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567 Aktuelle Fachpublikationen in Archiv der Pharmazie

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Fragment‐Based Drug Discovery in the Bromodomain and Extra‐Terminal Domain Family

17.07.2017 | Mostafa Radwan, Rabah Serya, Archiv der Pharmazie, 2017

Bromodomain and extra‐terminal domain (BET) inhibition has emerged recently as a potential therapeutic target for the treatment of many human disorders such as atherosclerosis, inflammatory disorders, chronic obstructive pulmonary disease (COPD), some viral infections, and cancer. Since the ...

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Acetamide Derivatives of Chromen‐2‐ones as Potent Cholinesterase Inhibitors

12.07.2017 | Suchita Prasad, Bipul Kumar, Shiv Kumar, Karam Chand, Shashank S. Kamble, Hemant K. Gautam, Sunil K. Sharma, Archiv der Pharmazie, 2017

Alzheimer's disease (AD), a neurodegenerative disorder, is a serious medical issue worldwide with drastic social consequences. Inhibition of cholinesterase is one of the rational and effective approaches to retard the symptoms of AD and, hence, consistent efforts are being made to develop ...

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Centennial Anniversary of Mannich's Report on the Formation of β‐Amino‐Ketones in the Archiv der Pharmazie

03.07.2017 | Andreas Link, Archiv der Pharmazie, 2017

In order to commemorate Carl Mannich's achievement with many implications in the fields of drug design and synthesis, stability of pharmaceutical preparations, and natural product chemistry, we invited researchers to submit their work related to Mannich's pioneering article at the occasion of ...

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Isophthalic Acid‐Based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni

22.06.2017 | Katharina Stenzel, Alokta Chakrabarti, Jelena Melesina, Finn K. Hansen, Julien Lancelot, Simon Herkenhöhner, Beate L ..., Archiv der Pharmazie, 2017

Schistosoma mansoni histone deacetylase 8 (SmHDAC8) has been recently identified as a new potential target for the treatment of schistosomiasis. A series of newly designed and synthesized alkoxyamide‐based and hydrazide‐based HDAC inhibitors were tested for inhibitory activity against SmHDAC8 ...

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Design, Synthesis, and Biological Evaluation of Isothiosemicarbazones with Antimycobacterial Activity

21.06.2017 | Eva Novotná, Karel Waisser, Jiří Kuneš, Karel Palát, Lenka Skálová, Barbora Szotáková, Vladimír Buchta, Jiřina Stola ..., Archiv der Pharmazie, 2017

A series of benzaldehyde and salicylaldehyde‐S‐benzylisothiosemicarbazones was synthesized and tested against 12 different strains of mycobacteria, Gram‐positive and Gram‐negative bacteria, and the significant selectivity toward mycobacteria was proved. Twenty‐eight derivatives were evaluated ...

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Design, Synthesis, and Evaluation of Novel Tyrosine‐Based DNA Gyrase B Inhibitors

16.06.2017 | Andrej E. Cotman, Marko Trampuž, Matjaž Brvar, Danijel Kikelj, Janez Ilaš, Lucija Peterlin‐Mašič, Sofia Montalvão, P ..., Archiv der Pharmazie, 2017

The discovery and synthesis of new tyrosine‐based inhibitors of DNA gyrase B (GyrB), which target its ATPase subunit, is reported. Twenty‐four compounds were synthesized and evaluated for activity against DNA gyrase and DNA topoisomerase IV. The antibacterial properties of selected GyrB ...

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Synthesis and Antiproliferative Activity of Thioxoflavones Mannich Base Derivatives

12.06.2017 | Wei Li, Xueli Li, Manhui Liu, Qiuan Wang, Archiv der Pharmazie, 2017

Two series of 12 novel thioxoflavones Mannich base derivatives 5a–f and 6a–f were synthesized via Mannich reaction of 4′,7‐dimethoxy‐5‐hydroxyflavothione (3) or 3′,4′,7‐trimethoxy‐5‐hydroxyflavothione (4) with appropriate aliphatic amines or alicyclic amines and formaldehyde. Thioxoflavones 3 ...

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Synthesis and Biological Evaluation of New Diarylpyrazole and Triarylimidazoline Derivatives as Selective COX‐2 Inhibitors

12.06.2017 | Khaled R.A. Abdellatif, Mohamed A. Abdelgawad, Madlen B. Labib, Taha H. Zidan, Archiv der Pharmazie, 2017

New series of diarylpyrazoles 8a–f and triarylimidazoline‐5‐ones 11a–g were synthesized and evaluated for their in vitro cyclooxygenase‐1 (COX‐1) and COX‐2 inhibitory activity and in vivo anti‐inflammatory activity. The synthesized compounds showed good selectivity for COX‐2; compounds 8a, 8d, ...

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Design and Synthesis of 1,2,4‐Triazolo[3,2‐b]‐1,3,5‐thiadiazine Derivatives as a Novel Template for Analgesic/Anti‐Inflammatory Activity

08.06.2017 | Seyma Sert‐Ozgur, Banu C. Tel, Elif I. Somuncuoglu, Inci Kazkayasi, Mevlut Ertan, Birsen Tozkoparan, Archiv der Pharmazie, 2017

Previously, we demonstrated that certain heterocyclic compounds derived from 3‐substituted‐1,2,4‐triazole‐5‐thiones had promising analgesic/anti‐inflammatory activities together with low ulcerogenic properties. Therefore, we sought to design and synthesize new derivatives of ...

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Mannich Curcuminoids as Potent Anticancer Agents

26.05.2017 | Márió Gyuris, László Hackler, Lajos I. Nagy, Róbert Alföldi, Eszter Rédei, Annamária Marton, Tibor Vellai, Nóra Fara ..., Archiv der Pharmazie, 2017

A series of novel curcuminoids were synthesised for the first time via a Mannich‐3CR/organocatalysed Claisen–Schmidt condensation sequence. Structure–activity relationship (SAR) studies were performed by applying viability assays and holographic microscopic imaging to these curcumin analogues ...

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