The author of 《Synthesis, antimicrobial activity, structure-activity relationship, and molecular docking studies of indole diketopiperazine alkaloids》 were Jia, Bin; Ma, Yang-min; Liu, Bin; Chen, Pu; Hu, Yan; Zhang, Rui. And the article was published in Frontiers in Chemistry (Lausanne, Switzerland) in 2019. SDS of cas: 7524-52-9 The author mentioned the following in the article:
Strategies for the synthesis of indole diketopiperazine alkaloids (indole DKPs) have been described and involve three analogs of indole DKPs – tryprostatin open-ring indole DKPs I [R1 = H, R2 = PhCH2, 4-MeOC6H4CH2, 4-HOC6H4CH2, 4-O2NC6H4CH2; R1 = COR, R = Ph, 4-MeOC6H4, CH:CHPh, 2-furyl, 4-(Me2N)2C6H3, R2 = H], fused pentacyclic indole DKPs II [R3 = Ph, (R)-4-MeOC6H4, (S)-4-HO6H4, etc.], and spiro-pentacyclic indole DKPs III [R4 = Et, n-Pr, n-Bu, CH2CHMe2] and IV [R5 = Ph, 4-MeOC6H4, 3-ClC6H4, 4-ClC6H4, 2-Br-5-ClC6H3]. . The antimicrobial activity and structure-activity relationship (SAR) of 24 indole DKPs were explored. Compounds I (R1 = COR, R = 4-MeOC6H4, 4-HOC6H4) were found to be the most active, with min. inhibitory concentrations (MIC) values in the range of 0.94-3.87μM (0.39-1.56μg/mL) against the four tested bacteria (Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, and Escherichia coli). Furthermore, compounds III (R4 = Et, n-Pr) displayed broad-spectrum antimicrobial activity with MIC values of 1.10-36.9μM (0.39-12.5μg/mL) against all tested bacteria and plant pathogenic fungi (Colletotrichum gloeosporioides, Valsa mali, Alternaria alternata and Alternaria brassicae). According to the in silico study, compound I (R1 = COR, R = 4-HOC6H4, R2 = H) showed significant binding affinity to the FabH protein from Escherichia coli, which has been identified as the key target enzyme of fatty acid synthesis (FAS) in bacteria. Therefore, these compounds are not only promising new antibacterial agents but also potential FabH inhibitors. In the experiment, the researchers used H-Trp-OMe.HCl(cas: 7524-52-9SDS of cas: 7524-52-9)
H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.SDS of cas: 7524-52-9
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