71173-46-1Relevant articles and documents
Synthesis and Antimicrobial Activity of New Thiazolidine-Based Heterocycles as Rhodanine Analogues
Abdel Hafez, Naglaa A.,Elsayed, Mohamed A.,El-Shahawi, Manal M.,Awad, Ghada E. A.,Ali, Korany A.
, p. 685 - 691 (2018)
A new series of compounds containing thiazole nucleus as Rhodanine analogues have been synthesized. The new compounds were prepared from the reactions of the thiosemicarbazones (3a,b) with a series of α-halo carbonyl compounds to give the corresponding Rh
Design, eco-friendly synthesis, molecular modeling and anticancer evaluation of thiazol-5(4: H)-ones as potential tubulin polymerization inhibitors targeting the colchicine binding site
El-Naggar, Abeer M.,Eissa, Ibrahim H.,Belal, Amany,El-Sayed, Amira A.
, p. 2791 - 2811 (2020)
In recent years, suppressing tubulin polymerization has been developed as a therapeutic approach for cancer treatment. Thus, new derivatives based on thiazol-5(4H)-ones have been designed and synthesized in an eco-friendly manner. The synthesized derivati
Eco-friendly sequential one-pot synthesis, molecular docking, and anticancer evaluation of arylidene-hydrazinyl-thiazole derivatives as CDK2 inhibitors
El-Naggar, Abeer M.,El-Hashash, Maher A.,Elkaeed, Eslam B.
, (2021/02/05)
One current approach in the treatment of cancer is the inhibition of cyclin dependent kinase (CDK) enzymes with small molecules. CDK are a class of enzymes, which catalyze the transfer of the terminal phosphate of a molecule of ATP to a protein that acts
Structural improvement of new thiazolidinones compounds with antinociceptive activity in experimental chemotherapy-induced painful neuropathy
Moreira, Diogo Rodrigo Magalhaes,Santos, Dourivaldo Silva,Espírito Santo, Renan Fernandes do,Santos, Flávia Evangelista dos,de Oliveira Filho, Gevanio Bezerra,Leite, Ana Cristina Lima,Soares, Milena Botelho Pereira,Villarreal, Cristiane Flora
, p. 297 - 307 (2017/07/13)
Chemotherapy-induced neuropathy is a disabling pain condition resulting from chemotherapy for cancers. Up to now, no drug is available to cure chemotherapy-induced neuropathy. In the present study, we describe the structural design, synthesis, chemical and pharmacological characterization of 15 thiazolidinones, a class of potential analgesic compounds. The synthesis of new thiazolidinones was achieved by using the thiazolidinone heterocyclic as main structural pharmacophoric group and varying the substituents attached to the phenyl near to the iminic bond. The analgesic potential of the compounds was investigated in a mice model of oxaliplatin-induced neuropathic pain, using von Frey, rota-rod and open-field tests. Except for compound 14, these thiazolidinones exhibited antinociceptive property without causing motor impairment. Thiazolidinones 12, 15 and 16 displayed a dose-dependent antinociceptive effect, with similar efficacy and enhanced potency than gabapentin, the gold standard drug used for neuropathic pain. In addition, the antinociceptive activity of 16 lasted longer than gabapentin. The antinociceptive effect of thiazolidinones was prevented by GW9662, a PPARγ antagonist. The main antinociceptive compounds exhibited positive Lipinski's index, predicting their oral bioavailability. In conclusion, the structural design performed here led to the identification of new compounds endowed with potent antinociceptive activity, potentially useful to treat chemotherapy-induced neuropathic pain.
Synthesis and evaluation of biological activities of 4-cyclopropyl-5-(2-fluorophenyl) arylhydrazono-2,3-dihydrothiazoles as potent antioxidant agents
Ghanbari Pirbasti,Mahmoodi, Nosrat O.,Abbasi Shiran, Jafar
, p. 196 - 210 (2016/03/25)
A new series of 4-cyclopropyl-5-(2-fluorophenyl)arylhydrazono-2,3-dihydrothiazole derivatives was synthesized via the reaction of prepared thiosemicarbazones with 2-bromo-1-cyclopropyl-2-(2-uorophenyl)ethanone in the presence of Et3 N as a catalyst throug
Structure-activity relationship study of thiosemicarbazones on an African trypanosome: Trypanosoma brucei brucei
Fatondji, Houssou Raymond,Kpoviessi, Salome,Gbaguidi, Fernand,Bero, Joanne,Hannaert, Veronique,Quetin-Leclercq, Joelle,Poupaert, Jacques,Moudachirou, Mansourou,Accrombessi, Georges Coffi
, p. 2151 - 2162 (2013/07/26)
To explore the structure-activity relationships of thiosemicarbazones on African trypanosome: Trypanosoma brucei brucei, a series of thirty-five thiosemicarbazones (1-35) have been synthesized and characterized by their 1H NMR, 13C NMR, and FT-IR spectra. All compounds were tested for trypanocidal activity using the method "Lilit alamar blue". The comparison of trypanocidal power of thiosemicarbazones was performed considering their structures. This study that was done using acetophenone thiosemicarbazone (1) as basic model, showed that: (a) the presence of lipophilic substituents in para position on benzene ring, (b) substitution of benzene ring and (c) substitution of hydrogen of thioamide function by a phenyl, strongly influence trypanocidal activity. The various modifications to basic structure (1) allowed the synthesis of 1-(4-chlorophenyl) ethylidene-4-phenyl- thiosemicarbazide (34). With a trypanocidal activity of 3.97 μM, this compound is the most active of the series.
A new type of synthesis of 1,2,3- Thiadiazole and 1,2,3-diazaphosphole derivatives via-hurd-mori cyclization
Hosny, Mona A.,El-Sayed, Taghreed H.,El-Sawi, Emtithal A.
experimental part, p. 1276 - 1287 (2012/06/01)
We present a short and efficient synthesis of the title compounds starting with cheap and readily available camphor and derivatives of acetophenone. The optimized sequence allows the large-scale preparation of this new type of synthesis in a few steps. Ne
