18199-97-8Relevant academic research and scientific papers
Synthesis, docking, and biological evaluation of thiazolidinone derivatives against hepatitis C virus genotype 4a
Al-Behery, Ahmed S.,Elberembally, Kamel M.,Eldawy, Mohammed A.
, p. 1151 - 1165 (2021/04/05)
Hepatitis C virus (HCV) genotype 4a (GT4a) is prevalent in Egypt. It did not gain the necessary scientific focus despite its high resistance. Since the crystal structure NS5B (RNA-dependent RNA polymerase) of HCV GT4a has not been resolved until now, homology modeling was conducted to build and validate the 3D model of the enzyme. Ligand binding sites including the allosteric thumb II pocket were detected and used in lead optimization. Sixty new 4-thiazolidinone derivatives have been virtually designed and docked into thumb II site of HCV NS5B GT4a using rigid docking approach. Eighteen compounds (7a–r) that show good docking scores were synthesized and tested in vitro against NS5B GT4a. Compounds 7b and 7n showed the best inhibitory activity (IC50 = 0.338 and 0.342 μM, respectively). Compounds 7a, 7b, 7c, 7d, 7k, 7n, 7q, and 7r that have IC50 values less than 2 μM were assessed for cellular anti-HCV GT4a activity using human hepatoma cell line (Huh 7.5). The percentages of viral growth inhibition are between 79.67 and 94.77%. Compound 7b is the most active in the in vitro and cellular assays and could be considered a potential new lead for future anti-HCV studies. [Figure not available: see fulltext.]
Synthesis and Biological Evaluation of Oxadiazole Clubbed Thiadiazole Derivatives as Antimicrobial Agents
Begari, Eeshwaraiah,Dave, Alpa Y.,Joshi, Deepkumar S.,Parmar, Kokila A.
, p. 273 - 280 (2021/08/03)
A series of 1,3,4-oxadiazole clubbed 1,3,4-thiadiazole derivatives were synthesized and assessed in vitro for their activity as antimicrobial agents. The target compounds 2-(5-(substituted aryl)-1, 3, 4-oxadiazol-2-ylthio)-N-(5-(substituted aryl)-1, 3, 4-thiadiazol-2-yl) acetamides (5a-5s) were synthesized using a basic condensation reaction between 5-(substituted aryl)-1,3,4-oxadiazole-2-thiol and 2-chloro-N-(5-(substituted aryl)-1,3,4-thiadiazol-2-yl)acetamide in presence of K2CO3 as a scavenging agent and acetone as reaction solvent. The titled compounds synthesized here, exhibited excellent to moderate antimicrobial activity against a broad panel of antibacterial strains of Gram-positive and Gram-negative bacteria and fungi.
Synthesis and evaluation of novel 1,3,4-thiadiazole–fluoroquinolone hybrids as antibacterial, antituberculosis, and anticancer agents
Demirci, Asl?,Karayel, Kaan G?k?e,Tatar, Esra,Okullu, Sinem ?KTEM,Unübol, Nihan,Ta?li, Pakize Neslihan,Kocag?z, Zühtü Tan?l,Sahin, Fikrettin,Kü?ükgüzel, Ilkay
, p. 839 - 858 (2018/06/07)
A series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16–25 were synthesized by reacting the correspondin
Novel 4-thiazolidinones as non-nucleoside inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase
akir, Gizem,Kücükgüzel, Ilkay,Guhamazumder, Rupa,Tatar, Esra,Manvar, Dinesh,Basu, Amartya,Patel, Bhargav A.,Zia, Javairia,Talele, Tanaji T.,Kaushik-Basu, Neerja
, p. 10 - 22 (2015/01/30)
In continuation of our efforts to develop new derivatives as hepatitis C virus (HCV) NS5B inhibitors, we synthesized novel 5-arylidene-4-thiazolidinones. The novel compounds 29-42, together with their synthetic precursors 22-28, were tested for HCV NS5B inhibitory activity; 12 of these compounds displayed IC50 values between 25.3 and 54.1 μM. Compound 33, an arylidene derivative, was found to be the most active compound in this series with an IC50 value of 25.3 μM. Molecular docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds.
Thiadiazole derivatives as potential anticonvulsant agents
Mullick, Pooja,Khan, Suroor A.,Verma, Surajpal,Alam, Ozair
, p. 1011 - 1016 (2012/01/03)
A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR,1HNMR,13C NMR and mass spectral data confir
Synthesis, characterization and antimicrobial activity of new thiadiazole derivatives
Mullick, Pooja,Khan, Suroor A.,Verma, Surajpal,Alam, Ozair
experimental part, p. 2345 - 2350 (2010/11/16)
A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data confirmed the
Synthesis of 2-(5-substituted-1,3,4-thiadiazolo-2-ylimino)-4- thiazolidinones under microwave irradiation
Wang, Xi-Cun,Huang, Guo-Li,Quan, Zheng-Jun,Lv, Cheng-Wei,Yang, Wen-Long
, p. 973 - 982 (2008/09/17)
Fifteen 2-(5-substituted-1,3,4-thiadiazolo-2-ylimino)-4-thiazolidinones were efficiently synthesized from the reaction of ammonium thiocyanate with 2-chloro-N-(5-substutited-1,3,4-thiadiazolo-2-yl)acetamides under microwave irradiation. The target compoun
