Synthesis and Biological Evaluation of Some New 2,5-Substituted 1-Ethyl-1H-benzoimidazole Fluorinated Derivatives as Direct Thrombin Inhibitors

2015 ◽  
Vol 348 (5) ◽  
pp. 353-365 ◽  
Author(s):  
Meilin Li ◽  
Yujie Ren
Keyword(s):  
Biological Evaluation ◽  
Thrombin Inhibitors ◽  
Direct Thrombin Inhibitors ◽  
Fluorinated Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

Synthesis and Biological Evaluation of Direct Thrombin Inhibitors Bearing 4-(Piperidin-1-yl)pyridine at the P1 Position with Potent Anticoagulant Activity

2013 ◽  
Vol 56 (21) ◽  
pp. 8696-8711 ◽  
Author(s):  
Modesto de Candia ◽  
Filomena Fiorella ◽  
Gianfranco Lopopolo ◽  
Andrea Carotti ◽  
Maria Rosaria Romano ◽  
...  
Keyword(s):  
Anticoagulant Activity ◽  
Biological Evaluation ◽  
Thrombin Inhibitors ◽  
Direct Thrombin Inhibitors ◽  
Synthesis And Biological Evaluation

Facile Synthesis and Biological Evaluation of Cyclopropyl-Pyrazole Hybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents

2019 ◽  
Vol 4 (3) ◽  
pp. 152-158
Author(s):  
P.C. Burde ◽  
A.M. Rahatgaonkar
Keyword(s):  
Ionic Liquid ◽  
Ambient Temperature ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Biphasic System ◽  
Facile Synthesis ◽  
Convenient Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are immiscible, has been easily recycled and reused after separation of the products without any noticeable diminution in its activity.

scholarly journals Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-N-substituted-hydrazinecarbothioamides

2012 ◽  
Vol 22 (4) ◽  
pp. 2014-2022 ◽  
Author(s):  
Subhas S. Karki ◽  
Amol A. Kulkarni ◽  
Sujeet Kumar ◽  
Suresh Kumar Veliyath ◽  
Erik De Clercq ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL THIAZOLE-PYRAZOLE INTEGRATED CHALCONES AS ANTIOXIDANT AND ANTI-INFLAMMATORY AGENTS

2019 ◽  
pp. 311-315
Author(s):  
DNYANESHWAR SIRSAT ◽  
PRADEEP KATE ◽  
MADHUSUDAN BACHUTE
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
Schmidt Reaction ◽  
Chemical Structures ◽  
1H Nuclear Magnetic Resonance ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

Objective: The objective of the present study was to synthesize the thiazole-pyrazole integrated chalcones and their in vitro antioxidant and anti- inflammatory evaluation. Methods: The designed hybrid thiazole-pyrazole integrated chalcones (3a-j) were synthesized by Claisen–Schmidt reaction of substituted 1-(4-methyl-2-phenylthiazol-5-yl) ethanone and substituted pyrazole aldehyde in the presence of 10% NaOH in ethanol solvent under reflux condition. The chemical structures of synthesized compounds were confirmed by IR, 1H nuclear magnetic resonance (NMR), 13C NMR, and high- resolution mass spectra. Results: All the title compounds were screened for their in vitro antioxidant and anti-inflammatory activity. The screening data indicated that tested compounds showed potent antioxidant activity with moderate anti-inflammatory potential. Conclusion: Antioxidant screening data reveal that most of the synthesized compounds possess excellent 1,1-diphenyl-2-picrylhydrazyl and NO radical scavenging activity. Most of the compounds found to possess marked anti-inflammatory potential by effectively inhibiting the heat-induced albumin denaturation.

Synthesis and Biological Evaluation of 2, 3-Diaryl substituted-1, 3-thiazolidin-4-ones as Anti-HIV Agents

2007 ◽  
Vol 3 (4) ◽  
pp. 355-363 ◽  
Author(s):  
Ravindra K. Rawal ◽  
Raj Kamal Tripathi ◽  
S.B. Katti ◽  
Christophe Pannecouque ◽  
Erik De Clercq
Keyword(s):  
Biological Evaluation ◽  
Anti Hiv Agents ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1 ◽  
Anti Hiv

scholarly journals Synthesis and Evaluation of Spumigin Analogues Library with Thrombin Inhibitory Activity

Marine Drugs ◽  
2018 ◽  
Vol 16 (11) ◽  
pp. 413 ◽  
Author(s):  
Aleš Žula ◽  
Izabela Będziak ◽  
Danijel Kikelj ◽  
Janez Ilaš
Keyword(s):  
Inhibitory Activity ◽  
Serine Proteases ◽  
Biological Effects ◽  
Factor Xa ◽  
Structural Type ◽  
Biological Evaluation ◽  
Central Core ◽  
Thrombin Inhibitors ◽  
Direct Thrombin Inhibitors ◽  
Lead Compounds

Spumigins are marine natural products derived from cyanobacteria Nodularia spumigena, which mimics the structure of the d-Phe-Pro-Arg sequence and is crucial for binding to the active site of serine proteases thrombin and factor Xa. Biological evaluation of spumigins showed that spumigins with a (2S,4S)-4-methylproline central core represent potential lead compounds for the development of a new structural type of direct thrombin inhibitors. Herein, we represent synthesis and thrombin inhibitory activity of a focused library of spumigins analogues with indoline ring or l-proline as a central core. Novel compounds show additional insight into the structure and biological effects of spumigins. The most active analogue was found to be a derivative containing l-proline central core with low micromolar thrombin inhibitory activity.

ChemInform Abstract: Synthesis and Biological Evaluation of Some 4-Substituted 1-[1-(4-Hydroxybutyl)-1,2,3-triazol-(4 and 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.

ChemInform ◽  
2010 ◽  
Vol 33 (9) ◽  
pp. no-no
Author(s):  
O. Moukha-Chafiq ◽  
M. L. Taha ◽  
H. B. Lazrek ◽  
J. J. Vasseur ◽  
C. Pannecouque ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

Statistical Molecular Design, Parallel Synthesis, and Biological Evaluation of a Library of Thrombin Inhibitors

2001 ◽  
Vol 44 (21) ◽  
pp. 3424-3439 ◽  
Author(s):  
Anna Linusson ◽  
Johan Gottfries ◽  
Thomas Olsson ◽  
Eivor Örnskov ◽  
Staffan Folestad ◽  
...  
Keyword(s):  
Molecular Design ◽  
Biological Evaluation ◽  
Parallel Synthesis ◽  
Thrombin Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Statistical Molecular Design
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