150059-52-2

Upstream product

• 99-91-2 para-chloroacetophenone 
• 79-19-6 thiosemicarbazide 

Downstream Products

• 78583-81-0 3-(4-chlorophenyl)-1H-pyrazol-5-amine 

Relevant academic research and scientific papers

Structural improvement of new thiazolidinones compounds with antinociceptive activity in experimental chemotherapy-induced painful neuropathy

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.

Crystallographic, experimental (FT-IR and FT-RS) and theoretical (DFT) investigation, UV-Vis, MEP, HOMO-LUMO and NBO/NLMO of (E)-1-[1-(4-Chlorophenyl) ethylidene]thiosemicarbazide

Crystallographic, experimental (FT-IR and FT-RS) and theoretical density function theory (DFT) and UV-Vis spectra of (E)-1-[1-(4-Chlorophenyl)ethylidene] thiosemicarbazide) (ECET) are investigated. The optimized geometry of the compound was calculated fro

Halogenated aromatic thiosemicarbazones as potent inhibitors of tyrosinase and melanogenesis

A set of 21 halogenated thiosemicarbazones (TSCs) have been synthesized and its inhibitory properties toward activity diphenolase of mushroom tyrosinase and their ability to inhibition of melanogenesis in B16F10 murine, melanoma cell line have been invest

Synthesis and antimicrobial activity of novel thiazole substituted pyrazole derivatives

A series of new 1-[4-(2,3,4-substituted-phenyl) thiazol-2-yl]-3-(2,3,4- substituted-phenyl)-1H-pyrazole-4-carbaldehyde (4a-m), 4-[4-(4-substituted- phenyl) thiazol-2-yl]-3-(4-substituted-phenyl)-1-phenyl-1H-pyrazole (7a-i), 4-[4-(4-substituted phenyl)thiazol-2-yl]-1-phenyl-1H-pyrazol-3-amine (10a-g) have been synthesized by using Vilsmeier Haack formylation and Hantzsch reaction in high yield. All the synthesized compounds were tested qualitative (Zone of inhibition) and quantitative antimicrobial activities (MIC). Most of the synthesized compounds showed potent antimicrobial activity against gram positive and gram negative bacteria as well as fungi species.

Synthesis of aryl-hydrazones via ultrasound irradiation in aqueous medium

The synthesis of aryl-hydrazones from aromatic aldehydes/ketones and hydrazides (semicarbazide, thiosemicarbazide and aminoguanidine) is described using aqueous medium (acid conditions) under ultrasound irradiation with short reaction times (20-30 min), t

Synthesis and antituberculosis activity of new thiazolylhydrazone derivatives

The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new thiazolylhydrazone derivatives were synthesized and