Design, synthesis and antimalarial evaluation of novel thiazole derivatives

2016 ◽  
Vol 26 (16) ◽  
pp. 3938-3944 ◽  
Author(s):  
José María Bueno ◽  
Miguel Carda ◽  
Benigno Crespo ◽  
Ana Carmen Cuñat ◽  
Cristina de Cozar ◽  
...  
Keyword(s):  
Thiazole Derivatives ◽  
Design Synthesis

Design, Synthesis and Pharmacological Evaluation of New Thiazole Derivatives as Anthelmintic Agents

2020 ◽  
Vol 13 (5) ◽  
pp. 5075-5081
Author(s):  
Sirisha Kalam ◽  
Sai Krishn G ◽  
Kumara Swamy D ◽  
Sai Santhoshi K ◽  
Durga Prasad K
Keyword(s):  
Anthelmintic Activity ◽  
Docking Studies ◽  
Molecular Property ◽  
Thiazole Derivatives ◽  
Pharmacological Agents ◽  
Design Synthesis ◽  
Standard Drug ◽  
Lipinski’S Rule ◽  
Mass Spectral ◽  
Tubulin Protein

Pharmacological agents that kills parasites are essential drugs in some tropical countries. In this study, a series of 2-amino substituted 4-phenyl thiazole derivatives (4a-e) have been synthesized by the conventional method. The thiazole derivatives were synthesized by three steps. The obtained five derivatives were purified by recrystallization using methanol as a solvent or column chromatography. They were characterized by melting point, TLC, FTIR, 1H NMR and MASS spectral data. Compounds 4a-e were evaluated in silico by using different software’s (Lipinski’s Rule of 5, OSIRIS molecular property explorer, Molsoft molecular property explorer, and PASS & docking studies). These compounds were then evaluated for their possible anthelmintic activity against Indian adult earth worms (Pherituma postuma). All the compounds displayed significant anthelmintic activity. Compound 4c and 4e were more potent compounds when compared with the standard drug (mebendazole). Molecular docking studies guided and proved the biological activity against beta tubulin protein (1OJ0). In conclusions, these new molecules have promising potential as anthelmintic for treatment of parasites.   

scholarly journals Design, synthesis and fungicidal activity of isothiazole–thiazole derivatives

RSC Advances ◽  
2018 ◽  
Vol 8 (69) ◽  
pp. 39593-39601 ◽  
Author(s):  
Qi-Fan Wu ◽  
Bin Zhao ◽  
Zhi-Jin Fan ◽  
Jia-Bao Zhao ◽  
Xiao-Feng Guo ◽  
...  
Keyword(s):  
Salicylic Acid ◽  
Systemic Acquired Resistance ◽  
Fungicidal Activity ◽  
Acquired Resistance ◽  
Thiazole Derivatives ◽  
Design Synthesis ◽  
Salicylic Acid Pathway ◽  
Acid Pathway

Compound 6u exhibits ultrahigh fungicidal activity by acting at its potent target PcORP1 and induces systemic acquired resistance by activating the salicylic acid pathway.

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.

scholarly journals Σχεδιασμός, σύνθεση και μελέτη βιολογικής δράσης θειαζολικών παραγώγων

2014 ◽  
Author(s):  
Κωνσταντίνος Λιάρας
Keyword(s):  
Wide Spectrum ◽  
Paw Edema ◽  
Thiazole Derivatives ◽  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Edema Model ◽  
Bacteria And Fungi ◽  
Cox 1

This thesis presents and discusses the design, synthesis and evaluation ofbiological activity of twenty-two (22) novel thiazole derivatives, twelve (12) of whichare chalcones, two (2) aminopyrimidines and eight (8), N-phenylpyrazolines.Prediction of biological activity spectra for all compounds was performed bythe program PASS.The aim was to design compounds that would combine antimicrobial and antiinflammatoryactivity, taking into account the wide spectrum of biological activitiesof thiazole derivatives, as well as, the interesting pharmacological properties ofchalcones, aminopyrimidines and N-phenylpyrazolines.The final compounds were identified by elemental analysis and spectroscopicmethods.Σheoritical calculations of several physicochemical parameters, includinglipophilicity, were performed for all final compounds.The evaluation of antimicrobial activity of the compounds against selected Gram(+) and Gram (-) bacteria and fungi was carried out in vitro using microdilution method.For a number of selected compounds, DNA gyrase inhibition assay was alsoperformed, in order to explain the possible mechanism of their antibacterial activity.The in vivo evaluation of anti-inflammatory activity of compounds was carriedout by use of carrageenin induced mouse paw edema model, while selected compoundswere also tested in vitro for their ability to inhibit cycloxygenase (COX 1 and 2).

Design, Synthesis and Fungicidal Activity of Novel 2‐aryl‐thiazole Derivatives Containing Saccharin Motif

2020 ◽  
Vol 5 (42) ◽  
pp. 13179-13182
Author(s):  
Danling Huang ◽  
Min Liao ◽  
Tianyuan Zhang ◽  
Shuyan You ◽  
Yun‐Feng Zhou ◽  
...  
Keyword(s):  
Fungicidal Activity ◽  
Thiazole Derivatives ◽  
Design Synthesis
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