Cover Picture: Arch. Pharm. Chem. Life Sci. (1/2018)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 3, 2018 Category: Drugs & Pharmacology Tags: COVER PICTURE Source Type: research
Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti ‐tubercular agents
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 2, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 2, 2018 Category: Drugs & Pharmacology Source Type: research
Biological evaluation and pharmacophore modeling of some benzoxazoles and their possible metabolites
Abstract
A series of benzoxazole derivatives and some possible primary metabolites were evaluated as anticancer agents. In vitro anti‐proliferative activities of the compounds were tested using the SRB assay on cancerous (HeLa) and non‐cancerous (L929) cell lines. It was found that 17 of 21 tested compounds had cytotoxic activity on HeLa cells and the cytotoxic activities of the compounds were 15–700 times higher than on L929 cells. We generated two distinct pharmacophore models for the cytotoxic activities of the compounds on HeLa and L929 cells. While active compounds such as camptothecin and X8 fitted the two mode...
Source: Archiv der Pharmazie - January 1, 2018 Category: Drugs & Pharmacology Authors: Fatma Zilifdar, Egemen Foto, Tugba Ertan ‐Bolelli, Esin Aki‐Yalcin, Ismail Yalcin, Nuran Diril Tags: FULL PAPER Source Type: research
Design, synthesis, and evaluation of new α‐aminonitrile‐based benzimidazole biomolecules as potent antimicrobial and antitubercular agents
Abstract
The study explores the one‐pot synthesis of novel α‐aminonitriles by reacting 4‐[(1H‐benzimidazol‐2‐yl)methoxy]benzaldehyde, substituted anilines and sodium cyanide using a catalytic amount of copper dipyridine dichloride (CuPy2Cl2) and employing the Strecker reaction under mild conditions. All the synthesized compounds were screened for antimicrobial and antitubercular activity. The promising lead compounds 4d and 4e were identified, with MIC values ranging between 3.9 and 7.8 µg/mL against different bacterial strains. Compounds 4c–e and 4g also showed good antifungal activities against the test...
Source: Archiv der Pharmazie - January 1, 2018 Category: Drugs & Pharmacology Authors: Irfan N. Shaikh, Kallappa M. Hosamani, Mahantesh M. Kurjogi Tags: FULL PAPER Source Type: research
Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity
Abstract
A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α‐glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14–3.92 nM against AChE, 0.24–1.64 nM against BChE, 6.73–51.10 nM against α‐glycosidase, 1.80–5.10 nM against hCA I, and 1.14–5.45 nM against hCA II.
A series of novel phloroglucinol derivatives...
Source: Archiv der Pharmazie - January 1, 2018 Category: Drugs & Pharmacology Authors: Serdar Burmaoglu, Ali O. Yilmaz, Parham Taslimi, Oztekin Algul, Deryanur Kilic, Ilhami Gulcin Tags: FULL PAPER Source Type: research
Oxaprozin prodrug as safer nonsteroidal anti ‐inflammatory drug: Synthesis and pharmacological evaluation
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 28, 2017 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 28, 2017 Category: Drugs & Pharmacology Source Type: research
Synthesis and elastase inhibition activities of novel aryl, substituted aryl, and heteroaryl oxime ester derivatives
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 18, 2017 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - December 18, 2017 Category: Drugs & Pharmacology Source Type: research
Silicon ‐containing analogs of camptothecin as anticancer agents
Abstract
The plant pentacyclic alkaloid camptothecin and its structural analogs were extensively studied. These compounds are interesting due to the antitumor activity associated with their ability to inhibit topoisomerase I in tumor cells. During the last decades of the 20th century, a large number of the silicon‐containing camptothecins (silatecans) were synthesized. 7‐tert‐Butyldimethylsilyl‐10‐hydroxy‐camptothecin (DB‐67 or AR‐67) has enhanced lipophilicity and demonstrates a antitumor activity superior to its carbon analog. To date, certain silatecans are under clinical trials and their ultimate role i...
Source: Archiv der Pharmazie - December 14, 2017 Category: Drugs & Pharmacology Authors: Nataliya F. Lazareva, Viktor P. Baryshok, Igor M. Lazarev Tags: REVIEW ARTICLE Source Type: research
Synthesis of novel benzimidazole acrylonitriles for inhibition of Plasmodium falciparum growth by dual target inhibition
Abstract
Antimalarial drug resistance has emerged as a threat for treating malaria, generating a need to design and develop newer, more efficient antimalarial agents. This research aimed to identify novel leads as antimalarials. Dual receptor mechanism could be a good strategy to combat developing drug resistance. A series of benzimidazole acrylonitriles containing 18 compounds were designed, synthesized and evaluated for cytotoxicity, heme binding, ferriprotoporphyrin IX biomineralisation inhibition, and falcipain‐2 enzyme assay. Furthermore, in silico docking and MD simulation studies were also performed.The tests reve...
Source: Archiv der Pharmazie - December 11, 2017 Category: Drugs & Pharmacology Authors: Kalicharan Sharma, Apeksha Shrivastava, Ram N. Mehra, Girdhar S. Deora, Mohammad M. Alam, Mohammad S. Zaman, Mymoona Akhter Tags: FULL PAPER Source Type: research
Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti ‐tubercular agents
Design, synthesis, and biological screening of 2,2‐dimethyl‐2,3‐dihydrobenzofuran tethered 1,3,4‐oxadiazole derivatives as anti‐tubercular agents were described. The synthesis of the target compounds was conducted by a series of reaction schemes. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR, and mass spectrometry. The therapeutic potential of the synthesized compounds was confirmed by molecular docking studies. Among the synthesized compounds, 12a, 12c, 12d, 12e, 12g, and 12j were found to be more active against non‐replicating than against replicating cultures of Mycobacterium tuberc...
Source: Archiv der Pharmazie - December 1, 2017 Category: Drugs & Pharmacology Authors: Somnath Gholap, Macchindra Tambe, Laxman Nawale, Dhiman Sarkar, Jaiprakash Sangshetti, Manoj Damale Tags: FULL PAPER Source Type: research
Oxaprozin prodrug as safer nonsteroidal anti ‐inflammatory drug: Synthesis and pharmacological evaluation
Abstract
Oxaprozin is a popular non‐steroidal anti‐inflammatory drug (NSAID) and its chronic oral use is clinically restricted due to its gastrointestinal (GI) complications. In order to circumvent the GI complications, oxaprozin was amended as a prodrug in a one‐pot reaction using N,N‐carbonyldiimidazole as an activating agent. Dextran of average molecular weight (60,000–90,000 Da) was exploited as a carrier in the process of oxaprozin prodrug production by esterification. The structural profiles of the synthesized oxaprozin prodrug were characterized by FT‐IR and NMR spectroscopy. The oxaprozin prodrug poss...
Source: Archiv der Pharmazie - December 1, 2017 Category: Drugs & Pharmacology Authors: Jaya P. Peesa, Lakshmana R. Atmakuri, Prasanna R. Yalavarthi, Basaveswara R. Mandava Venkata, Arun Rasheed, Vengalrao Pachava Tags: FULL PAPER Source Type: research
Synthesis and elastase inhibition activities of novel aryl, substituted aryl, and heteroaryl oxime ester derivatives
Abstract
Fifteen novel aryl, substituted aryl and heteroaryl γ‐hydroxy‐ (2a–e), γ‐methoxyimino‐ (3a–e), and γ‐benzyloxyimino‐ (4a–e) butyric acid methyl esters were investigated for their enzyme inhibition, and the synthesis of 10 compounds (3a–e, 4a–e) is given in this study. The other five compounds (2a–e) were synthesized before in another study. Compounds 3a–e and 4a–e were synthesized in this work as original compounds and characterized by 1H and 13C NMR, IR, mass, and elemental analyses. Their (E/Z)‐isomerisation ratios were analyzed by 1H and 13C NMR. All of them are of pure (E)‐co...
Source: Archiv der Pharmazie - December 1, 2017 Category: Drugs & Pharmacology Authors: Belma Hasdemir, Ozlem Sacan, Hasniye Yasa, Hatice B. Kucuk, Ayse S. Yusufoglu, Refiye Yanardag Tags: FULL PAPER Source Type: research
