Design, synthesis, SAR study, and biological investigation of novel N-substituted benzamide enaminones as potential anticonvulsant agents

2020 ◽  
Author(s):  
Patrice Ayotunde ◽  
Yayin Fang ◽  
Isis J Amaye ◽  
Miguel Martin
Keyword(s):  
Biological Investigation ◽  
Design Synthesis ◽  
Anticonvulsant Agents ◽  
Substituted Benzamide ◽  
Sar Study

Design, Synthesis, and Biological Investigation of Thailanstatin A and Spliceostatin D Analogues Containing Tetrahydropyran, Tetrahydrooxazine, and Fluorinated Structural Motifs

2021 ◽  
Vol 86 (3) ◽  
pp. 2499-2521
Author(s):  
K. C. Nicolaou ◽  
Santhosh Reddy Rekula ◽  
S. Mothish Kumar ◽  
Ananda Rao Podilapu ◽  
Ryan P. Matuszak ◽  
...  
Keyword(s):  
Biological Investigation ◽  
Structural Motifs ◽  
Design Synthesis

scholarly journals Novel Acetohydrazide Pyrazole Derivatives: Design, Synthesis, Characterization and Antimicrobial Activity

2019 ◽  
Vol 31 (12) ◽  
pp. 2740-2744
Author(s):  
Anil Verma ◽  
Vinod Kumar ◽  
Ramesh Kataria ◽  
Joginder Singh
Keyword(s):  
Mass Spectrometry ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
Structure Activity ◽  
Electron Withdrawing Group ◽  
Sar Study

Eleven acetohydrazide linked pyrazole derivatives were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. 6b, 6c and 6d were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives as compared to other groups present in the ring. Hence, among compounds 6b-c, compound 6d could be explored further against other microbes to prove its vitality.

Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents

2013 ◽  
Vol 22 (12) ◽  
pp. 5823-5831 ◽  
Author(s):  
Mohamed F. Zayed ◽  
Hany E. A. Ahmed ◽  
Abdel-Sattar M. Omar ◽  
Adel S. Abdelrahim ◽  
Khaled El-Adl
Keyword(s):  
Evaluation Studies ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Anticonvulsant Agents ◽  
Quinazolinone Derivatives ◽  
Synthesis And Biological Evaluation

scholarly journals Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents

2016 ◽  
Vol 112 ◽  
pp. 91-98 ◽  
Author(s):  
Maryam Mohammadi-Khanaposhtani ◽  
Mohammad Shabani ◽  
Mehrdad Faizi ◽  
Iraj Aghaei ◽  
Reza Jahani ◽  
...  
Keyword(s):  
Docking Study ◽  
Design Synthesis ◽  
Anticonvulsant Agents ◽  
Pharmacological Evaluation

Design, synthesis and biological evaluation of novel thiosemicarbazide analogues as potent anticonvulsant agents

2014 ◽  
Vol 54 ◽  
pp. 68-72 ◽  
Author(s):  
Reshma J. Nevagi ◽  
Avinash S. Dhake ◽  
Harsha I. Narkhede ◽  
Prabhjeet Kaur
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Anticonvulsant Agents ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists

Molecules ◽  
2014 ◽  
Vol 19 (3) ◽  
pp. 3539-3551 ◽  
Author(s):  
Libao Xu ◽  
Yang Zhang ◽  
Wenjie Dai ◽  
Ying Wang ◽  
Dan Jiang ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Amide Derivatives ◽  
Sar Study

Design, Synthesis and biological evaluation of diazeno-thiazole derivatives as ribonucleotide reductase inhibitors

2017 ◽  
Vol 4 (2) ◽  
pp. 20-24 ◽  
Author(s):  
Mohd Usman Mohd Siddique ◽  
Surender Singh Jadav ◽  
Geraldine Graser ◽  
Philipp Saiko ◽  
Thomas Szekeres ◽  
...  
Keyword(s):  
Dna Synthesis ◽  
Ribonucleotide Reductase ◽  
Biological Evaluation ◽  
Thiazole Derivatives ◽  
Design Synthesis ◽  
Reductase Inhibitors ◽  
Good Target ◽  
Cell Synthesis ◽  
Ribonucleotide Reductase Inhibitors ◽  
Sar Study

Ribonucleotide reductase(RNR) is a metalloenzyme that catalyses the rate limiting step in DNA synthesis and repair. It causes the reduction of ribonucleotide to 2’-deoxyribonuclotides which are used as precursors for DNA synthesis, thus offering a good target for inhibition of cell synthesis. Experimental results have been proven that RNR inhibitors can be used as antiviral, anticancer or antibacterial agents. Here we report the synthesis of a novel class of diazeno-thiazole derivatives as potent RNR inhibitors. A series of forty molecules were synthesized and evaluated for their RNR inhibitory properties. All compounds were found to be good inhibitors of the RNR. Compound 3iwas found to be most active showing an IC50 value of 0.8 µm. The established SAR study indicated the presence of a polar bridge with an adjacent flexible aromatic ringprerequisite for RNR inhibitory activity. Moreover, compounds having an additional 4-chloro phenyl ring were found to be most potent.

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