Cover Picture: Arch. Pharm. Chem. Life Sci. (5/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - May 2, 2017 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
New Anti ‐Seizure (Arylalkyl)azole Derivatives: Synthesis, In Vivo and In Silico Studies
(Arylalkyl)azoles are a class of antiepileptic compounds including nafimidone, denzimol, and loreclezole (LRZ). Nafimidone and denzimol are thought to inhibit voltage‐gated sodium channels (VGSCs) and enhance γ‐aminobutyric acid (GABA)‐mediated response. LRZ, a positive allosteric modulator of A‐type GABA receptors (GABAARs), was reported to be sensitive to Asn265 of the β2/β3 subunit. Here, we report new N‐[1‐(4‐chlorophenyl)‐2‐(1H‐imidazol‐1‐yl)ethylidene]hydroxylamine esters showing anticonvulsant activity in animal models, including the 6‐Hz psychomotor seizure test, a model for therapy‐r...
Source: Archiv der Pharmazie - May 2, 2017 Category: Drugs & Pharmacology Authors: Suat Sari, Sevim Dalkara, Filiz Bet ül Kaynak, Jóhannes Reynisson, Selma Saraç, Arzu Karakurt Tags: Full Paper Source Type: research
Mannich Curcuminoids as Potent Anticancer Agents
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 for anti‐proliferative activity against A549 and H1975 lung adenocarcinoma cells. The TNFα‐induced NF‐κB inhibition and autophagy induction effects correlated strongly with the cytotoxic potential of the analogues. Significant inhibition of tumour growth was observed when the most potent analogue 44 was added in liposome...
Source: Archiv der Pharmazie - May 1, 2017 Category: Drugs & Pharmacology Authors: M árió Gyuris, László Hackler, Lajos I. Nagy, Róbert Alföldi, Eszter Rédei, Annamária Marton, Tibor Vellai, Nóra Faragó, Béla Ózsvári, Anasztázia Hetényi, Gábor K. Tóth, Péter Sipos, Iván Kanizsai, László G. Puskás Tags: Full Paper Source Type: research
Oxazolo[4,5 ‐b]pyridine‐Based Piperazinamides as GSK‐3β Inhibitors with Potential for Attenuating Inflammation and Suppression of Pro‐Inflammatory Mediators
Recent studies reveal that glycogen synthase kinase‐3β (GSK‐3β) acts as a pro‐inflammatory enzyme, and by inhibiting this kinase, inflammation can be controlled. In this regard, a series of 17 piperazine‐linked oxazolo[4,5‐b]pyridine‐based derivatives was synthesized and evaluated for in vitro GSK‐3β inhibitory and in vivo anti‐inflammatory activity. The compounds 7d, 7e, 7g, and 7c displayed the best GSK‐3β inhibitory activity among all the synthesized compounds, with corresponding IC50 values of 0.34, 0.39, 0.47, and 0.53 µM. Among the compounds 7d, 7e, 7g, and 7c examined for in vivo anti‐infl...
Source: Archiv der Pharmazie - May 1, 2017 Category: Drugs & Pharmacology Authors: Mushtaq A. Tantray, Imran Khan, Hinna Hamid, Mohammad Sarwar Alam, Abhijeet Dhulap, Ajaz Ahmad Ganai Tags: Full Paper Source Type: research
A Novel Pregabalin Functionalized Salicylaldehyde Derivative Afforded Prospective Pain, Inflammation, and Pyrexia Alleviating Propensities
A novel pregabalin derivative named as pregsal ((S,E)‐3‐(((2‐hydroxybenzylidene)amino)methyl)‐5‐methylhexanoic acid) was synthesized by a simple imination reaction between pregabalin and salicylaldehyde and was evaluated in the in vivo testing paradigms. The compound was characterized by UV, IR, 1H, 13C NMR, HR ESI‐MS, and elemental analysis. It was screened (30, 50, 75, and 100 mg/kg) for antinociceptive, anti‐inflammatory, and antipyretic activities in relation to pregabalin. The synthesized compound significantly attenuated the tonic acetic acid‐induced nociceptive pain (30 mg/kg (P < 0.05), 5...
Source: Archiv der Pharmazie - May 1, 2017 Category: Drugs & Pharmacology Authors: Nisar Ahmad, Fazal Subhan, Nazar Ul Islam, Muhammad Shahid, Faiz Ur Rahman, Khwaja Fawad Tags: Full Paper Source Type: research
Synthesis and Biological Evaluation of New Combined α/β‐Adrenergic Blockers
The synthesis, characterization, and pharmacological evaluation of new aryloxyaminopropanol compounds based on substituted (4‐hydroxyphenyl)ethanone with alterations in the alkoxymethyl side chain in position 2 and with 2‐methoxyphenylpiperazine in the basic part of the molecule are reported. For the in vitro pharmacological evaluation, isolated aorta and atria from normotensive Wistar rats were used. Compared to naftopidil, compounds with ethoxymethyl, propoxymethyl, butoxymethyl, and methoxyethoxymethyl substituent displayed similar α1‐adrenolytic potency. Compounds with methoxymethyl, ethoxymethyl, and propoxymet...
Source: Archiv der Pharmazie - May 1, 2017 Category: Drugs & Pharmacology Authors: Andrej N émethy, Peter Vavrinec, Diana Vavrincová‐Yaghi, Diana Čepcová, Svetozár Mišúth, Eva Král'ová, Ružena Čižmáriková, Eva Račanská Tags: Full Paper Source Type: research
Novel NHC Precursors: Synthesis, Characterization, and Carbonic Anhydrase and Acetylcholinesterase Inhibitory Properties
Three series of imidazolidinium ligands (NHC precursors) substituted with 4‐vinylbenzyl, 2‐methyl‐1,4‐benzodioxane, and N‐propylphthalimide were synthesized. N‐Heterocyclic carbene (NHC) precursors were prepared from N‐alkylimidazoline and alkyl halides. The novel NHC precursors were characterized by 1H NMR, 13C NMR, FTIR spectroscopy, and elemental analysis techniques. The enzymes inhibition activities of the NHC precursors were investigated against the cytosolic human carbonic anhydrase I and II isoenzymes (hCA I and II) and the acetylcholinesterase (AChE) enzyme. The inhibition parameters (IC50 and Ki valu...
Source: Archiv der Pharmazie - May 1, 2017 Category: Drugs & Pharmacology Authors: Ayd ın Aktaş, Parham Taslimi, İlhami Gülçin, Yetkin Gök Tags: Full Paper Source Type: research
Synthesis and Evaluation of 5 ‐(o‐Tolyl)‐1H‐tetrazole Derivatives as Potent Anticonvulsant Agents
A series of 5‐(o‐tolyl)‐1H‐tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1‐(2‐Methylbenzyl)‐5‐(o‐tolyl)‐1H‐tetrazole (3h) showed important anticonvulsant activity against the MES‐induced seizures, as well as lower neurotoxicity with an ED50 value of 12.7 mg/kg and a TD50 value of over 500 mg/kg after intraperitoneal injection into mice, providing 3h with a high protective index (TD50/ED50) of over 39.4. The achieved results prove that the distinctive compounds could be valuable as a model for future development, adaptation, and investigation to constru...
Source: Archiv der Pharmazie - April 18, 2017 Category: Drugs & Pharmacology Authors: Shiyang Dong, Tiantian Wang, Huayu Wang, Kun Qian, Zhongli Zhang, Yueming Zuo, Guangming Luo, Yi Jin, Zengtao Wang Tags: Full Paper Source Type: research
Benzodioxole –Pyrazole Hybrids as Anti‐Inflammatory and Analgesic Agents with COX‐1,2/5‐LOX Inhibition and Antioxidant Potential
Two series of benzodioxole–pyrazole hybrids were synthesized and the IC50 values for in vitro inhibition of the enzymes cyclooxygenase 1/2 (COX‐1, COX‐2) and 5‐lipoxygenase (5‐LOX) were investigated. All compounds were tested for their in vivo anti‐inflammatory and analgesic potentials using diclofenac sodium as a reference standard. Compounds 4, 11, 17, 20, 21, 26, and 27, which showed good analgesic and/or anti‐inflammatory activities, were also evaluated for their ability to inhibit tumor necrosis factor (TNF)‐α production, myeloperoxidase and proteinase, beside their antioxidant activity. Collectively,...
Source: Archiv der Pharmazie - April 18, 2017 Category: Drugs & Pharmacology Authors: Heba A. Abd El Razik, Mona H. Badr, Attia H. Atta, Samar M. Mouneir, Marwa M. Abu ‐Serie Tags: Full Paper Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (3 ‐4/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - April 4, 2017 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (3 ‐4/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - April 4, 2017 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Synthesis and Evaluation of Thiazolidine Amide and N ‐Thiazolyl Amide Fluoroquinolone Derivatives
In an effort to develop new fluoroquinolones, we synthesized eight compounds and tested them against a panel of bacteria. The design of these compounds was guided by the introduction of the isothiazoloquinolone motif. The three most active compounds in this series, 8–10, demonstrated good antibacterial activity against methicillin‐sensitive Staphylococcus aureus and healthcare‐acquired methicillin‐resistant Staphylococcus aureus (MIC 0.62–6.3 µg/mL). Further, when these three active compounds were tested for their inhibitory effects on bacterial enzymes, compound 9 was the most effective agent exhibiting IC50 ...
Source: Archiv der Pharmazie - April 1, 2017 Category: Drugs & Pharmacology Authors: Isaac Garza, Miranda J. Wallace, Dinesh Fernando, Aman Singh, Richard E. Lee, Jason S. Gerding, Cynthia Franklin, Raghunandan Yendapally Tags: Full Paper Source Type: research
Evaluation of Biological Activity and Computer ‐Aided Design of New Soft Glucocorticoids
In this study, local anti‐inflammatory activity of these derivatives was evaluated by use of the croton oil‐induced ear edema test. Glucocorticoids with the highest maximal edema inhibition (MEI) were pointed out, and the systemic side effects of those with the lowest EC50 values were significantly lower in comparison to dexamethasone. A 3D‐QSAR model was created and employed for the design of 27 compounds. By use of the sequential combination of ligand‐based and structure‐based virtual screening, three compounds were selected from the ChEMBL library and used as a starting point for the design of 15 derivatives. ...
Source: Archiv der Pharmazie - April 1, 2017 Category: Drugs & Pharmacology Authors: Vladimir Dobri čić, Vesna Jaćević, Jelica Vučićević, Katarina Nikolic, Sote Vladimirov, Olivera Čudina Tags: Full Paper Source Type: research
Synthesis, Characterization, and Biological Evaluation of Some Novel Quinoxaline Derivatives as Antiviral Agents
Ethyl (6,7‐dimethyl‐2‐oxo‐3,4‐dihydroquinoxalin‐3‐yl)acetate and ethyl (6‐methyl‐2‐oxo‐3,4‐dihydroquinoxalin‐3‐yl)acetate (1a,b), 3‐methylquinoxalin‐2(1H)‐one (4) and 1,4‐dihydroquinoxaline‐2,3‐dione (11) were the starting precursors for nine novel quinoxaline compounds, 3a, 6, 10, 13, 15, 16, 17, 18, and 20, via adopting different nucleophilic reactions. The synthesized compounds were tested for their antiviral activity against HCV, HBV, HSV‐1, and HCMV. Concomitantly, their safety profile was investigated as well as their selectivity against the viral strains. The Virology Unit a...
Source: Archiv der Pharmazie - April 1, 2017 Category: Drugs & Pharmacology Authors: Heba S. A. El ‐Zahabi Tags: Full Paper Source Type: research
Synthesis and Evaluation of Novel [1,2,4]Triazolo[5,1 ‐c][1,2,4]‐triazines and Pyrazolo[5,1‐c][1,2,4]triazines as Potential Antidiabetic Agents
Inhibition of the dipeptidyl peptidase‐4 (DPP4) enzyme activity and prevention of advanced glycation end (AGE) products formation represents a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In the frames of this research study, several triazolo‐ and pyrazolotriazines were synthesized and evaluated as inhibitors of AGE products formation, DPP4, glycogen phosphorylase and α‐glucosidase activities, as well as AGE cross‐link breakers. From the two considered classes of heterocyclic compounds, the pyrazolotriazines showed the highest potency a...
Source: Archiv der Pharmazie - April 1, 2017 Category: Drugs & Pharmacology Authors: Vladimir L. Rusinov, Irina M. Sapozhnikova, Anastasiya M. Bliznik, Oleg N. Chupakhin, Valery N. Charushin, Alexander A. Spasov, Pavel M. Vassiliev, Valentina A. Kuznetsova, Andrey I. Rashchenko, Denis A. Babkov Tags: Full Paper Source Type: research
