Design, synthesis, antifungal activity, and molecular docking studies of benzothiazole, S-benzyl-2,4-isodithiobiuret, and thiourea derivatives of 1-hepta-O-benzoyl-β-d-maltose nanoparticles [0.03%]
1-庚氧苯甲酰基-β-d-麦芽糖纳米颗粒的苯并噻唑、S-苄基-2,4-异二硫代生物脲和硫脲衍生物的设计、合成、抗真菌活性及分子对接研究
Shankesh C Zyate,Nikita V Awajare,Sanjay S Gaikwad et al.
Shankesh C Zyate et al.
The surge in fungal infection-related mortality worldwide is being caused by drug resistance to well-established antifungals such azole derivatives (bifonazole, fluconazole, miconazole, and clotrimazole). Finding novel molecules that are st...
Synthesis of new Pyridazinone derivatives and their dual inhibitory activity on aldose reductase and α-glucosidase [0.03%]
新的吡啶并咪唑酮衍生物的合成及对该酶和α-葡萄糖苷酶的双重抑制活性研究
Mevlüt Akdağ,Merve Güneş Çam,Derya Ergen et al.
Mevlüt Akdağ et al.
Diabetes mellitus is a chronic metabolic disorder associated with microvascular complications such as neuropathy, nephropathy, and retinopathy. Two complementary therapeutic strategies are targeting the polyol pathway via aldose reductase (...
Discovery of novel imidazo[4,5-b]pyridine derivatives as noncovalent reversible Bruton's tyrosine kinase inhibitors [0.03%]
一类新型非共价可逆的BTK抑制剂——咪唑并吡啶衍生物的研究发现
Yeojeong Kim,Jingyang Sun,Kyoungyim Lee et al.
Yeojeong Kim et al.
Bruton's tyrosine kinase (BTK) has emerged as a validated therapeutic target for B-cell malignancies and autoimmune disorders, and covalent BTK inhibitors have demonstrated remarkable clinical efficacy. However, because of concerns regardin...
Exploring the therapeutic potential of deuterated PPARγ agonists for NASH [0.03%]
氘代PPARγ激动剂治疗NASH的潜力研究
Xudong Pang,Dawei Cui,Ruifeng Liu et al.
Xudong Pang et al.
NASH represents an increasingly prevalent chronic liver disease, and TZDs are investigated as a potential therapeutic strategy. However, the inherent enolic structure of TZDs leads to enantiomeric instability and racemization, often requiri...
Design, synthesis, and activity evaluation of alpinetin derivatives as potential anti-liver cancer drugs [0.03%]
设计、合成和活性评价异阿尔皮宁衍生物作为潜在的抗肝癌药物
Yanhui Yi,Yupei Sun,Xiangyang Zhang et al.
Yanhui Yi et al.
Liver cancer represents a major global health challenge, significantly impacting populations both in China and worldwide. Alpinetin (ALP), extracted from the ginger plant cardamom, has been shown to possess significant anti-liver cancer act...
Iridium and rhenium complexes in photodynamic and sonodynamic therapy: mechanistic insights and therapeutic potential [0.03%]
用于光动力和声动力治疗的铱和铑配合物：机理见解与治疗潜力
Sreejani Ghosh,Rinku Chakrabarty,Priyankar Paira
Sreejani Ghosh
Cancer maintains to be a major worldwide health epidemic, and despite breakthroughs in targeted agents, immunotherapy, chemotherapy, and surgery, considerable limitations persist. These comprise therapeutic resistance, dose-limiting toxicit...
LXH254 hybrid with adamantane: synthesis and in vitro evaluation of 2,4,6-trisubstituted pyridine derivative Z-001 containing adamantyl moiety as a novel B-RAF inhibitor [0.03%]
含金刚烷基的新化合物Z-001的合成及其体外抑制B-RAF活性的研究
Wei Fan,Meina Li,Yeming Wang
Wei Fan
In this study, 2,4,6-trisubstituted pyridine derivative Z-001 containing adamantyl moiety was designed through the hybridization strategy of LXH254 and adamantane. A new and effective synthetic route was established to achieve the synthesis...
Jiyun Zhu,Sara Gutkin,Shiyu Chen et al.
Jiyun Zhu et al.
The cysteine cathepsins are a family of proteases that are widely expressed in diverse cell types. However, because their activity is highly upregulated at sites of inflammation, they are ideal targets for imaging a range of disease patholo...
Structural modification of atractylenolides: synthesis and evaluation of derivatives with potent anti-Aβ aggregation and neuroprotective activities against Alzheimer's disease [0.03%]
苍术香升高效抗阿兹海默病Tau及Aβ毒性的结构改造研究
Tiancheng Sun,Zhonghua Li,Bingyu Xiao et al.
Tiancheng Sun et al.
Alzheimer's disease (AD), a progressive neurodegenerative disorder characterized by β-amyloid (Aβ) deposition, hyperphosphorylated Tau tangles, and neuronal loss, lacks effective disease-modifying therapies. Herbal medicines like Atractyl...
Discovery of DS79540454 via fragment-based drug discovery strategy: New scaffolds of hypoxia-inducible factor prolyl hydroxylase inhibitor [0.03%]
基于片段的药物发现策略的新构架：低氧诱导因子脯氨酰羟化酶抑制剂DS79540454的发现
Takeshi Fukuda,Tatsuya Nishi,Takashi Ishiyama et al.
Takeshi Fukuda et al.
The inhibition of hypoxia-inducible factor prolyl hydroxylase domain proteins (HIF-PHDs) represents a promising strategy for treating renal anemia. We identified a hydroxypyrimidine core with HIF-PHD inhibitory activity based on a fragment-...