Structural Modification of Heterocyclic Scaffolds: A Strategy for Antibacterial Drug Discovery [0.03%]
杂环骨架的结构修饰在抗菌药物发现中的应用策略
Raksha Gupta,Anubhuti Koshle,Santosh Kumar Verma et al.
Raksha Gupta et al.
Multidrug-resistant (MDR) bacterial infections are on the rise worldwide, and there are fewer clinically available medications to treat them. Methicillin-resistant Staphylococcus aureus (MRSA) is one of the most compelling and harmful bacte...
Targeted Metabolomics and Network Pharmacology to Screen Endogenous Biomarkers Indicating Dose-Dependent Liver Injury Induced by Genipin and the Mechanism Uncovered [0.03%]
基于靶点代谢组和网络药理学的广陈皮内用金革钉所致剂量依赖性肝损伤内源性标志物筛选及机制研究
Dongxia Lyu,Fan Zhang,Jiaqi Qin et al.
Dongxia Lyu et al.
Genipin is the primary active pharmacological component of several commonly used traditional Chinese medicines, and it has a variety of applications. In addition to medical uses, it has applications in food and biomaterials. However, becaus...
Huda M Younis,Amal A Mohamed
Huda M Younis
Turmeric is a common spice obtained from the rhizomes of the Curcuma longa plant. It belongs to the Zingiberaceae (ginger family). The rhizome is a horizontally growing stem that sends roots and shoots from below ground. Turmeric has many u...
Current Landscape of Novel Therapeutic Agents and Drug Targets in Irritable Bowel Syndrome [0.03%]
当前 irritable bowel syndrome 的新型治疗药物和作用靶点的现状
Deepak Chandra Joshi,Neha Raina,Nirmal Joshi et al.
Deepak Chandra Joshi et al.
Irritable bowel disease or syndrome (IBD/IBS) is a prevalent gastrointestinal tract problem affecting approximately 4% of the total population of the world. Choosing effective pharmacological treatments for IBS is still challenging due to t...
Characterization of the Systemic Effects of Casiopeina III-Ia Using an In Vivo Glioma Model: Antitumoral, Pharmacokinetics, and Immune Responses [0.03%]
一种体内胶质瘤模型对III-Casiopeina-Ia系统作用的表征：抗肿瘤，药代动力学和免疫反应
Cristina Trejo-Solís,Inés Fuentes-Noriega,Alma Ortiz-Plata et al.
Cristina Trejo-Solís et al.
The antineoplastic properties of the Cu(II) coordination compound Casiopeina III-ia (Cas III-ia) are revealed using an in vivo glioma model, and its biopharmaceutical properties are predicted through an in silico analysis. C6 cells of the m...
An Insight Into Commercially Available SGLT2 Inhibitors and Their Structure-Activity Relationship Studies [0.03%]
SGLT2抑制剂的结构活性关系及其商用产品分析
Asiya Parveen,Shazia Parveen,Nisha Vats et al.
Asiya Parveen et al.
A serious, rapidly growing global health issue is diabetes mellitus (Type 2) caused by insulin deficiency or insulin resistance. This is a chronic condition that demands ongoing care and management. Although a variety of anti-hyperglycaemic...
Discovery and Structure-Activity Relationship Study of Pyrazolyl Indolenine Derivatives as Staphylococcus aureus Biofilm Inhibitors [0.03%]
作为金黄色葡萄球菌生物膜抑制剂的吡唑吲哚啉衍生物的发现及构效关系研究
Jason Jonah James,Cheng Hong Yap,Neni Frimayanti et al.
Jason Jonah James et al.
Staphylococcus aureus-associated infections pose a significant clinical challenge due to biofilm formation, which contributes to antibiotic resistance and persistent infections. The prevalence of methicillin-resistant S. aureus (MRSA) furth...
Ultra-Fast UPLC-MS/MS Method for the Ripretinib Quantification in the HLMs Matrix With Metabolic Stability Assessment: In-Silico Study for Toxic Alerts and the Metabolic Lability [0.03%]
基于HLMs基质的瑞普替尼高通量定量及其代谢稳定性评价方法：与毒性预测及代谢脆性评价相关的计算化学研究
Mohamed W Attwa,Adnan A Kadi
Mohamed W Attwa
Ripretinib (QINLOCK) is a broad-spectrum, orally-administered, switch-controlled kinase inhibitor that got FDA approval in May 2020 for the treatment of advanced gastrointestinal stromal tumors (GIST) in adult patients who have formerly had...
Synthesis and Biological Evaluation of Novel 2-(Piperidin-4-yl)-1,2,3,4-tetrahydroisoquinoline and 2-(Piperidin-4-yl)decahydroisoquinoline Antimycotics [0.03%]
新型2-(哌啶-4-基)-1,2,3,4-四氢异喹啉和2-(哌啶-4-基)十氢异喹啉类抗真菌化合物的设计、合成及生物活性研究
Marie-Christin Hain,Monika Klimt,Franz Bracher et al.
Marie-Christin Hain et al.
Piperidine antimycotics like fenpropidin are well established in agrochemistry. On the other hand, numerous isoquinoline derivatives show remarkable antimycotic effects. Here we present a series of 13 hybrid molecules of both lead structure...
Structure-Based Design of Chiral Thioureas as Anticholinesterase Inhibitors Using Enantiopure α-Methylbenzylamines: Synthesis, Enzyme Inhibition, and In Silico Studies [0.03%]
基于结构的手性硫脲乙醇胺的设计作为抗胆碱酯酶抑制剂：使用单一对映体α-甲基苄基胺的合成、酶抑制和计算机模拟研究
Zafer Bulut,Ayşegül Karaküçük-Iyidoğan,Melike Bilge et al.
Zafer Bulut et al.
A detailed analysis of the research on the treatment of Alzheimer's disease indicates that selective inhibition of butyrylcholinesterase (BChE) is the most promising strategy for identifying a drug target. According to this perspective, in ...