scholarly journals Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors

2010 ◽  
Vol 26 (4) ◽  
pp. 506-513 ◽  
Author(s):  
Yu Liu ◽  
Lei Zhang ◽  
Jianzhi Gong ◽  
Hao Fang ◽  
Ailin Liu ◽  
...  
Keyword(s):  
Biological Activity ◽  
Neuraminidase Inhibitors ◽  
Thiazole Derivatives ◽  
Design Synthesis

Design, synthesis and biological activity of thiazolidine-4-carboxylic acid derivatives as novel influenza neuraminidase inhibitors

2011 ◽  
Vol 19 (7) ◽  
pp. 2342-2348 ◽  
Author(s):  
Yu Liu ◽  
Fanbo Jing ◽  
Yingying Xu ◽  
Yuanchao Xie ◽  
Fangyuan Shi ◽  
...  
Keyword(s):  
Biological Activity ◽  
Carboxylic Acid ◽  
Neuraminidase Inhibitors ◽  
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.   

Design, Synthesis and Biological Activity of Aromatic Diketone Derivatives as HIV-1 Integrase Inhibitors

2015 ◽  
Vol 11 (2) ◽  
pp. 180-187 ◽  
Author(s):  
Liming Hu ◽  
Zhipeng Li ◽  
Zhanyang Wang ◽  
Gengxin Liu ◽  
Xianzhuo He ◽  
...  
Keyword(s):  
Biological Activity ◽  
Integrase Inhibitors ◽  
Design Synthesis ◽  
Hiv 1

Biological Activity of Thiazole Derivatives on Some Pathogenic Microorganisms

2011 ◽  
Vol 14 (1) ◽  
pp. 1-6
Author(s):  
Firas A. Hassan ◽  
◽  
Zahraa. S. Saeed ◽  
Shayma M. Ahmad ◽  
◽  
...  
Keyword(s):  
Biological Activity ◽  
Pathogenic Microorganisms ◽  
Thiazole Derivatives

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

1-Methyl-3H-pyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones. Design, Synthesis, and Biological Activity of New Antitumor Agents

2005 ◽  
Vol 48 (8) ◽  
pp. 2859-2866 ◽  
Author(s):  
Anna Maria Almerico ◽  
Francesco Mingoia ◽  
Patrizia Diana ◽  
Paola Barraja ◽  
Antonino Lauria ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis

scholarly journals Design, Synthesis, and Biological Activity of Sulfonamide Analogues of Antofine and Cryptopleurine as Potent and Orally Active Antitumor Agents

2015 ◽  
Vol 58 (19) ◽  
pp. 7749-7762 ◽  
Author(s):  
Yongseok Kwon ◽  
Jayoung Song ◽  
Honggu Lee ◽  
Eun-Yeong Kim ◽  
Kiho Lee ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis ◽  
Orally Active

Design, synthesis, and biological activity of anti-angiogenic hypoxic cell radiosensitizer haloacetylcarbamoyl-2-nitroimidazoles

1997 ◽  
Vol 5 (3) ◽  
pp. 591-599 ◽  
Author(s):  
Hitoshi Hori ◽  
Cheng-Zhe Jin ◽  
Masatoshi Kiyono ◽  
Soko Kasai ◽  
Mariko Shimamura ◽  
...  
Keyword(s):  
Biological Activity ◽  
Hypoxic Cell ◽  
Design Synthesis
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