Dual-target inhibitors of mycobacterial aminoacyl-tRNA synthetases among N-benzylidene- N'-thiazol-2-yl-hydrazines [0.03%] N-苯甲基-N'-噻唑-2-基肼类的双靶点抑制剂:针对分枝杆菌氨酰-tRNA合成酶
Oksana P Kovalenko,Galyna P Volynets,Mariia Yu Rybak et al. Oksana P Kovalenko et al.
Effective treatment of tuberculosis is challenged by the rapid development of Mycobacterium tuberculosis (Mtb) multidrug resistance that presumably could be overcome with novel multi-target drugs. Aminoacyl-tRNA synthetases (AARSs) are an e...
Overcoming synthetic challenges in targeting coenzyme A biosynthesis with the antimicrobial natural product CJ-15,801 [0.03%] 克服抗菌天然产物CJ-15,801靶向辅酶A生物合成的合成挑战
Riyad Domingo,Renier van der Westhuyzen,Anton R Hamann et al. Riyad Domingo et al.
The biosynthesis of the essential metabolic cofactor coenzyme A (CoA) has been receiving increasing attention as a new target that shows potential to counter the rising resistance to established antimicrobials. In particular, phosphopantoth...
Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists [0.03%] 柚皮酰胺衍生物是形式肽受体1拮抗剂
Margherita Mastromarino,Liliya N Kirpotina,Igor A Schepetkin et al. Margherita Mastromarino et al.
Formyl peptide receptor 1 (FPR1) is expressed on a variety of immune system cells and is a key regulator of the inflammatory environment. Therefore, the development of FPR1 antagonists may represent a novel approach for modulating innate im...
Current and emerging therapeutic targets of alzheimer's disease for the design of multi-target directed ligands [0.03%] 用于设计多靶标导向配体的阿尔茨海默病当前及新兴治疗靶点
Laura Blaikie,Graeme Kay,Paul Kong Thoo Lin Laura Blaikie
Alzheimer's disease (AD) is the most prevalent neurodegenerative disease, and a major cause of death worldwide. The number of people suffering from this debilitating disorder is rising at an unprecedented rate, with a subsequent surge in he...
Recent developments on zinc(ii) metal-organic framework nanocarriers for physiological pH-responsive drug delivery [0.03%] 用于生理pH响应型药物输送的锌金属有机框架纳米载体的研究进展
Weicong Liu,Ying Pan,Weiwei Xiao et al. Weicong Liu et al.
The high storage capacities and excellent biocompatibilities of zinc(ii) metal-organic frameworks (Zn-MOFs) have made them outstanding candidates as drug delivery carriers. Recent studies on the pH-responsive processes based on carrier-drug...
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules [0.03%] 用小分子化合物阻断环二核苷酸-cGAS-STING信号轴
Herman O Sintim,Clinton G Mikek,Modi Wang et al. Herman O Sintim et al.
The cyclic dinucleotide-cGAS-STING axis plays important roles in host immunity. Activation of this signaling pathway, via cytosolic sensing of bacterial-derived c-di-GMP/c-di-AMP or host-derived cGAMP, leads to the production of inflammator...
Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors [0.03%] 甲基磺酰氨基取代基可改善二环并吡啶类沙眼衣原体抑制剂的药代动力学性质
Martina Kulén,Carlos Núñez-Otero,Andrew G Cairns et al. Martina Kulén et al.
Chlamydia trachomatis infections are a global health problem and new approaches to treat C. trachomatis with drugs of high specificity would be valuable. A library of substituted ring fused 2-pyridones has been synthesized and evaluated for...
Small antibacterial molecules highly active against drug-resistant Staphylococcus aureus [0.03%] 一类对耐甲氧西林金黄色葡萄球菌高效的新型小分子抗菌化合物
Rajib Dey,Kathakali De,Riya Mukherjee et al. Rajib Dey et al.
The rapid growth of antibiotic resistance in Staphylococcus aureus coupled with their biofilm forming ability has made the infections difficult to treat with conventional antibiotics. This has created a massive threat towards public health ...
Structural modification of azolylacryloyl derivatives yields a novel class of covalent modifiers of hemoglobin as potential antisickling agents [0.03%] 异唑丙烯酰基衍生物的结构修饰得到一类新型的与血红蛋白共价结合的抗溶血剂化合物
A M Omar,T David,P P Pagare et al. A M Omar et al.
The intracellular polymerization and the concomitant sickling processes, central to the pathology of sickle cell disease, can be mitigated by increasing the oxygen affinity of sickle hemoglobin (HbS). Attempts to develop azolylacryloyl deri...
Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study [0.03%] 茋衍生物PPAR激动剂的可成药性评价:物理化学性质及PAMPA研究
Pasquale Linciano,Barbara De Filippis,Alessandra Ammazzalorso et al. Pasquale Linciano et al.
PPAR agonists represent a new therapeutic opportunity for the prevention and treatment of neurodegenerative disorders, but their pharmacological success depends on favourable pharmacokinetic properties and capability to cross the BBB. In th...