Mannich ‐Benzimidazole Derivatives as Antioxidant and Anticholinesterase Inhibitors: Synthesis, Biological Evaluations, and Molecular Docking Study
A series of Mannich bases of benzimidazole derivatives having a phenolic group were designed to assess their anticholinesterase and antioxidant activities. The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities were evaluated in vitro by using Ellman's method. According to the activity results, all of the compounds exhibited moderate to good AChE inhibitory activity (except for 2a), with IC50 values ranging from 0.93 to 10.85 μM, and generally displayed moderate BuChE inhibitory activity. Also, most of the compounds were selective against BuChE. Compound 4b was the most active molecule o...
Source: Archiv der Pharmazie - April 1, 2017 Category: Drugs & Pharmacology Authors: Ay şe Selcen Alpan, Görkem Sarıkaya, Güneş Çoban, Sülünay Parlar, Güliz Armagan, Vildan Alptüzün Tags: Full Paper Source Type: research
Synthesis and Structure –Activity Relationships of Novel Benzylamine‐Type Antifungals as Butenafine‐Related Antimycotics
Benzylamine‐type antimycotics like naftifine, butenafine, or terbinafine are a well‐known class of antimycotics since the 1980s. The following paper describes the synthesis and biological evaluation of a series of novel benzylamine‐type antimycotics characterized by an isooctyl side chain and various substituents at the benzylamine moiety. The compounds were prepared from benzaldehyde derivatives and 2‐amino‐6‐methylheptane by reductive amination with sodium triacetoxyborohydride and subsequent precipitation with hydrogen chloride. The antimycotic activity of the resulting compounds was evaluated in an agar dif...
Source: Archiv der Pharmazie - April 1, 2017 Category: Drugs & Pharmacology Authors: J ürgen Krauss, Martina Stadler, Franz Bracher Tags: Full Paper Source Type: research
Design, Synthesis, and Evaluation of the Kinase Inhibition Potential of Pyridylpyrimidinylaminophenyl Derivatives
In view of potent kinase inhibitors for the treatment of myriad human disorders, we synthesized some structurally variant amide/cyclic amide derivatives based on pyridylpyrimidinylaminophenyl amine, the key pharmacophore of the kinase inhibitor drug molecule, imatinib, and evaluated their kinase inhibition potency. Among the various synthesized amides, compound 20, a cyclic amide/pyridin‐2(1H)‐one derivative, exhibited an IC50 value comparable to that of the drug imatinib against c‐Src kinase, and another compound (14) containing a 2‐((4‐methyl‐2‐oxo‐2H‐chromen‐6‐yl)oxy)acetamide demonstrated an IC50 ...
Source: Archiv der Pharmazie - March 19, 2017 Category: Drugs & Pharmacology Authors: Priyanka Manchanda, Badri Parshad, Amit Kumar, Rakesh K. Tiwari, Amir N. Shirazi, Keykavous Parang, Sunil K. Sharma Tags: Full Paper Source Type: research
Synthesis and Anticonvulsant Properties of New 3,3 ‐Diphenyl‐2,5‐dioxo‐pyrrolidin‐1‐yl‐acetamides and 3,3‐Diphenyl‐propionamides
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 appropriate secondary amines in the presence of carbonyldiimidazole (CDI) as a coupling reagent. The initial anticonvulsant screening was performed in mice intraperitoneally (i.p.) using the “classical” maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure models, whereas the acute ...
Source: Archiv der Pharmazie - March 19, 2017 Category: Drugs & Pharmacology Authors: Jolanta Obniska, Anna Rapacz, Sabina Rybka, Ma łgorzata Góra, Paweł Żmudzki, Krzysztof Kamiński Tags: Full Paper Source Type: research
Design, Synthesis, and Cytotoxic Evaluation of Certain 7 ‐Chloro‐4‐(piperazin‐1‐yl)quinoline Derivatives as VEGFR‐II Inhibitors
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 2‐chloro‐1‐(4‐(7‐chloroquinolin‐4‐yl)piperazin‐1‐yl)ethanone (3) with different secondary amines. The structures of the target compounds were confirmed by IR, 1H‐NMR, 13C‐NMR, HRMS, and microanalysis. Compounds 4a–t were subjected to in vitro anticancer screening against human breast cancer (MCF‐7) and ...
Source: Archiv der Pharmazie - March 16, 2017 Category: Drugs & Pharmacology Authors: Mohamed Nabil Aboul ‐Enein, Aida M. Abd El‐Sattar El‐Azzouny, Fatma Abdel‐Fattah Ragab, Mohamed Farouk Hamissa Tags: Full Paper Source Type: research
Interaction of Approved Drugs with Synaptic Vesicle Protein 2A
Levetiracetam (LEV) and its recently approved derivative brivaracetam are anti‐epileptic drugs with a unique mechanism of action. The synaptic vesicle protein 2A (SV2A) was previously identified as their main target. In the current study, we tested a collection of 500 approved drugs for interaction with the human SV2A protein expressed in Chinese hamster ovary cells. Competition binding studies were performed using cell lysates with high SV2A expression and [3H]brivaracetam as a radioligand. A hit rate of 3% was obtained, defined as compounds that inhibited radioligand binding by more than 90% at a screening concentratio...
Source: Archiv der Pharmazie - February 20, 2017 Category: Drugs & Pharmacology Authors: Azeem Danish, Vigneshwaran Namasivayam, Anke C. Schiedel, Christa E. M üller Tags: Full Paper Source Type: research
Synthesis, Anticonvulsant Activity, and SAR Study of Novel 4 ‐Quinazolinone Derivatives
Series of N‐(4‐substitutedphenyl)‐4‐(1‐methyl (or 1,2‐dimethyl)‐4‐oxo‐1,2‐dihydroquinazolin‐3(4H)‐yl)‐alkanamides (5a–j) and 4‐chloro‐N′‐((1‐methyl (or 1,2‐dimethyl)‐4‐oxo‐1,2‐dihydroquinazolin‐3(4H)‐yl)‐alkaloyl)benzohydrazides (6a–f) were designed based on the previously reported essential structural features for anticonvulsant activity. Several amino acids were incorporated within the synthesized quinazolin‐4(3H)‐ones to improve their bioavailability and the anticonvulsant activity. Synthesis of the target compounds was accomplished in four steps starting from ...
Source: Archiv der Pharmazie - February 7, 2017 Category: Drugs & Pharmacology Authors: Nada A. Noureldin, Hend Kothayer, El ‐Sayed M. Lashine, Mohamed M. Baraka, Wafaa El‐Eraky, Sally A. El Awdan Tags: Full Paper Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (2/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 7, 2017 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (2/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 7, 2017 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Diclofenac ‐Based Hydrazones and Spirothiazolidinones: Synthesis, Characterization, and Antimicrobial Properties
We report here the synthesis, structural characterization, and biological evaluation of novel diclofenac‐based hydrazone (4a–f) and spirothiazolidinone (5a–f, 6a–f) derivatives designed as potential antimicrobial agents. The compounds were evaluated in vitro for their antiviral activity against a wide spectrum of DNA and RNA viruses. They were further screened in vitro against different strains of bacteria and fungi. The hydrazone derivatives, 4a and 4c–f, were found to be active against herpesviruses (HSV‐1, HSV‐2, and HSV‐1 TK−), vaccinia virus, and Coxsackie B4 virus, with EC50 values between 6.6 µg...
Source: Archiv der Pharmazie - February 1, 2017 Category: Drugs & Pharmacology Authors: Ay şe Kocabalkanlı, Gökçe Cihan‐Üstündağ, Lieve Naesens, Emel Mataracı‐Kara, Mebble Nassozi, Gültaze Çapan Tags: Full Paper Source Type: research
Synthesis, Anti ‐Inflammatory Activity, and COX‐1/2 Inhibition Profile of Some Novel Non‐Acidic Polysubstituted Pyrazoles and Pyrano[2,3‐c]pyrazoles
The synthesis and evaluation of the anti‐inflammatory activity of some structure hybrids comprising basically the 5‐hydroxy‐3‐methyl‐1‐phenyl‐4‐substituted‐1H‐pyrazole scaffold directly linked to a variety of heterocycles and functionalities, or annulated as pyrano[2,3‐c]pyrazoles, is described. According to the in vivo results and a comprehensive structure–activity relationship study, five analogs (5, 10, 17, 19, and 27) displayed remarkable anti‐inflammatory profiles showing distinctive % protection and ED50 values, especially 10 and 27 (ED50 35.7 and 38.7 μmol/kg, respectively) which were ne...
Source: Archiv der Pharmazie - February 1, 2017 Category: Drugs & Pharmacology Authors: Hassan M. Faidallah, Sherif A. F. Rostom Tags: Full Paper Source Type: research
Synthesis, Characterization, and Evaluation of Difluoropyrido[4,3 ‐b]indoles as Potential Agents for Acetylcholinesterase and Antiamnesic Activity
Acetylcholinesterase (AChE) inhibitors are currently the most widely prescribed drugs for Alzheimer's disease. The high potential of indole compounds in medicinal chemistry led us to discover a novel series of fluoroindole compounds. The synthesis and pharmacological analysis of the difluoropyrido[4,3‐b]indoles 11–34 are described. Compounds 11–34 were tested for AChE inhibition activity using a rat brain homogenate. Compounds 25–29 display a promising in vitro profile with an IC50 value range of 46–51.6 nM and show significant protective effect on scopolamine‐induced amnesia. The present data indicate that c...
Source: Archiv der Pharmazie - February 1, 2017 Category: Drugs & Pharmacology Authors: Malavalli Madaiah, Bidarur K. Jayanna, Arakere S. Manu, Maralekere K. Prashanth, Hosakere D. Revanasiddappa, Bantal Veeresh Tags: Full Paper Source Type: research
Design and Synthesis of Novel Anti ‐Plasmodial Histone Deacetylase Inhibitors Containing an Alkoxyamide Connecting Unit
Despite recent declines in mortality, malaria remains an important global health problem. New therapies are needed, including new drugs with novel modes of action compared to existing agents. Among new potential therapeutic targets for malaria, inhibition of parasitic histone deacetylases (HDACs) is a promising approach. Homology modeling of PfHDAC1, a known target of some anti‐plasmodial HDAC inhibitors, revealed a unique threonine residue at the rim of the active site in close proximity to the location of the cap group of vorinostat‐type HDAC inhibitors. Aiming to obtain HDAC inhibitors with potent and preferential a...
Source: Archiv der Pharmazie - January 31, 2017 Category: Drugs & Pharmacology Authors: Leandro A. Alves Avelar, Jana Held, Jessica A. Engel, Parichat Sureechatchaiyan, Finn K. Hansen, Alexandra Hamacher, Matthias U. Kassack, Benjamin Mordm üller, Katherine T. Andrews, Thomas Kurz Tags: Full Paper Source Type: research
Antiviral and Cytostatic Evaluation of 5 ‐(1‐Halo‐2‐sulfonylvinyl)‐ and 5‐(2‐Furyl)uracil Nucleosides
Transition metal‐catalyzed halosulfonylation of 5‐ethynyl uracil nucleosides provided (E)‐5‐(1‐chloro‐2‐tosylvinyl)uridines. Tetrabutylammonium fluoride‐mediated direct CH arylation of 5‐iodouracil nucleosides with furan or 2‐heptylfuran gave 5‐furyl‐substituted nucleosides without the necessity of using the organometallic substrates. These two classes of 5‐substituted uracil nucleosides as well their corresponding ester derivatives were tested against a broad range of DNA and RNA viruses and the human immunodeficiency virus (HIV). The 3′,5′‐di‐O‐acetyl‐5‐(E)‐(1‐chloro‐2‐t...
Source: Archiv der Pharmazie - January 31, 2017 Category: Drugs & Pharmacology Authors: Zhiwei Wen, Sazzad H. Suzol, Jufang Peng, Yong Liang, Robert Snoeck, Graciela Andrei, Sandra Liekens, Stanislaw F. Wnuk Tags: Full Paper Source Type: research
Synthesis and Pharmacological Evaluation of Acrylate ‐Based Gastrosparing NSAID Prodrugs
Dexibuprofen and aceclofenac are well‐known NSAID molecules, their oral use leads to gastrointestinal (GI) toxicity. To circumvent that GI toxicity, the prodrug approach is a better alternative. Hence, this research was undertaken to synthesize prodrugs of dexibuprofen and aceclofenac using acrylic polymers with degradable ester bonds. Dexibuprofen was linked to 2‐hydroxypropyl methacrylate by an activated ester technique. The resulting material was copolymerized with 2‐hydroxyethyl methacrylate and methyl methacrylate (in 1:3 mole ratios) by the free radical polymerization method, utilizing azoisobutyronitrile at 65...
Source: Archiv der Pharmazie - January 31, 2017 Category: Drugs & Pharmacology Authors: Arun Rasheed, Prasanna Raju Yalavarthi, Haseena Cheramparambil, Jaya Preethi Peesa, Azeem Abdul Khareem Tags: Full Paper Source Type: research
