An Efficient Synthesis of bi ‐Aryl Pyrimidine Heterocycles: Potential New Drug Candidates to Treat Alzheimer's Disease
A series of 13 novel pyrimidine‐based sulfonamides 6a–m were synthesized in short periods of time under microwave conditions in good to excellent yield (54–86%). The chemical structures of these heterocycles consist of a central pyrimidine ring having a phenyl group and pyrimidine groups with sulfonamide motifs. The enzyme inhibitory potential of these compounds was investigated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) because these enzymes play a crucial role in the treatment of Alzheimer's disease. As compared to the reference compound eserine (IC50 = 0.04 ± 0.0001 μM for ACh...
Source: Archiv der Pharmazie - January 31, 2017 Category: Drugs & Pharmacology Authors: Tanzeel Ur Rehman, Islam Ullah Khan, Muhammad Ashraf, Hamadeh Tarazi, Sadaf Riaz, Muhammad Yar Tags: Full Paper Source Type: research
Design, Synthesis, and Biological Evaluation of Novel 1,2,4 ‐Trioxanes as Potential Antimalarial Agents
A series of substituted 1,2,4‐trioxanes were synthesized and evaluated for their antimalarial potential, in silico ADME properties and cytotoxicity on neuronal cell lines. Among the 15 synthesized substituted 1,2,4‐trioxanes, two compounds (compound 15, IC50 = 25.71 nM; compound 21, IC50 = 19.6 nM) exhibited promising in vitro antimalarial potential comparable to those of the existing drugs chloroquine and artemisinin. Both of these compounds were found to be nontoxic up to 20 µM concentration in neuronal PC‐12 cells. Compound 21 may serve as an optimized lead compound because of its less in vitro toxi...
Source: Archiv der Pharmazie - January 31, 2017 Category: Drugs & Pharmacology Authors: Amit K. Gupta, Kanika Varshney, Vivek Kumar, Kumkum Srivastava, Aditya B. Pant, Sunil K. Puri, Anil K. Saxena Tags: Full Paper Source Type: research
2 ‐Benzamido‐4‐methylthiazole‐5‐carboxylic Acid Derivatives as Potential Xanthine Oxidase Inhibitors and Free Radical Scavengers
The new chemical entities febuxostat and topiroxostat have been approved by the US Food and Drug Administration, opening new avenues for exploiting different heterocycles other than purines as xanthine oxidase (XO) inhibitors. A different series of substituted 2‐benzamido‐4‐methylthiazole‐5‐carboxylic acid derivatives (5a–r) was synthesized and characterized by the collective use of IR, 1H and 13C NMR, and mass spectroscopy, for the treatment of gout and hyperuricemia. In vitro studies of the synthesized derivatives revealed that the presence of a fluoro group at the para position in 5b (IC50 = 0.57 μm) ...
Source: Archiv der Pharmazie - January 29, 2017 Category: Drugs & Pharmacology Authors: Md. Rahmat Ali, Suresh Kumar, Obaid Afzal, Nishtha Shalmali, Wazid Ali, Manju Sharma, Sandhya Bawa Tags: Full Paper Source Type: research
Further Developments
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Source: Archiv der Pharmazie - January 4, 2017 Category: Drugs & Pharmacology Authors: Holger Stark Tags: Editorial Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (1/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 4, 2017 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (1/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 4, 2017 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
New 3 ‐Substituted‐2‐(4‐hydroxyanilino)pyridine Derivatives: Synthesis, Antitumor Activity, and Tubulin Polymerization Inhibition
A series of new pyridine derivatives 4a–c, 5a–d, 6a–d, 7a–f, and 8a–f structurally related to ABT‐751 were synthesized and characterized by spectroscopic means and elemental analysis. All the synthesized compounds were tested for their cytotoxic activity in vitro against the HCT‐116 and HepG‐2 cancer cell lines using the MTT assay. The results showed that compound 8d has higher cytotoxic activity than the reference antimitotic agent colchicine, against both tested cell lines, with IC50 = 0.52 and 1.40 μM, respectively. The three most active compounds, 5d, 8b, and 8d, were further screened in vitro fo...
Source: Archiv der Pharmazie - December 31, 2016 Category: Drugs & Pharmacology Authors: Salwa Elmeligie, Nadia A. Khalil, Eman M. Ahmed, Soha H. Emam Tags: Full Paper Source Type: research
Design and Synthesis of Novel 4 ‐Phenoxyquinolines Bearing 3‐Hydrosulfonylacrylamido or 1H‐Imidazole‐4‐carboxamido Scaffolds as c‐Met Kinase Inhibitors
A series of novel 6,7‐disubstituted‐4‐phenoxyquinoline derivatives bearing (E)‐3‐hydrosulfonylacrylamido or 1H‐imidazole‐4‐carboxamido moieties were designed, synthesized and evaluated for their cytotoxicity against A549, MKN‐45, and HT‐29 cancer cell lines in vitro. All the target compounds showed moderate to significant cytotoxic activity against the tested cells with IC50 values ranging from 0.13 to 2.65 µM. Five of them were further examined for their inhibitory activity against c‐Met kinase, which identified compound 30 as a promising agent (c‐Met IC50 = 1.52 nM) with IC50 values of 0....
Source: Archiv der Pharmazie - December 31, 2016 Category: Drugs & Pharmacology Authors: Jiao Wang, Lijun Xie, Yu Wang, Xiaoqiang Wang, Shuancheng Xi, Tianfang Zeng, Ping Gong, Xin Zhai Tags: Full Paper Source Type: research
Design, Synthesis, and Biological Evaluation of Novel Quinazoline Clubbed Thiazoline Derivatives
A novel series of quinazoline clubbed thiazoline derivatives was rationally designed and synthesized. The newly synthesized compounds were evaluated for in vitro dipeptidyl peptidase IV (DPP‐4) inhibitory activity. Compounds that showed good to moderate activity were compared using linagliptin as standard. Compound 4x (IC50 = 1.12 nM) exhibited the most promising results. The special chemical feature of compound 4x also imparts good inhibition selectivity for DPP‐4 over DPP‐8/9. Moreover, docking of compound 4x into the active site of DPP‐4 illustrates its possible binding interactions.
A novel series of qui...
Source: Archiv der Pharmazie - December 31, 2016 Category: Drugs & Pharmacology Authors: Zulphikar Ali, Md J. Akhtar, Anees A. Siddiqui, Ahsan A. Khan, Md R. Haider, Mohammad S. Yar Tags: Full Paper Source Type: research
Design and Synthesis of 5 ‐Substituted Benzo[d][1,3]dioxole Derivatives as Potent Anticonvulsant Agents
A series of 5‐substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six compounds, 3a, 3c, 3d, and 4d–f, showed promising anticonvulsant activities in the MES model, and compounds 4c and 4d exhibited full protection against seizures at doses of 300 mg/kg in the scPTZ model. Among the synthesized compounds, 3c as the most active compound showed high protection against the MES‐induced seizures with...
Source: Archiv der Pharmazie - December 31, 2016 Category: Drugs & Pharmacology Authors: Shiyang Dong, Tiantian Wang, Chundi Hu, Xiaodong Chen, Yi Jin, Zengtao Wang Tags: Full Paper Source Type: research
Contents: Arch. Pharm. Chem. Life Sci. (12/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 1, 2016 Category: Drugs & Pharmacology Tags: Contents Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (12/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 1, 2016 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (12/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 1, 2016 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Synthesis of Novel Pyrazolines, Their Boron –Fluorine Complexes, and Investigation of Antibacterial, Antioxidant, and Enzyme Inhibition Activities
New 3,5‐disubstituted‐2‐pyrazoline derivatives (4–6), their boron‐fluorine complexes (boron (3‐(2′‐aminophenyl),5‐(2′‐/3′‐/4′‐pyridyl)pyrazoline, BOAPPY) (7–9) and boron 1,2′‐diazaflavone complex (BODAF) (11) were synthesized starting from azachalcones (1–3) to diazaflavone (10), respectively. Biological evaluation of compounds 4–9 and 11 showed remarkable antioxidant, antibacterial, and acetylcholinesterase and tyrosinase enzyme inhibition activities. All newly synthesized compounds 4–9 and 11 showed respectable antibacterial effect with minimum inhibitory concentrations in the ra...
Source: Archiv der Pharmazie - November 30, 2016 Category: Drugs & Pharmacology Authors: Nuran Kahriman, Zeynep Ha şimoğlu, Vildan Serdaroğlu, Fatih Şaban Beriş, Burak Barut, Nurettin Yaylı Tags: Full Paper Source Type: research
Discovery of Bisindole as a Novel Scaffold for Protein Tyrosine Phosphatase 1B Inhibitors
Protein tyrosine phosphatase 1B (PTP1B) has been proposed to be an effective target for the treatment of both type II diabetes and obesity. However, no PTP1B inhibitor has come into clinic application. Herein, we report mixed 3,3′‐bisindoles as novel PTP1B inhibitors with low micromole‐ranged inhibitory activity. The best active compound 9f inhibited PTP1B activity with an IC50 of 2.79 µM. Meanwhile, it had low cytotoxicity and enhanced glucose uptake in vitro. Further studies demonstrated that some of these active compounds had a specific selectivity over other PTPs. Computational analysis further showed the bind...
Source: Archiv der Pharmazie - November 30, 2016 Category: Drugs & Pharmacology Authors: Changcheng Jing, Ziyan Li, Kaili Jia, Chen Chen, Xiao Liu, Beibei Wang, Wenhao Hu, Jia Li, Tong Zhu, Suzhen Dong Tags: Full Paper Source Type: research
