scholarly journals Microwave-Assisted Synthesis of Hydroxybenzylidene-Andrographolides and Its Inhibitory Activity against HIV-1 Protease

2018 ◽  
Keyword(s):  
Inhibitory Activity ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Hiv 1

4-Thiazolidinone derivatives as potent antimicrobial agents: microwave-assisted synthesis, biological evaluation and docking studies

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 319-326 ◽  
Author(s):  
Eleni Pitta ◽  
Evangelia Tsolaki ◽  
Athina Geronikaki ◽  
Jovana Petrović ◽  
Jasmina Glamočlija ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Activity ◽  
Antimicrobial Agents ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Hiv 1

A series of ten thiazolidin-4-one derivatives was synthesized and evaluated for their antibacterial, antifungal and HIV-1 reverse transcriptase (RT) inhibitory activity.

scholarly journals Design and Microwave Assisted Synthesis of Coumarin Derivatives as PDE Inhibitors

2016 ◽  
Vol 2016 ◽  
pp. 1-16 ◽  
Author(s):  
Mahadev N. Kumbar ◽  
Ravindra R. Kamble ◽  
Atulkumar A. Kamble ◽  
Sujith Raj Salian ◽  
Sandhya Kumari ◽  
...  
Keyword(s):  
Microwave Irradiation ◽  
Inhibitory Activity ◽  
Human Spermatozoa ◽  
Microwave Assisted Synthesis ◽  
Coumarin Derivatives ◽  
Motility Pattern ◽  
Microwave Assisted ◽  
Pde Inhibitors ◽  
Pde Inhibition ◽  
Potent Inhibitory Activity

Coumarins appended to benzimidazole through pyrazole are designed and synthesized using microwave irradiation. These compounds were analyzed for phosphodiesterase (PDE) inhibition indirectly by motility pattern in human spermatozoa. Some of the synthesized compounds, namely, 5d, 5e, 5f, 5g, 5h, and 5k, have exhibited potent inhibitory activity on PDE.

New chalcones and thiopyrimidine analogues derived from mefenamic acid: microwave-assisted synthesis, anti-HIV activity and cytotoxicity as antileukemic agents

2017 ◽  
Vol 72 (4) ◽  
pp. 249-256 ◽  
Author(s):  
Hanan A. Al-Hazam ◽  
Zeki A. Al-Shamkani ◽  
Najim A. Al-Masoudi ◽  
Bahjat A. Saeed ◽  
Christophe Pannecouque
Keyword(s):  
Mefenamic Acid ◽  
Leukemia Cells ◽  
Basic Medium ◽  
Microwave Assisted Synthesis ◽  
Schmidt Reaction ◽  
Microwave Assisted ◽  
Amide Derivatives ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

AbstractThe development of new HIV non-nucleoside reverse transcriptase inhibitors offers the possibility of generating structures of increased potency. To this end, coupling of mefenamic acid (4) with 4-amino-acetophenone (6) in the presence of dicyclohexylcarbodiimide and dimethylaminopyridine (DMAP) reagents afforded 4-(acetyphenyl)-2-((2,3-dimethylphenyl)amino)benzamide (7). Analogously, treatment of mefenamyl chloride (5) prepared from 4 with 6 under microwave irradiation (MWI) afforded 7. A new series of substituted chalconyl-incorporated amide derivatives of mefenamic acid 8–13 were synthesized from condensation of 7 with various substituted benzaldehydes via the Claisen–Schmidt reaction. Treatment of 8 and 11 with thiourea in a basic medium afforded the thiopyrimidine analogues 14 and 15, respectively. The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compounds 9 and 11 showed cytotoxicity values of 2.17 and 2.06 μm, respectively, against mock-infected MT-4 cells (C type adult T leukemia cells), which considered to be promising antileukemic agents.

scholarly journals Microwave-Assisted Synthesis of Fluoroquinolones and Their Nucleosides as Inhibitors of HIV Integrase

2006 ◽  
Vol 71 (7) ◽  
pp. 978-990 ◽  
Author(s):  
Martina M. Adams ◽  
Jan W. Bats ◽  
Nadja V. Nikolaus ◽  
Myriam Witvrouw ◽  
Zeger Debyser ◽  
...  
Keyword(s):  
Microwave Assisted Synthesis ◽  
Hiv Integrase ◽  
Inhibitory Effects ◽  
Microwave Assisted ◽  
Microwave Application ◽  
Anti Conformation ◽  
One Step ◽  
New Type ◽  
The One ◽  
Hiv 1

Six fluoroquinolone ribonucleosides were synthesized by using microwave irradiation starting from fluoroanilines. In most cases the microwave application proved superior in time and yield, especially the one step decarboxylation of the carboxyquinolone esters3a-3cand the Vorbrüggen glycosylation. The former led to the new type of fluoroquinolone ribosides8a-8c. Compound8cin the crystal structure showed C3'-endo and anti conformation. The nucleosides were examined, but found inactive against the replication of HIV-1(IIIB) in cell culture, while they were toxic for the cells at a 50% cytotoxic concentration ranging from 31 to >125 μg/ml. But measurements of the inhibitory effects against HIV-1 integrase enzymatic activity showed an interesting activity for compound8c.

Parallel Solution-Phase and Microwave-Assisted Synthesis of NewS-DABO Derivatives Endowed with Subnanomolar Anti-HIV-1 Activity

2005 ◽  
Vol 48 (25) ◽  
pp. 8000-8008 ◽  
Author(s):  
Fabrizio Manetti ◽  
José A. Esté ◽  
Imma Clotet-Codina ◽  
Mercedes Armand-Ugón ◽  
Giovanni Maga ◽  
...  
Keyword(s):  
Solution Phase ◽  
Microwave Assisted Synthesis ◽  
Parallel Solution ◽  
Microwave Assisted ◽  
Anti Hiv ◽  
Hiv 1

Synthesis and evaluation of novel heterocycles as potential HIV-1 enzyme inhibitors

2014 ◽  
Author(s):  
◽  
Gaëlle Tatiana Ngnie Tuemgnie
Keyword(s):  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Aldol Condensation ◽  
Click Reaction ◽  
Microwave Assisted Synthesis ◽  
Spectroscopic Techniques ◽  
Drug Molecules ◽  
Palladium Catalyzed ◽  
Dual Action ◽  
Hiv 1

This project has focussed on the synthesis and the evaluation of organic compounds as potential HIV-1 enzyme inhibitors, by making use of green chemistry (microwave assisted synthesis and click chemistry), palladium catalyzed reactions (Heck and Sonogashira coupling), Baylis Hillman methodology and aldol condensation. These compounds were synthesized in good yields and fully characterised by spectroscopic techniques. Biological assay data revealed that some of the compounds possess high inhibitory activity and their effective inhibitory concentration was as good as those of drugs in clinical use. These potential drug molecules were identified by preliminary investigations carried out by molecular modelling where a trend of their inhibitory activity against different enzymes was anticipated. Benzotriazole-AZT conjugates generated by 1,3-dipolar cycloaddition of anthranilic acid derivatives with AZT showed good inhibitory activity in silico against both HIV-1 protease (PR) and HIV-1 reverse transcriptase (RT) enzymes. Still in line with our dual action strategy, cinnamate ester-AZT conjugates were synthesized in three steps starting from benzaldehyde derivatives with a click reaction at the final step. These compounds also showed some inhibitory activity against HIV-1 RT enzyme (88%). In addition, the cinnamoyl fragment attached to AZT appeared to improve the activity of AZT against HIV-1 RT. Peptide chemistry involving carbonyl diimidazole as a coupling reagent between cinnamic acid derivatives and protected amino acids was used to prepare substituted amino acid derivatives which appeared to be very active against the integrase (IN) enzyme (88%). Commercially available coumarin was iodinated and derivatized through palladium catalyzed Heck and Sonogashira reactions with activated alkenes and a terminal alkyne respectively to afford novel coumarin derivatives in good yields. Optimization studies on the Heck reaction with regards to the phosphine ligand, the palladium catalyst and the solvent were carried out to afford novel formyl substituted cinnamate esters with nonaflyl salicylaldehyde derivatives.

An expeditious, environment-friendly, and microwave-assisted synthesis of 5-isatinylidenerhodanine derivatives

2011 ◽  
Vol 65 (3) ◽  
Author(s):  
Abdelmounaim Safer ◽  
Mustapha Rahmouni ◽  
François Carreaux ◽  
Ludovic Paquin ◽  
Olivier Lozach ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Microwave Assisted Synthesis ◽  
Environment Friendly ◽  
Microwave Assisted

AbstractA series of nine 5-arylidenerhodanine derivatives was prepared in good yields and purity without the use of a solvent or catalyst under microwave-assisted condensation with some substituted isatins. All 5-arylidenerhodanines were evaluated as possible inhibitors of the CK1α/β, CDK5/p25, and GSK-3α/β kinases. None of them showed substantive inhibitory activity against these kinases when evaluated at the concentration of 10 μM.

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