289503-27-1

Upstream product

• 3993-78-0 2-amino-4-chloropyrimidine 
• 289503-26-0 N-tosyl-6-bromo-3-indolylboronic acid 
• 189265-99-4 6-bromo-1-(4-methylphenylsulfonyl)-1H-indole 
• 289503-25-9 N-tosyl-3,6-dibromoindole 
• 316181-82-5 1-(6-bromo-1H-indol-3-yl)ethan-1-one 
• 50-01-1 guanidine hydrochloride 
• 341998-58-1 (E)-1-(6-bromo-1-tosyl-1H-indol-3-yl)-3-(dimethylamino)prop-2-en-1-one 
• 52415-29-9 6-bromo-1H-indole 
• 224434-85-9 1-(6-bromo-1-tosyl-1H-indol-3-yl)ethan-1-one 
• 98-59-9 p-toluenesulfonyl chloride 

Relevant academic research and scientific papers

Meridianin D Analogues Display Antibiofilm Activity against MRSA and Increase Colistin Efficacy in Gram-Negative Bacteria

In the last 30 years, development of new classes of antibiotics has slowed, increasing the necessity for new options to treat multidrug resistant bacterial infections. Development of antibiotic adjuvants that increase the effectiveness of currently available antibiotics is a promising alternative approach to classical antibiotic development. Reports of the ability of the natural product meridianin D to modulate bacterial behavior have been rare. Herein, we describe the ability of meridianin D to inhibit biofilm formation of methicillin-resistant Staphylococcus aureus (MRSA) and to increase the potency of colistin against colistin-resistant and sensitive Gram-negative bacteria. Analogues were identified that are capable of inhibiting and dispersing MRSA biofilms and lowering the colistin MIC to below the CLSI breakpoint against Acinetobacter baumannii, Klebsiella pneumoniae, and Escherichia coli.

Synthesis of indolylpyrimidines via cross-coupling of indolylboronic acid with chloropyrimidines facile synthesis of meridianin D

Palladium catalyzed cross-coupling reaction of 3-indolylboronic acid with 2,4-dichloropyrimidines proceeded regioselectively to yield indolyl-or bis(indolyl)pyrimidines in high yield, depending on the projection of 3indolylboronic acid. The marine indole alkaloid meridianin D and an analogue were synthesised via the palladium catalyzed cross-coupling reaction as a key step.