Endoperoxide delivered singlet oxygen: the future of PDT, without light or oxygen [0.03%]
内过氧化物递送单线态氧：无需光或氧气的PDT的未来
Wanwan Wang,Lei Wang,Rensong Sun et al.
Wanwan Wang et al.
Chemically generated singlet oxygen via cycloreversion reaction of aromatic endoperoxides is poised to evolve into a highly promising therapeutic protocol. Singlet oxygen can also be produced endogenically, with a short half-life especially...
The dual functions of a nor-sesquiterpene-triazole derivative against influenza A viruses through the activation of the Nrf2/HO-1 signaling pathway and interaction with hemagglutinin [0.03%]
一种nor-seco倍半萜三唑衍生物通过激活Nrf2/HO-1信号通路和与血凝素相互作用对抗流感病毒的双重功能研究
Shaofen Zhou,Jingyan Wei,Shixin Li et al.
Shaofen Zhou et al.
Influenza viruses are the main causative agents of seasonal influenza epidemics in humans. The emergence of drug-resistant strains has significantly limited the effectiveness of existing antiviral therapies, highlighting the urgent need for...
Structure-activity optimization of N-arylindole GPR52 agonists for enhanced antipsychotic efficacy: design, synthesis, and pharmacological evaluation [0.03%]
N-芳基吲哚GPR52激动剂的结构活性优化以增强抗精神病功效：设计、合成和药理学评价
Xiaojie Hu,Qingshan Gu,Qiuyu Xiong et al.
Xiaojie Hu et al.
GPR52 is a promising therapeutic target for schizophrenia, capable of addressing positive, negative, and cognitive symptoms simultaneously. In this study, we designed and synthesized a series of N-arylindole GPR52 agonists by optimizing the...
Medicinal attributes of nitrogen heterocycles directing aldose reductase selectivity and potency [0.03%]
含氮杂环化合物通过调节己糖还原酶的选择性和活性发挥药理作用
Anita Kumari,Shyamal Kumar Manna,Kajal Rani et al.
Anita Kumari et al.
Diabetic complications arise primarily from hyperglycemia-induced metabolic disturbances, among which the polyol pathways play a significant role through the overactivation of aldose reductase. ARIs have therefore emerged as a potent therap...
Empowering molecular complexity via biocatalysis: emerging blueprints in the total synthesis of medicinally relevant natural products [0.03%]
生物催化作用下的分子复杂度提升：药物相关天然产物全合成中的新蓝图
Ram N Yadav,Sovan Dey,Md Firoj Hossain et al.
Ram N Yadav et al.
Biocatalysis has ascended as a defining force in contemporary total synthesis, furnishing catalytic modalities that deliver molecular complexity with unparalleled chemo-, regio-, and stereo-control. As structurally sophisticated therapeutic...
Structure-activity landscape of Nurr1 (NR4A2) modulators: medicinal chemistry strategies for neurodegenerative disease intervention [0.03%]
Nurr1(NR4A2)调节剂的构效关系：神经退行性疾病干预的药物化学策略
Sahil Jaidka,Ankush Kumar,Thakur Gurjeet Singh et al.
Sahil Jaidka et al.
Nuclear receptor-related 1 protein (Nurr1/NR4A2) is an orphan nuclear receptor essential for dopaminergic neuron development, maintenance, and survival. Nurr1 is highly expressed in the substantia nigra and regulates transcription of key do...
A medicinal chemistry perspective on SIRT3 modulators in disease treatment [0.03%]
从药物化学角度解析SIRT3调节剂的疾病治疗潜力
Yaoliang Li,Yuqi Bao,Yunxia Cui et al.
Yaoliang Li et al.
As the primary mitochondrial deacetylase, SIRT3 plays a central role in key biological processes such as cellular energy metabolism, oxidative stress response, and apoptosis regulation. It is also closely associated with the development and...
Integrating green synthesis and liquid-liquid extraction of lidocaine in deep eutectic solvents [0.03%]
深共熔溶剂中利多卡因绿色合成与液液萃取的集成体系研究
Assunta Perri,Leonardo C Parrotta,Stefania Gencarelli et al.
Assunta Perri et al.
The development of greener and more sustainable processes for active pharmaceutical ingredients (APIs) remains a major challenge for the chemical industry. Here we present a fully integrated process for the synthesis of lidocaine carried ou...
Novel glycine amides, semicarbazides and fluoroallylamines as inhibitors of the amine oxidase vascular adhesion protein-1 (VAP-1) [0.03%]
新型甘氨酸酰胺、异半胱胺酸衍生物和氟丙氨衍生物作为胺氧化酶血管粘附蛋白-1（VAP-1）的抑制剂
Timo Pöstges,Jan Kampschulze,Walburga Hanekamp et al.
Timo Pöstges et al.
Vascular adhesion protein-1 (VAP-1), also known as copper-containing amine oxidase 3 (AOC3), is an enzyme implicated in the pathogenesis of various diseases. Increasing evidence highlights VAP-1 as a promising therapeutic target, particular...
Discovery of RP-37 analogues as potent, selective irreversible inhibitors targeting DNA polymerase theta (POLθ) [0.03%]
用于靶向DNA聚合酶θ（POLθ）的高效选择性不可逆抑制剂RP-37类似物的研究发现
Zhenwei Wang,Mengyuan Qiu,Deming Liu et al.
Zhenwei Wang et al.
DNA polymerase theta (POLθ) is a promising synthetic lethal target for BRCA-deficient cancers, while reversible POLθ-pol inhibitors exhibit limited cellular efficacy. Here, we report the structure-guided discovery of RP-37 analogue B2 as ...