77344-62-8

Upstream product

• 100-18-5 1,4-bis(1-methylethyl)benzene 
• 75-36-5 acetyl chloride 
• 75-15-0 carbon disulfide 
• 7446-70-0 aluminium trichloride 
• 3445-42-9 α,α-dimethyl-p-isopropylbenzyl alcohol 
• 645-13-6 4-isopropylacetophenone 
• 2388-14-9 para-isopropenyl cumene 

Downstream Products

• 40428-87-3 1-[3-(propan-2-yl)phenyl]ethan-1-one 
• 136215-93-5 2-(2,5-diisopropyl-phenyl)-propan-2-ol 
• 948-32-3 1,2,4-triisopropylbenzene 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains

Antimicrobial resistance (AMR) is a major health problem worldwide, because of ability of bacteria, fungi and viruses to evade known therapeutic agents used in treatment of infections. Aryldiketo acids (ADK) have shown antimicrobial activity against several resistant strains including Gram-positive Staphylococcus aureus bacteria. Our previous studies revealed that ADK analogues having bulky alkyl group in ortho position on a phenyl ring have up to ten times better activity than norfloxacin against the same strains. Rational modifications of analogues by introduction of hydrophobic substituents on the aromatic ring has led to more than tenfold increase in antibacterial activity against multidrug resistant Gram positive strains. To elucidate a potential mechanism of action for this potentially novel class of antimicrobials, several bacterial enzymes were identified as putative targets according to literature data and pharmacophoric similarity searches for potent ADK analogues. Among the seven bacterial targets chosen, the strongest favorable binding interactions were observed between most active analogue and S. aureus dehydrosqualene synthase and DNA gyrase. Furthermore, the docking results in combination with literature data suggest that these novel molecules could also target several other bacterial enzymes, including prenyl-transferases and methionine aminopeptidase. These results and our statistically significant 3D QSAR model could be used to guide the further design of more potent derivatives as well as in virtual screening for novel antibacterial agents.

4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters and a process for their preparation

4-Hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, process for their preparation, their use as pharmaceuticals, and pharmaceutical preparations and precursors. Compounds of the formula I STR1 and the corresponding open-chain dihydroxycarboxylic acids of the formula II STR2 in which X, Y, R1, R2, R3, R4 and R5 have the meanings indicated, and also their pharmacologically tolerable salts with bases and their pharmacologically tolerable esters, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. In addition, compounds of the formula III STR3 in which R1, R2, R3, R4, R5, X and Y have the meanings indicated are described.