797053-22-6

Upstream product

• 59-88-1 phenylhydrazine hydrochloride 
• 76348-92-0 ethyl 1-(4'-fluorophenyl)-3-(dimethylamino)prop-2-enone-2-carboxylate 
• 1999-00-4 ethyl 3-(4'-fluorophenyl)-3-oxopropionate 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 100-63-0 phenylhydrazine 
• 403-42-9 1-(4-fluorophenyl)ethanone 

Downstream Products

• 936127-72-9 5-(4-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxylic acid 
• 1421848-87-4 5-(4-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide 
• 1421848-88-5 5-(4-fluorophenyl)-1-phenyl-1H-pyrazole-4-carbothioamide 
• 1421848-90-9 ethyl {2-[5-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-1,3-thiazol-4-yl}acetate 
• 1421848-91-0 {2-[5-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-1,3-thiazol-4-yl}acetic acid 
• 1421847-27-9 2-{2-[5-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-1,3-thiazol-4-yl}-N-(tetrahydro-2H-pyran-4-ylmethyl)acetamide 
• 797053-56-6 [5-(4-fluoro-phenyl)-1-phenyl-1H-pyrazol-4-yl]-phenyl-methanol 
• 797053-44-2 5-(4-fluoro-phenyl)-1-phenyl-1H-pyrazole-4-carbaldehyde 
• 797053-33-9 [5-(4-fluoro-phenyl)-1-phenyl-1H-pyrazol-4-yl]-methanol 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUND

Provided is a heterocyclic compound having an RORγt inhibitory activity. A compound represented by the formula (I): wherein ring A is an optionally substituted cyclic group, Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene, R1 is a substituent, ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2, and R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group, or a salt thereof.

Synthesis, antimicrobial activity and molecular modeling studies of halogenated 4-[1H-imidazol-1-yl(phenyl)methyl]-1,5-diphenyl-1H-pyrazoles

Halogenated diphenylpyrazole analogues of bifonazole were prepared and their microbiological properties were investigated. During the course of our studies in the azole antifungals area, we synthesized a number of 1,5-disubstituted 4-[1H-imidazol-1-yl(phenyl)methyl]-1H-pyrazoles, analogues of bifonazole. 1,5-Diphenyl-1H-pyrazole 3 showed weak antimycotic and antibacterial activities in vitro against Candida albicans, Cryptococcus neoformans and Staphylococcus aureus. In order to increase these properties, given that the halo substitution was found to be capable of enhancing antifungal effects, we prepared a series of fluoro and chloro derivatives of 3. The microbiological evaluation carried out on newly synthesized compounds included in vitro assays for antifungal, antibacterial and antimycobacterial activities. Among the tested compounds, some dichloro and trichloro-derivatives showed interesting antimicrobial properties. In particular, compounds 10j,k,l produced inhibitory effects against pathogen representatives of yeast (C. albicans, C. neoformans) and Gram positive bacteria (S. aureus) similar or superior to those of bifonazole. In addition, their activity against Mycobacterium tuberculosis was superior to that of clotrimazole and econazole, which were used as reference drugs. The replacement, in these compounds, of chlorine with fluorine atoms led to inactive derivatives.Docking studies were carried out on the most active compounds, in order to rationalize the pharmacological results.