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567 Aktuelle Fachpublikationen in Archiv der Pharmazie

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Design, synthesis, and molecular docking of novel indole scaffold‐based VEGFR‐2 inhibitors as targeted anticancer agents

11.01.2018 | Hanaa M. Roaiah, Iman A. Y. Ghannam, Islam H. Ali, Ahmed M. El Kerdawy, Mamdouh M. Ali, Safinaz E‐S. Abbas, Sally S. ..., Archiv der Pharmazie, 2018

Abstract A series of new indole derivatives 1–18 was synthesized and tested for their cytotoxic activity on a panel of 60 tumor cell lines. Additionally, molecular docking was carried out to study their binding pattern and binding affinity in the VEGFR‐2 active site using sorafenib as a ...

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Oxaprozin prodrug as safer nonsteroidal anti‐inflammatory drug: Synthesis and pharmacological evaluation

28.12.2017 | Jaya P. Peesa, Lakshmana R. Atmakuri, Prasanna R. Yalavarthi, Basaveswara R. Mandava Venkata, Arun Rasheed, Vengalra ..., Archiv der Pharmazie, 2017

Abstract Oxaprozin is a popular non‐steroidal anti‐inflammatory drug (NSAID) and its chronic oral use is clinically restricted due to its gastrointestinal (GI) complications. In order to circumvent the GI complications, oxaprozin was amended as a prodrug in a one‐pot reaction using ...

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Synthesis and elastase inhibition activities of novel aryl, substituted aryl, and heteroaryl oxime ester derivatives

18.12.2017 | Belma Hasdemir, Ozlem Sacan, Hasniye Yasa, Hatice B. Kucuk, Ayse S. Yusufoglu, Refiye Yanardag, Archiv der Pharmazie, 2017

Abstract Fifteen novel aryl, substituted aryl and heteroaryl γ‐hydroxy‐ (2a–e), γ‐methoxyimino‐ (3a–e), and γ‐benzyloxyimino‐ (4a–e) butyric acid methyl esters were investigated for their enzyme inhibition, and the synthesis of 10 compounds (3a–e, 4a–e) is given in this study. The other five ...

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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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Synthesis and Functional Investigations of Computer Designed Novel Cladribine‐Like Compounds for the Treatment of Multiple Sclerosis

28.09.2017 | Serkan Yavuz, Aysu Çetin, Atilla Akdemir, Doğukan Doyduk, Ali Dişli, Gurbet Çelik Turgut, Alaattin Şen, Yılmaz Yıldırır, Archiv der Pharmazie, 2017

Cladribine (2‐CdA) is used as an anti‐cancer drug but is currently studied as a potential treatment for use in relapsing‐remitting multiple sclerosis (MS). In this study, we computer designed, synthesized, and characterized two novel derivatives of 2‐CdA, K1–5d and K2–4c, and investigated their ...

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Evaluation of β‐Aminocarboxylic Acid Derivatives in Hippocampal Excitatory Synaptic Transmission

05.09.2017 | Daniela R. Oliveira, Cibele V. Luchez, Zuner A. Bortolotto, João P. S. Fernandes, Archiv der Pharmazie, 2017

β‐Aminocarboxylic acid derivatives (LINS04 series) were screened with the aim to explore their potential functional role in excitatory synaptic transmission in the central nervous system. We used field recordings in rat hippocampal slices to investigate the effects of the LINS04 series on the ...

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Design, Synthesis, and Biological Evaluation of New Peptide Analogues as Selective COX‐2 Inhibitors

05.09.2017 | Mohammad A. Ahmaditaba, Soraya Shahosseini, Bahram Daraei, Afshin Zarghi, Mohammad H. Houshdar Tehrani, Archiv der Pharmazie, 2017

A new class of peptide derivatives possessing SO2Me and N3 pharmacophores at the para position of a phenyl ring bound to different aromatic amino acids were synthesized based on solid‐phase synthesis methodology, and evaluated as selective cyclooxygenase‐2 (COX‐2) inhibitors. One of the ...

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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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The Effect of Carboxamide/Sulfonamide Replacement in Arylpiperazinylalkyl Derivatives on Activity to Serotonin and Dopamine Receptors

28.08.2017 | Piotr Kowalski, Paweł Śliwa, Grzegorz Satała, Rafał Kurczab, Ilona Bartos, Karol Zuchowicz, Archiv der Pharmazie, 2017

A series of carboxamide and sulfonamide alkyl (p‐xylyl and benzyl) 1‐(2‐methoxyphenyl)piperazine (o‐OMe‐PhP) and 1‐(2,3‐dichlorophenyl)piperazine (2,3‐DCPP) analogs were prepared and tested for their affinity to bind to serotonin 5‐HT1A/5‐HT6/5‐HT7 and dopamine D2 receptors. This chemical ...

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Delivery of Therapeutic Proteins Using Electrospun Fibers—Recent Developments and Current Challenges

28.08.2017 | Salem Seif, Viktoria Planz, Maike Windbergs, Archiv der Pharmazie, 2017

Proteins play a vital role within the human body by regulating various functions and even serving as structural constituent of many body parts. In this context, protein‐based therapeutics have attracted a lot of attention in the last few decades as potential treatment of different diseases. Due ...

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