82100-92-3

Upstream product

• 7275-22-1 1-acetylthiosemicarbazide 
• 403-29-2 2-bromo-4'-fluoroacetophenone 
• 79-19-6 thiosemicarbazide 
• 1629144-29-1 2-phenoxy-4-(4-fluorophenyl)thiazole 

Downstream Products

• 82100-85-4 2-(4'-carbethoxymethyl-3',5'-dimethyl-1'yl)-4-(p-fluorophenyl)thiazole 
• 82100-77-4 2-(3',5'-dimethyl-4'-ethylpyrazol-1'yl)-4-(p-fluorophenyl)thiazole 
• 402607-49-2 2-(2-(4-bromobenzylidene)hydrazinyl)-4-(4-fluorophenyl)thiazole 
• 364057-81-8 1-(4-methoxybenzylidene)-2-[4-(4-fluorophenyl)thiazol-2-yl]hydrazine 

Relevant academic research and scientific papers

Fluorine-containing compound and application thereof as antifungal drug

The invention discloses a fluorine-containing compound and application thereof as an antifungal drug. The invention claims to protect a compound as shown in a formula I or pharmaceutically acceptable salt, ester and solvate thereof. In the formula I, R is-NH2 or-N = C (CH3) 2. Compared with itraconazole, fluconazole and amphotericin B, the compound as shown in the formula I provided by the invention has a smaller MIC (Minimum Inhibitory Concentration) value, which shows that the compound has a more excellent antifungal effect.

Novel thiazole–pyrazolone hybrids as potent ACE inhibitors and their cardioprotective effect on isoproterenol-induced myocardial infarction

A facile synthesis of a group of novel thiazole–pyrazolone hybrids and their investigation for angiotensin-converting enzyme (ACE) inhibition are reported in this study. These compounds were synthesized using a well-known approach, based on the condensation of ethyl acetoacetate with thiazolylhydrazines, and characterized by various spectroscopic and analytical techniques. The entire set of compounds displayed a moderate-to-excellent inhibitory activity against ACE. In particular, compound 4i was found to be the most potent ACE inhibitor and was further studied for cardioprotective effects against isoproterenol (ISO)-induced myocardial infarction (MI) in rats. Compound 4i improved the cardiac function and prevented cardiac injury induced by ISO in Sprague Dawley rats. The levels of oxidative stress and proinflammatory cytokines were also restored to near normal by 4i as compared with the ISO group. In the Western blot analysis, compound 4i prevented mitochondrial apoptosis after MI by downregulating the expression of cleaved caspase-3 and Bax, with the upregulation of Bcl-2, as compared with the ISO group.

2,4- and 2,5-disubstituted arylthiazoles: Rapid synthesis by C-H coupling and biological evaluation

Life-threatening infections caused by bacteria that have developed resistance to common antibiotics, such as methicillin-resistant Staphylococcus aureus (MRSA), have become a serious problem in hospitals and other areas all over the world. Thus, the development of an effective class of antibiotics against these bacteria is an urgent subject. Herein, we report a step-economical and diversity-oriented synthesis of a series of 2-arylidenehydrazinyl-4- arylthiazole and 2-arylidenehydrazinyl-5-arylthiazole analogues that utilizes C-H coupling methodologies. A library of 54 new congeners were synthesized and tested for their biological potential. Moreover, new knowledge regarding the structure-activity relationships (SARs) of these heterobiaryl compounds was collected. Copyright

Synthesis and Mass Spectral Studies of Some 2-(3',5'-Dimethylpyrazol-1'-yl)-4-arylthiazoles and Their 4'-Alkyl/Carboxymethyl Analogues

A number of 2-(3',5'-dimethylpyrazol-1'-yl)-4-arylthiazoles (IIa, d, g, j) and their 4'-alkyl (IIb, c, e, f, h, i, k, l) and 4'-carbethoxymethyl (III) analogues have been synthesized by the condensation of appropriate 2-hydrazino-4-arylthiazoles (I) with pentane-2,4-dione and its 3-substituted analogues.Alkaline hydrolysis of III gives the corresponding acids (IVa-d).The mass spectral studies reveal that the major fragmentation of II involves decomposition of pyrazole ring with the expulsion of methyl cyanide, fission of thiazole ring and the loss of methyl groupfrom the molecular ion.These and the other competing processes which involve skeletal rearrangement in the pyrazole moiety have been supported by the high resolution measurements.Presence of ethoxycarbonyl (III) or a carboxy function (IV), however, triggers an alternative low-energy pathway involving the preferential expulsion of these groups from the molecular ion prior to the decomposition of either of the heterocyclic moieties.The compounds have been screened for their antiinflammatory activity.