56915-76-5

Upstream product

• 21867-64-1 1-n-propylpiperazine 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 106-94-5 propyl bromide 
• 51639-48-6 4'-piperazinoacetophenone 

Downstream Products

• 56915-94-7 2-oxo-6-[4-(4-propyl-piperazin-1-yl)-phenyl]-1,2-dihydro-pyridine-3-carbonitrile 

Relevant academic research and scientific papers

1-SUBSTITUTED, 4-(SUBSTITUTED PHENOXYMETHYL)-1,2,3-TRIAZOLE COMPOUNDS WITH ANTIFUNGAL PROPERTIES AND METHODS FOR PREPARATION THEREOF

Disclosed herein are novel antifungal compounds of Formula 1, containing 1 -substituted, 4-(substituted phenoxymethyl)-l,2,3-triazole moieties coupled to a core having triazole ring, (un)substituted phenyl ring and tertiary alcoholic functionality, and pharmaceutically acceptable salts thereof; methods for preparing these compounds; and pharmaceutical preparations containing these novel compounds for prevention and treatment of fungal infections.

Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors

We have previously reported the discovery and preliminary structure activity relationships of a series of β-aminoketones that disrupt the binding of coactivators to TR. However, the most active compounds had moderate inhibitory potency and relatively high cytotoxicity, resulting in narrow therapeutic index. Additionally, preliminary evaluation of in vivo toxicology revealed a significant dose related cardiotoxicity. Here we describe the improvement of pharmacological properties of thyroid hormone receptor coactivator binding inhibitors. A comprehensive survey of the effects of substitutents in key areas of the molecule was carried out based on mechanistic insight from the earlier report. This study revealed that both electron withdrawing and hydrophobic substituents on the aromatic ring led to higher potency. On the other hand, moving from an alkyl to a sulfonyl alkyl side chain led to reduced cytotoxicity. Finally, utilization of amine moieties having low pKa's resulted in lowered ion channel activity without any loss of pharmacological activity.

Trialkylsilyl esters of 6(substituted amino)phenyl-1,-dihydro-2-oxonicotinic acid, methods for their production and conversion to the corresponding acid chlorides

Trialkylsilyl esters of 6-(substituted amino)phenyl-1,2-dihydro-2-oxonicotinic acid and acid addition salts thereof are disclosed. The compounds are useful intermediates in the preparation of pharmacological agents, especially antimicrobials of the penicillin or cephalosporin type. The compounds can be produced by reacting a 6-(substituted amino)phenyl-1,2-dihydro-2-oxonicotinic acid with a silylating agent and are converted to the useful corresponding acid chloride by reaction with thionyl chloride.

Novel antibacterial amide compounds and process means for producing the same

Novel organic amide compounds which are N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-amino-penicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.