Fluorinated Aminopiperidones as Non-Glutarimide Thalidomide Analogs: Stereodivergent Synthesis and Validation [0.03%]
以非谷氨酰亚胺硫杂药类似物氟化氨基哌啶酮的立体发散合成与验证
Boštjan Adamlje,Tihomir Tomašič,Christian Steinebach et al.
Boštjan Adamlje et al.
The glutarimide fragment is a key pharmacophore in cereblon-binding immunomodulatory drugs and proteolysis-targeting chimeras, yet exploration of non-glutarimide scaffolds remains limited. Here, we report the design, synthesis, and evaluati...
Pharmacology, Medicinal Chemistry, and Therapeutic Potential of Imidazoline Receptor Ligands [0.03%]
咪唑啉受体配体的药理学、药物化学和治疗潜力
Maria-Eleni Kouridaki,Mercè Pallàs,Carmen Escolano
Maria-Eleni Kouridaki
The imidazoline receptor (IR) system, comprising the I1R, I2R, and I3R subtypes, consists of binding sites involved in cardiovascular, metabolic, and neurological disorders. This review updates the 2004 compilation by Dardonville and Rozas ...
Drug Repurposing Against Cestode Fatty Acid Binding Proteins Through Integrated Virtual Screening and In Vitro Validation [0.03%]
基于集成虚拟筛选和体外验证的cestode脂肪酸结合蛋白药物再定位研究
Santiago Rodríguez,Lucas N Alberca,Luciana Gavernet et al.
Santiago Rodríguez et al.
Echinococcosis is a neglected tropical disease (NTD) caused by Echinococcus granulosus and Echinococcus multilocularis, the etiological agents of cystic and alveolar echinococcosis, respectively. These infections pose a significant public h...
Investigating the Inhibitory Properties of Diazo and Pyrazole-Carboxamide-Linked Benzenesulfonamides Against Carbonic Anhydrase Isoforms I, II, IX, and XII [0.03%]
叠氮和吡唑甲酰胺连接的苯磺酰胺类化合物对碳酸酐酶I、II、IX和XII同工酶抑制性能的研究
Suleyman Akocak,Nebih Lolak,Andrea Ammara et al.
Suleyman Akocak et al.
A novel library of diazo and pyrazole-carboxamide-linked molecules containing the sulfonamide pharmacophore was developed and synthesized, yielding selective inhibitors of clinically relevant carbonic anhydrase (CA) isoforms. The synthesis ...
Quinoxaline-Based Monoamine Oxidase Inhibitors: Design Strategies, Synthesis, Structure-Activity Relationships, and Therapeutic Potential in Neurological Disorders: A Review From 1996 to 2026 [0.03%]
基于喹噁啉的单胺氧化酶抑制剂：设计策略、合成、构效关系及其在神经疾病治疗中的潜力（1996-2026年综述）
Sandeep Bindra,Ramajayan Pandian,Bijo Mathew et al.
Sandeep Bindra et al.
Monoamine oxidases (MAOs) are key enzymes involved in the metabolism of neurotransmitters and play a significant role in the pathophysiology of neurological disorders such as depression, Parkinson's disease, and Alzheimer's disease. Inhibit...
Immunomodulatory Potential of Quinoline Q3, a Selective Inhibitor of the Canonical NF-κB Pathway in Macrophages [0.03%]
喹啉Q3具有免疫调节潜能，可选择性抑制巨噬细胞的常规NF-κB途径
Konstantinos Michail,Panagiotis Ntavaroukas,Vasiliki Petriki et al.
Konstantinos Michail et al.
The NF-κB transcription factor pathway is a major driver of inflammation, regulating proinflammatory cytokine synthesis in innate immune cells. Its dysregulation is linked to chronic inflammatory diseases, as well as autoimmune conditions....
Synthesis and Biological Evaluation of C6-O-Glycosylated α-Mangostin Derivatives Against Methicillin-Resistant Staphylococcus aureus With Enhanced Bacterial Membrane Selectivity [0.03%]
具有增强细菌膜选择性的抗MRSa的C6-O-糖基α-紫珠茋衍生物的合成及生物学评价
Wenchong Ye,Chuangchuang Fan,Tiantian Zhou et al.
Wenchong Ye et al.
Methicillin-resistant Staphylococcus aureus (MRSA) remains a major global health threat, driving demand for antibacterial agents with robust efficacy and low propensity for resistance. The natural xanthone α-mangostin (α-MG) shows potent ...
Piperazine Derivatives Carrying an Imidazole Ring as Selective Modulators of Human Carbonic Anhydrase Isozymes [0.03%]
含咪唑环的哌嗪衍生物作为人碳酸酐酶同工酶的选择性调节剂
Alessio Gabellini,Andrea Angeli,Alessandro Bonardi et al.
Alessio Gabellini et al.
A small library of piperazine and piperazinone derivatives carrying an imidazole ring was synthesized, with the aim to find selective carbonic anhydrase (CA) modulators. These compounds can be regarded as reduced-flexibility analogues of hi...
Discovery of Ligands for the TNFR1 Extracellular Domain Using Fragment-Based Drug Discovery [0.03%]
基于片段的药物发现用于TNFR1胞外域配体的筛选与鉴定
Henri Chédotal,Katrine Povlsen,Dilip Narayanan et al.
Henri Chédotal et al.
Tumor necrosis factor receptor 1 (TNFR1) plays a major role in immunoregulation. It is involved in inflammatory and autoimmune diseases like rheumatoid arthritis, psoriasis, Alzheimer's disease, and multiple sclerosis. However, few small-mo...
An Ugi-Joullié Platform for Medicinally Relevant 1,4-Dihydrobenzothiazines [0.03%]
用于药学相关1,4-二氢苯并噻嗪的Ugi-Joullié平台
Xiaofang Lei,Christina Tomza,Maria-Aikaterini Giannakaki et al.
Xiaofang Lei et al.
A concise and modular synthetic platform for the rapid assembly of functionalized 1,4-dihydrobenzothiazines is reported through an Ugi-Joullié two-component reaction of a preformed benzothiazine-derived imine with diverse isocyanides. The ...