Cover Picture: Arch. Pharm. Chem. Life Sci. (9/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 31, 2016 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Contents: Arch. Pharm. Chem. Life Sci. (8/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 1, 2016 Category: Drugs & Pharmacology Tags: Contents Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (8/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 1, 2016 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (8/2016)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 1, 2016 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Antimycobacterial Metabolites from Marine Invertebrates
Marine organisms play an important role in natural product‐based drug research due to accumulation of structurally unique and bioactive metabolites. The exploration of marine‐derived compounds may significantly extend the scientific knowledge of potential scaffolds for antibiotic drug discovery. Development of novel antitubercular agents is especially significant as the emergence of drug‐resistant Mycobacterium tuberculosis strains remains threateningly high. Marine invertebrates (i.e., sponges, corals, gorgonians) as a source of new chemical entities are the center of research for several scientific groups, and the ...
Source: Archiv der Pharmazie - July 31, 2016 Category: Drugs & Pharmacology Authors: Georgios Daletos, Elena Ancheeva, Chaidir Chaidir, Rainer Kalscheuer, Peter Proksch Tags: Review Article Source Type: research
Microwave Assisted Synthesis of Pyrimidines in Ionic Liquid and Their Potency as Non ‐Classical Malarial Antifolates
Synthesis of pyrazole‐linked triazolo‐pyrimidine hybrids was achieved by employing Biginelli‐type reaction methodology in an ionic liquid (triethylammonium acetate) under microwave irradiation. This method proved to be highly efficient and the ionic liquid employed was found recyclable for up to five consecutive cycles. The synthesized molecules were further screened for their antimalarial efficacy screening out the active scaffolds J15, J18, J21, J24, J27, and J30. The active molecules were evaluated in an enzyme inhibition study against the active Plasmodium falciparum dihydrofolate reductase (Pf‐DHFR), computati...
Source: Archiv der Pharmazie - July 31, 2016 Category: Drugs & Pharmacology Authors: Jaimin D. Bhatt, Chaitanya J. Chudasama, Kanuprasad D. Patel Tags: Full Paper Source Type: research
Suppression of Toll ‐Like Receptor 4 Dimerization by 1‐[5‐Methoxy‐2‐(2‐nitrovinyl)phenyl]pyrrolidine
Toll‐like receptor 4 (TLR4) recognizes lipopolysaccharide (LPS) and triggers the activation of myeloid differention factor 88 (MyD88) and the Toll/interleukin‐1 receptor domain‐containing adapter, inducing interferon‐β (TRIF)‐dependent major downstream signaling pathways. To evaluate the therapeutic potential of 1‐[5‐methoxy‐2‐(2‐nitrovinyl)phenyl]pyrrolidine (MNP), previously synthesized in our laboratory, its effect on signal transduction via the TLR signaling pathways was examined. Here, we investigated whether MNP modulates the TLR4 signaling pathways and which anti‐inflammatory target in TLR4 si...
Source: Archiv der Pharmazie - July 31, 2016 Category: Drugs & Pharmacology Authors: Sang ‐Il Ahn, Ji‐Soo Kim, Gyo‐Jeong Gu, Hyeon‐Myeong Shin, Ah‐Yeon Kim, Hyun‐Jin Shim, Yeon Joo Kim, Kwang Oh Koh, Joo Yang Mang, Dae Young Kim, Hyung‐Sun Youn Tags: Full Paper Source Type: research
Structure –5‐HT/D2 Receptor Affinity Relationship in a New Group of 1‐Arylpiperazynylalkyl Derivatives of 8‐Dialkylamino‐3,7‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione
In our previous papers, we have reported that some 8‐amino‐1,3‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione derivatives possessed high affinity and displayed agonistic, partial agonistic, or antagonistic activity for serotonin 5‐HT1A and dopamine D2 receptors. In order to examine further the influence of the substituent in the position 8 of the purine moiety and the influence of the xanthine core on the affinity for serotonin 5‐HT1A, 5‐HT2A, 5‐HT6, 5‐HT7, and dopamine D2 receptors, two series of 1‐arylpiperazynylalkyl derivatives of 8‐amino‐3,7‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione were synthes...
Source: Archiv der Pharmazie - July 31, 2016 Category: Drugs & Pharmacology Authors: Pawe ł Żmudzki, Grzegorz Satała, Grażyna Chłoń‐Rzepa, Andrzej J. Bojarski, Grzegorz Kazek, Agata Siwek, Anna Gryboś, Monika Głuch‐Lutwin, Anna Wesołowska, Maciej Pawłowski Tags: Full Paper Source Type: research
Canthin ‐4‐ones as Novel Antibacterial Agents
Based on the chemotype of canthin‐4‐one alkaloids with moderate antimicrobial activity, a collection of variously substituted canthin‐4‐ones and desaza analogs were synthesized. Key steps in the syntheses were regioselective halogenations of (desaza) canthin‐4‐one, followed by Pd‐catalyzed cross‐coupling reactions. The in vitro screening for antimicrobial activity revealed that two 5‐substituted canthin‐4‐ones (3‐pyridyl, 2‐bromophenyl) exhibit significant activity against Streptococcus entericus, coupled with high selectivity and the lack of cytotoxicity against mammalian cells. The intact canthi...
Source: Archiv der Pharmazie - July 31, 2016 Category: Drugs & Pharmacology Authors: Tim Tremmel, Andreas Puzik, Andr é P. Gehring, Franz Bracher Tags: Full Paper Source Type: research
Organocatalyzed Novel Synthetic Methodology for Highly Functionalized Piperidines as Potent α‐Glucosidase Inhibitors
An efficient atom‐economic one‐pot synthesis of highly functionalized piperidines was achieved by catalytic multicomponent reaction. A wide range of heterogeneous and homogenous catalysts were explored; however, promising results were achieved when a β‐keto‐ester was reacted with selected aromatic aldehydes and anilines by using N‐acetyl glycine (NAG) as catalyst. The implication of this methodology is straightforward since the products were precipitated out from the reaction solution, eliminating the need of column chromatography purifications. The synthesized piperidines were screened against α‐glucosidase ...
Source: Archiv der Pharmazie - July 31, 2016 Category: Drugs & Pharmacology Authors: Ariba Farooq, Lubna Shahazadi, Marek Bajda, Nisar Ullah, Abdul Rauf, Sohail Anjum Shahzad, Ather Farooq Khan, Muhammad Ashraf, Muhammad Yar Tags: Full Paper Source Type: research
Synthesis and In Vitro Pharmacological Evaluation of 5 ‐(Alkoxymethyl)‐2‐(3‐alkylamino‐2‐hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol
The structure–activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2‐hydroxyphenylethanone as potential β‐blockers are described. The synthesized compounds possess an isopropyl or a tert‐butyl group in the hydrophilic part of the molecule and an alkoxymethyl substitution in the lipophilic moiety. The target compounds were prepared by an established four‐step method and their structures were confirmed by interpretation of their UV, IR, 1H NMR and 13C NMR spectra, and by elemental analysis. The β‐adrenolytic efficacy of the prepared racemic compounds was determined on isolated guinea p...
Source: Archiv der Pharmazie - July 14, 2016 Category: Drugs & Pharmacology Authors: Katar ína Bruchatá, Andrej Némethy, Ružena Čižmáriková, Eva Račanská, Ladislav Habala Tags: Full Paper Source Type: research
Synthesis and Anti ‐Proliferative Activity of Sulfanyltriazolylnaphthalenols and Sulfanyltriazolylnaphthalene‐1,4‐diones
A series of new sulfanyltriazolylnaphthalenols (10a–f and 13a–f) and sulfanyltriazolylnaphthalene‐1,4‐diones (14a–f) were synthesized and evaluated against a panel of cancer cell lines. Among the tested compounds, 10b and 10d showed the best anti‐proliferative activity with GI50 values ranging from 2.72 to 10 and 3.13 to 13.1 µM, respectively, in several of the tumor cell lines tested. Compound 10d is highly selective toward leukemia cell lines and can be regarded as a good model for the development of new anti‐leukemic agents.
New sulfanyltriazolylnaphthalenols and sulfanyltriazolylnaphthalene‐1,4‐di...
Source: Archiv der Pharmazie - July 11, 2016 Category: Drugs & Pharmacology Authors: Ibrahim Chaaban, El Sayeda M. El Khawass, Heba A. Abd El Razik, Nehad S. El Salamouni, Mariano Redondo ‐Horcajo, Isabel Barasoain, José Fernando Díaz, Jari Yli‐Kauhaluoma, Vânia M. Moreira Tags: Full Paper Source Type: research
Synthesis of Arylazide ‐ and Diazirine‐Containing CrAsH‐EDT2 Photoaffinity Probes
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 3, 2016 Category: Drugs & Pharmacology Authors: Shameem S. Syeda, Daren Rice, Derek J. Hook, Leslie L. Heckert, Gunda I. Georg Tags: Erratum Source Type: research
Identification of Indole ‐Based Chalcones: Discovery of a Potent, Selective, and Reversible Class of MAO‐B Inhibitors
A series of 11 indole‐based chalcones (IC1–11) with various electron donating and withdrawing groups at the para position of the phenyl ring B were synthesized. All the compounds were tested for their human monoamine oxidase (hMAO)‐A and hMAO‐B inhibitory potencies. Most of the synthesized candidates proved to be potent and selective inhibitors of MAO‐B rather than MAO‐A, with a reversible and competitive mode. Among them, compound IC9 was found to be a potent inhibitor of hMAO‐B with Ki = 0.01 ± 0.005 μM and a selectivity index of 120. It was found to be better than the standard drug, selegiline ...
Source: Archiv der Pharmazie - July 3, 2016 Category: Drugs & Pharmacology Authors: Rani Sasidharan, Sreedharannair Leelabaiamma Manju, G ülberk Uçar, Ipek Baysal, Bijo Mathew Tags: Full Paper Source Type: research
Synthesis of Arylazide‐ and Diazirine‐Containing CrAsH‐EDT2 Photoaffinity Probes
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 3, 2016 Category: Drugs & Pharmacology Authors: Shameem S. Syeda, Daren Rice, Derek J. Hook, Leslie L. Heckert, Gunda I. Georg Tags: Erratum Source Type: research
