2107-15-5

Upstream product

• 1240952-24-2 2,4-bis(3-fluorophenyl)-3-azabicyclo[3.3.1]nonan-9-one 
• 79-19-6 thiosemicarbazide 
• 456-48-4 3-Fluorobenzaldehyde 

Downstream Products

• 461686-66-8 2-(2-(3-fluorobenzylidene)hydrazinyl)thiazol-4(5H)-one 
• 467246-13-5 C₂₀H₁₄FN₃S 
• 127066-01-7 Cu⁽¹⁺⁾*C₈H₇FN₃S^(1-)={Cu(C₆H₄FCHNNCSNH₂)} 
• 276254-76-3 5-(3-fluoro-phenyl)-[1,3,4]thiadiazole-2-thiol 
• 276254-78-5 2-(3-fluoro-phenyl)-5-methylsulfanyl-[1,3,4]thiadiazole 
• 91660-20-7 2-Chloro-5-(3-fluoro-phenyl)-[1,3,4]thiadiazole 
• 59565-52-5 5-(3-fluorophenyl)-1,3,4-thiadiazol-2-amine 

Relevant academic research and scientific papers

Synthesis and anticonvulsant activity of 5-aryl-1,3,4-thiadiazole derivatives

5-Aryl-1,3,4-thiadiazole derivatives were synthesized and tested for anticonvulsant activity using the pentylenetetrazole-induced lethal convulsion test. The results showed that 2-amino derivatives have anticonvulsant activity (LD50 > 500 mg kg-1) and this effect was not mediated through benzodiazepine receptors. The fluoro electron-withdrawing substituent on the phenyl ring did not potentiate the activity of the compounds.

Assessment of Thiosemicarbazone-Containing Compounds as Potential Antileukemia Agents against P-gp Overexpressing Drug Resistant K562/A02 Cells

P-Glycoprotein (P-gp) overexpression is considered to be the leading cause of multidrug resistance (MDR) and failure of chemotherapy for leukemia. In this study, seventeen thiosemicarbazone-containing compounds were prepared and evaluated as potential ant

Synthesis, antimicrobial and antioxidant evaluation with in silico studies of new thiazole Schiff base derivatives

A series of nineteen thiazole Schiff base derivatives 2a-2s were synthesized (Scheme 1) and elucidated by spectral analyses (IR, 1H NMR and HRMS). The evaluation of their antimicrobial activities against two gram-positive, two gram-negative, an

2 - (2 - Animal pen asia jingjing base) -5 - acyl thiazole and its medical use (by machine translation)

The invention formula I shown by 2 - (2 - animal pen asia jingjing base) - 5 - acyl thiazole and its pharmaceutically acceptable salt, pharmaceutical composition and thereof in the preparation of influenza virus neuraminidase inhibitors in the application. Wherein R is selected from: methyl, ethyl, C3 - C4 Straight-chain or C3 - C4 Branched alkyl; R1 Is selected from: hydrogen, C1 - C2 Alkyl, C3 - C4 Straight-chain or C3 - C4 Branched alkyl, fluoromethyl, difluoromethyl, trifluoromethyl, bromomethyl, [...], three bromine methyl, chloromethyl, dichloro methyl or trichloromethyl; X1 , X5 Is selected from: hydrogen, deuterium, C1 - C2 Alkyl, hydroxy, methoxy, ethoxy, fluoro, chloro, bromo, iodo, nitro, amino, methylamino, dimethylamino, acetyl, carboxy, methoxycarbonyl or ethoxycarbonyl; X2 , X4 Is selected from: hydrogen, deuterium, C1 - C2 Alkyl, C3 - C4 Straight or branched chain alkyl, hydroxy, methoxy, ethoxy, fluoro, chloro, bromo, iodo, nitro, amino, methylamino, dimethylamino, acetyl, carboxy, methoxycarbonyl or ethoxycarbonyl; X3 Is selected from: hydrogen, deuterium, C1 - C2 Alkyl, hydroxy, methoxy, ethoxy, fluoro, chloro, bromo, iodo, nitro, amino, methylamino, dimethylamino, acetyl, carboxy, methoxycarbonyl or ethoxycarbonyl. (by machine translation)

Synthesis and antifungal activities of drimane-amide derivatives from sclareol

Aim and Objective: Plant diseases are caused by fungal pathogens lead to severe economic losses in many agriculture crops. And the increasing resistance of many fungi to commonly used antifungal agents necessitates the discovery and development of new fungicides. So this study was focused on synthesizing novel skeleton compounds to effectively control plant diseases. Materials and Methods: A series of drimane-amide derivatives were designed, synthesized by aminolysis reaction of amine with intermediate sclareolide which was prepared from sclareol. The structures of all the synthesized compounds were confirmed using1H NMR,13C NMR, and HR-MS (ESI) spectroscopic data. Their in vitro antifungal activity were preliminarily evaluated by using the mycelium growth rate method against five phytopathogenic fungi: Botrytis cinerea, Glomerella cingulata, Alternaria alternate, Alternaria brassicae, and Fusarium graminearum. Results: 23 target compounds were successfully obtained in yields of 52-95%. Compounds358 A2 and A3 displayed favorable inhibitory potency against B. cinerea, G. cingulata and A. brassicae with IC50 values ranging from 3.18 to 10.48 μg/mL. These two compounds displayed higher fungicidal activity than sclareol against all the tested phytopathogenic fungi, and were more effective than the positive control thiabendazole against A. alternate and A. brassicae. The structure-activity relationship studies of compounds A1-10 indicated that both the position and type of substituent on the phenyl ring had significant effects on antifungal activity. Conclusion: The drimane-amide derivatives A2 and A3 were the most promising derivatives and should be selected as new templates for the potential antifungal agents.

Novel 4-thiazolidinones as non-nucleoside inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase

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.

Refinement of arylthiosemicarbazone pharmacophore in inhibition of mushroom tyrosinase

Melanin play a major role in human skin protection and their biosynthesis is vital. Due to their color, they contribute to the skin pigmentation. Tyrosinase is a key enzyme involved in the first stage of melanin biosynthesis, it catalyzes the transformation of tyrosine into l-dopaquinone. The aim of the present study was to study molecules able to inhibit tyrosinase to be used in treating depigmentation-related disorders. In this study, we targeted arylthiosemicarbazone analogs with the aim to contribute to the identification of the optimal aryl ring to be linked to the thiosemicarbazone moiety. The biological activity was evaluated on commercial mushroom tyrosinase which was purified prior use. The results demonstrated that several of our compounds (1a-h, 1j, 1r and 5) had more potent inhibitory activities than kojic acid which was used as the reference inhibitor.

Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors

Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene)hydrazinyl)thiazol-4(5H)-one (12) displayed the most potent inhibitory activity (IC50 = 0.09 μM for EGFR and IC50 = 0.42 μM for HER-2), comparable to the positive control erlotinib. Docking simulation was performed to position compound 12 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the thiazolidinone derivatives own high antiproliferative activity against MCF-7. Compound 12 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.

Design, synthesis and biological evaluation of novel 2-[(2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazono]-1,3-thiazolidin-4-ones as a new class of antimicrobial agents

New series of 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-one thiosemicarbazones (9-16) obtained from the corresponding 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones (1-8) upon cyclization with ethylbromoacetate in the presence of sodium acetate-acetic acid buffer afforded novel 2-[(2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazono]-1,3-thiazolidin-4-ones (17-24). The synthesized compounds have been characterized by their elemental, analytical and spectral studies. Besides, the reported compounds were screened for their antibacterial and antifungal activities against a spectrum of microbial organisms. These studies proved that compounds 11/18/20/23 against Staphylococcus aureus, 19/20/24 against Salmonella typhi show maximum inhibition potency at low concentration (6.25 μg/ml) whereas 18/19 against Candida albicans and 19/20/21 against Rhizopus sp. showed beneficial antifungal activity at minimum concentration.