gu, Tianyu Tu, Hanfang Liu, Taotao Lu, Yueming Zheng, Jian Li, Zhaobing Gao, Yixiang Xu   +15 more
wiley   +1 more source

Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy

Molecules
The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development.
Silvia Cesarini, Ilaria Vicenti, Federica Poggialini, Silvia Filippi, Eleonora Mancin, Lia Fiaschi, Elisa De Marchi, Federica Giammarino, Chiara Vagaggini, Bruno Mattia Bizzarri, Raffaele Saladino, Elena Dreassi, Maurizio Zazzi, Lorenzo Botta   +13 more
doaj   +1 more source

NAD⁺ Reduction in Glutamatergic Neurons Induces Lipid Catabolism and Neuroinflammation in the Brain via SARM1

Advanced Science, EarlyView.
NAD⁺ homeostasis maintains neuronal integrity through opposing actions of NMNAT2 and SARM1. Loss of NMNAT2 in glutamatergic neurons reprograms cortical metabolism from glucose to lipid catabolism, depletes lipid stores, and triggers inflammation and neurodegeneration.
Zhen‐Xian Niou, Sen Yang, Andrea Enriquez, Nino A. Espinas, Anoosha Sri, Caliel D. Hines, Jason M. Tennessen, Chia‐Shan Wu, Jui‐Yen Huang, Hui‐Chen Lu   +9 more
wiley   +1 more source

Synthesis and Antioxidant Activities of Novel Pyrimidine Acrylamides as Inhibitors of Lipoxygenase: Molecular Modeling and In Silico Physicochemical Studies

Molecules
The pyrimidine ring is present in various biomolecules such as DNA and RNA bases, aminoacids, vitamins, etc. Additionally, many clinically used drugs including methotrexate and risperidone contain the pyrimidine heterocyclic scaffold as well.
Michail Saragatsis, Eleni Pontiki
doaj   +1 more source

ACSL5 Regulates Glucose Metabolism and Chemotherapy Sensitivity in Colorectal Cancer Cells under Glutamine Deficiency

Advanced Science, EarlyView.
Glutamine deprivation triggers ACSL5 upregulation in tumor cells, sustaining their viability via dual metabolic rewiring programs. ACSL5 enhances glycolysis by relieving p53's inhibition of PGAM1 while also sustaining mitochondrial respiration and TCA cycle flux through promoting IDH2 dimerization.
Shuai Tian, Qiaoxia Zhang, Xuedan Sun, Rick Francis Thorne, Zeyuan Shi, Qiang Ji, Zhangran Sun, Yuanxiang Lu, Qun Zhao, Xianjun Yu, Wanglai Hu, Mian Wu   +11 more
wiley   +1 more source

Effectiveness of Multivitamins vs Folic Acid on Prevention of Neural Tube Defects in Mouse Genetic Models and Human Organoids

Advanced Science, EarlyView.
Folic acid (FA) and multivitamins/minerals (MVM) are recommended for the prevention of neural tube defects (NTDs). Using a novel human neural tube‐like organoid system and mouse models, the study compares the effectiveness of two supplements on NTDs and cellular behaviors.
Huili Li, Jing Zhang, Lori Bulwith, Lee Niswander   +3 more
wiley   +1 more source

PHGDH Defines a Metabolic Subtype in Lung Adenocarcinomas with Poor Prognosis

Cell Reports, 2017
Molecular signatures are emerging determinants of choice of therapy for lung adenocarcinomas. An evolving therapeutic approach includes targeting metabolic dependencies in cancers.
Boxi Zhang, Adi Zheng, Per Hydbring, Gorbatchev Ambroise, Amanda Tomie Ouchida, Michel Goiny, Helin Vakifahmetoglu-Norberg, Erik Norberg   +7 more
doaj   +1 more source

GOT1 Inhibition Induces Extracellular Matrix Remodeling in Pancreatic Cancer

Advanced Science, EarlyView.
Using tumor tissue engineering, we recreated pancreatic cancer and found that inhibiting glutamic‐oxaloacetic transaminase 1 (GOT1) induces extracellular matrix remodeling and secretome rewiring, as well as promotes cell death. ABSTRACT Pancreatic cancer cells rely on glutamine to sustain their survival in the stiff and poorly vascularized tumor ...
Rodrigo Curvello, Sandra Hauser, Michael Seifert, Christopher K. Barlow, Joel R. Steele, Emma Salisbury, Daniel Croagh, Kathryn S. Stok, Anna V. Taubenberger, Ralf B. Schittenhelm, Daniela Loessner   +10 more
wiley   +1 more source