Design, synthesis, and biological evaluation of disubstituted thiazolidinedione derivatives as pancreatic lipase inhibitors for the management of obesity [0.03%]
二取代硫唑烷二酮衍生物作为抗肥胖脂肪酶抑制剂的设计、合成及生物学评价
Mhd Shabbu Khan,Rakesh Khator,Nisha Yadav et al.
Mhd Shabbu Khan et al.
Aim: Inspired by our previous research findings and to explore the effect of N-3 and C-5 substitution in relation to pancreatic lipase (PL) inhibitory activity, the present study aims at the design and synthesis of a seri...
Recent advances in the design and development of small molecules targeting the TLR4 signaling pathway [0.03%]
靶向TLR4信号通路的小分子设计与开发进展
Muhammad Ishfaq,Muhammad Shahab,Guosong Jiang
Muhammad Ishfaq
Toll-like receptor-4 (TLR4) is a key pattern recognition receptor that plays an essential role in initiating innate immune responses. However, dysregulated TLR4 signaling is associated with the progression of sepsis, neurodegenerative disor...
Novel multitargeted Imidazo[1,2- a]pyridine-1,3,4-oxadiazole hybrids: design, synthesis and biological evaluation as anti-Alzheimer's agents [0.03%]
新型多靶标imidazo[1,2-a]吡啶-1,3,4-恶二唑衍生物的设计、合成及抗阿尔茨海默病活性研究
Drashti Shah,Ashish Patel,Alkesh Patel
Drashti Shah
Aims: To design, synthesize, and evaluate novel imidazo[1,2-a]pyridine derivatives as dual acetylcholinesterase (AChE) and β-secretase (BACE1) inhibitors for potential Alzheimer's disease (AD) therapy. ...
Targets for bacterial resistance: recent advances in small-molecule FtsZ inhibitors [0.03%]
细菌抗性靶点——近期小分子FtsZ抑制剂研究进展
Wu-Bin Shao,Xiang Zhou,Song Yang et al.
Wu-Bin Shao et al.
ESKAPE pathogens (including Staphylococcus aureus, Enterococcus faecalis, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacteriaceae) represent a core challenge in the global antimicrobial resistance (AMR...
Rational design and biological investigation of benzylidene-substituted pyrazolo[3,4- b]pyridine derivatives as novel PIM-1 kinase inhibitors with anticancer potential [0.03%]
新型PIM-1激酶抑制剂茋取代的吡唑并[3,4-b]吡啶衍生物的设计、合成及抗肿瘤活性研究
Aastha Singh,Subhadip Maity,Priya Devi et al.
Aastha Singh et al.
Background: PIM-1 kinase is a significant oncogenic serine/threonine kinase that is implicated in various aspects of cancer cell proliferation, survival, and tumor progression. In this manuscript, a novel series of benzyl...
A comprehensive review of indole hybrids as anti-bacterial and anti-fungal agents: synthetic protocols and SAR studies [0.03%]
作为抗菌和抗真菌剂的吲哚杂化物的全面综述：合成方案和构效关系研究
Sri Mounika Bellapukonda,Muhammed Anas Kt,Shivam Mishra et al.
Sri Mounika Bellapukonda et al.
Antimicrobial resistance, a consequence of the prevalent overuse and misuse of antibiotics, has become a serious global health concern. While extensive drug discovery efforts are constantly underway to combat this, the relentless emergence ...
Evaluation of new 5-benzylidenethiazolidin-2,4-dione derivatives linked to nitric oxide donor oxime moiety as VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative assessment and in silico studies [0.03%]
评估新型5-苯基缩氨硫脲并二氢噁唑啉-2,4-二酮衍生物与一氧化氮供体肟部分相连作为VEGFR-2抑制剂和促凋亡诱导物：设计、合成、抗增殖评价及分子对接研究
Abeer M Abd El-Hameed,Naglaa M Ahmed,Wael A A Fadaly et al.
Abeer M Abd El-Hameed et al.
Aim: Approaching VEGFR-2 blockers, two novel series of 5-benzylidenethiazolidine-2,4-dione 16c-f and 17a-f were synthesized. Methods: S...
Newly synthesized 2-cyclopentylidenehydrazinylthiazoles as potential therapeutic agents against peptic ulcer [0.03%]
新合成的2-环戊撑基肼基噻唑类化合物作为潜在的抗消化性溃疡药物
Sehrish,Uzma Salar,Farzana Naz et al.
Sehrish et al.
Background: Urease increases the stomach's pH by hydrolyzing urea and fostering the growth of Helicobacter pylori, linked to a variety of gastrointestinal issues, including peptic ulcers. Despite the availability of conve...
Wogonin-derived chemotype enables discovery of novel GLS1 inhibitors with potent antitumor activity [0.03%]
从沃尔格非林衍生的化学类型可发现具有强大抗肿瘤活性的新型GLS1抑制剂
Xuhong Li,Yan Liang,Xiaoyu Zhang et al.
Xuhong Li et al.
Aims: This study evaluates LX-191, a wogonin-derived glutaminase-1 (GLS1) inhibitor featuring a non-BPTES chemotype, designed to overcome the limitations of existing GLS1-targeted therapies. ...
Synthesis, characterization & molecular docking studies of rationally designed azobenzene-Derived 5-oxoimidazoline derivatives as potent antimicrobial agents [0.03%]
合理设计的偶氮苯衍生物5-氧化咪唑啉衍生物作为抗菌剂的研究、表征及分子对接研究
Vipasha Sharma,Sumitra Nain
Vipasha Sharma
Aim: The study aimed to design the series of azobenzene-induced 5-oxoimidazoline moiety, represents as a promising structural framework for the development of a new class of antimicrobial agents, supported by molecular do...