38256-07-4Relevant articles and documents
Identification of inhibitors targeting polyketide synthase 13 of Mycobacterium tuberculosis as antituberculosis drug leads
Wang, Xiao,Zhao, Wenting,Wang, Bin,Ding, Wei,Guo, Hao,Zhao, Hongyi,Meng, Jianzhou,Liu, Sihan,Lu, Yu,Liu, Yishuang,Zhang, Dongfeng
, (2021/06/30)
Polyketide synthase 13 (Pks13) is an essential enzyme in the synthesis of mycolic acids in Mtb. Therefore, Pks13 is a promising drug target for tuberculosis treatment. We used a structure-guided approach to identify novel chemotype inhibitors of Pks13 and assessed them using a Pks13 enzymatic assay and surface plasmon resonance. The structure–activity relationships (SAR) results demonstrated that the substituents at the 2, 5, and 6 positions of the 4H-chromen-4-one scaffold are critical for maintaining the MIC. Compound 6e with 2-hydroxyphenyl at the 2 position of the 4H-chromen-4-one scaffold, exhibited potent activity against Mtb H37Rv (MIC = 0.45 μg/mL) and displayed good Pks13 affinity and inhibition (IC50 = 14.3 μM). This study described here could provide an avenue to explore a novel inhibitor class for Pks13 and aid the further development of antituberculosis drugs.
Design, synthesis and biological evaluation of 2-Phenyl-4H-chromen-4-one derivatives as polyfunctional compounds against Alzheimer’s disease
Singh, Manjinder,Kaur, Maninder,Vyas, Bhawna,Silakari, Om
, p. 520 - 530 (2017/10/09)
Polyfunctional compounds comprise a novel class of therapeutic agents for the treatment of multi-factorial diseases. A series of 2-Phenyl-4H-chromen-4-one and its derivatives (5a–n) were designed, synthesized, and evaluated for their poly-functionality against acetylcholinestrase (AChE) and advanced glycation end products (AGEs) formation inhibitors against Alzheimer’s disease (AD). The screening results showed that most of them exhibited a significant ability to inhibit AChE AGEs formation with additional radical scavenging activity. Especially, 5m, 5b, and 5j displayed the greatest ability to inhibit AChE (IC50 = 8.0, 8.2, and 11.8 nM, respectively) and AGEs formation (IC50 = 55, 79, and 54 μM, respectively) with good antioxidant activity. Molecular docking studies explored the detailed interaction pattern with active, peripheral, and mid-gorge sites of AChE. These compounds, exhibiting such multiple pharmacological activities, can be further taken a lead for the development of potent drugs for the treatment of Alzheimer’s disease.
Five-membered heterocycle (or amide)-flavonoid compound-matrine ternary conjugate and application thereof
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Paragraph 0039; 0040, (2016/10/08)
The invention discloses a five-membered heterocycle (or amide)-flavonoid compound-matrine ternary conjugate and application thereof. The five-membered heterocycle (or amide)-flavonoid compound-matrine ternary conjugate has a structure as shown in the specification, has an effective antibacterial activity, and has a potential application value in the aspect of antibacterial drug development. The five-membered heterocycle (or amide)-flavonoid compound-matrine ternary conjugate has a remarkable effect on the antibacterial aspect, and can be applied to prevention and treatment of MRSA, P.aeru, E.coli, Ab and other clinical common pathogens.