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64 Aktuelle Fachpublikationen zum Thema Screening

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Design, Synthesis, and Screening of Triazolopyrimidine–Pyrazole Hybrids as Potent Apoptotic Inducers

16.10.2017 | Raj Kamal, Vipan Kumar, Ravinder Kumar, Jitender K. Bhardwaj, Priyanka Saraf, Priya Kumari, Vikas Bhardwaj, Archiv der Pharmazie, 2017

An efficient synthesis of novel 3‐(3‐aryl‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐5,7‐dimethyl‐[1,2,4]triazolo[4,3‐a]‐pyrimidines was accomplished by the oxidation of pyrimidinylhydrazones by using organoiodine(III) reagent. All new triazolopyrimidine derivatives bearing the pyrazole scaffold were screened ...

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Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

01.09.2017 | Sangh Partap, Mohammad Shahar Yar, Md. Zaheen Hassan, Md. Jawaid Akhtar, Anees A. Siddiqui, Archiv der Pharmazie, 2017

A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard ...

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Marine Drugs, Vol. 15, Pages 281: Biological and Chemical Diversity of Bacteria Associated with a Marine Flatworm

01.09.2017 | Lin, Hui-Na ; Wang, Kai-Ling ; Wu, Ze-Hong ; Tian, Ren-Mao ; Liu, Guo-Zhu ; Xu, Ying, Marine Drugs, 2017

Marine Drugs, Vol. 15, Pages 281: Biological and Chemical Diversity of Bacteria Associated with a Marine Flatworm Marine Drugs doi: 10.3390/md15090281 Authors: Hui-Na Lin Kai-Ling Wang Ze-Hong Wu Ren-Mao Tian Guo-Zhu Liu Ying Xu The aim of this research is to explore the ...

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Diarylpyrazole Ligated Dihydropyrimidine Hybrids as Potent Non‐Classical Antifolates and Their Efficacy Against Plasmodium falciparum

10.08.2017 | Jaimin D. Bhatt, Chaitanya J. Chudasama, Kanuprasad D. Patel, Archiv der Pharmazie, 2017

A series of diarylpyrazole clubbed dihydropyrimidine derivatives (J1–J30) was synthesized under microwave‐assisted heating conditions by employing Biginelli reaction methodology and utilizing triethylammonium acetate both as a catalyst and as reaction medium, leading towards a greener reaction ...

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Synthesis of Some Novel 2,6‐Disubstituted Pyridazin‐3(2H)‐one Derivatives as Analgesic, Anti‐Inflammatory, and Non‐Ulcerogenic Agents

09.08.2017 | Tamer H. Ibrahim, Yasser M. Loksha, Hosam A. Elshihawy, Dina M. Khodeer, Mohamed M. Said, Archiv der Pharmazie, 2017

Some novel 2,6‐disubstituted pyridazine‐3(2H)‐one derivatives were synthesized and evaluated for in vitro cyclooxygenase‐2 (COX‐2) inhibitory efficacy. Compounds 2‐{[3‐(2‐methylphenoxy)‐6‐oxopyridazin‐1(6H)‐yl]methyl}‐1H‐isoindole‐1,3(2H)‐dione (5a), 2‐propyl‐6‐(o‐tolyloxy)pyridazin‐3(2H)‐one ...

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Some Novel Mannich Bases of 5‐(3,4‐Dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one and Their Anti‐Inflammatory Activity

04.08.2017 | Meric Koksal, Irem Ozkan‐Dagliyan, Tugce Ozyazici, Beril Kadioglu, Hande Sipahi, Ayhan Bozkurt, Suleyman S. Bilge, Archiv der Pharmazie, 2017

Non‐steroidal anti‐inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is ...

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Three‐Component Aminoalkylations Yielding Dihydronaphthoxazine‐Based Sirtuin Inhibitors: Scaffold Modification and Exploration of Space for Polar Side‐Chains

26.05.2017 | Steffen Vojacek, Katja Beese, Zayan Alhalabi, Sören Swyter, Anja Bodtke, Carola Schulzke, Manfred Jung, Wolfgang Sip ..., Archiv der Pharmazie, 2017

Nonpolar derivatives of heterocyclic aromatic screening hits like the non‐selective sirtuin inhibitor splitomicin tend to be poorly soluble in biological fluids. Unlike sp3‐rich natural products, flat aromatic compounds are prone to stacking and often difficult to optimize into leads with ...

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Synthesis and Anticonvulsant Properties of New 3,3‐Diphenyl‐2,5‐dioxo‐pyrrolidin‐1‐yl‐acetamides and 3,3‐Diphenyl‐propionamides

20.03.2017 | Jolanta Obniska, Anna Rapacz, Sabina Rybka, Małgorzata Góra, Paweł Żmudzki, Krzysztof Kamiński, Archiv der Pharmazie, 2017

The focused library of new amides derived from 3,3‐diphenyl‐2,5‐dioxo‐pyrrolidin‐1‐yl‐acetic acid (2a–t) and 3,3‐diphenyl‐propionic acid (3a–t) as potential anticonvulsant agents was synthesized. The final products were obtained in the amidation reaction of the given carboxylic acid (2, 3) with ...

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Chemical screening identifies ROCK as a target for recovering mitochondrial function in Hutchinson‐Gilford progeria syndrome

20.03.2017 | Hyun Tae Kang, Joon Tae Park, Kobong Choi, Hyo Jei Claudia Choi, Chul Won Jung, Gyu Ree Kim, Young‐Sam Lee, Sang Chu ..., Aging Cell, 2017

Summary Hutchinson‐Gilford progeria syndrome (HGPS) constitutes a genetic disease wherein an aging phenotype manifests in childhood. Recent studies indicate that reactive oxygen species (ROS) play important roles in HGPS phenotype progression. Thus, pharmacological reduction in ROS levels has ...

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Design, Synthesis, and Cytotoxic Evaluation of Certain 7‐Chloro‐4‐(piperazin‐1‐yl)quinoline Derivatives as VEGFR‐II Inhibitors

17.03.2017 | Mohamed Nabil Aboul‐Enein, Aida M. Abd El‐Sattar El‐Azzouny, Fatma Abdel‐Fattah Ragab, Mohamed Farouk Hamissa, Archiv der Pharmazie, 2017

Signaling pathway inhibition of VEGFR‐II is visualized as valuable tool in cancer management. In the current study, the synthesis of novel 1‐4‐(7‐chloroquinolin‐4‐yl)piperazin‐1‐yl)‐2‐(N‐substituted‐amino)‐ethanone derivatives (4a–t) was achieved through the amination of ...

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