Design, synthesis, and molecular modeling of novel thiazolopyridine-based inhibitors of enoyl acyl carrier protein reductase (InhA) as anti- Mycobacterium tuberculosis agents [0.03%]
新型噻唑并吡啶类抑制结核分枝杆菌烯酰基乙酰载体蛋白还原酶( inh a)的抑制剂的设计、合成及分子模拟研究
Ahmed Sabt,Małgorzata Korycka-Machała,Asmaa F Kassem et al.
Ahmed Sabt et al.
The updated guidelines from the World Health Organization highlight that treatment options for multidrug-resistant tuberculosis (MDR-TB) remain limited due to the scarcity of effective drugs. As a result, there is an urgent necessity to dev...
Inhibitors of type II NADH-dehydrogenase, cytochrome bd oxidase, and ATP synthase for anti-tubercular response [0.03%]
II型NADH脱氢酶、细胞色素bd氧化酶和ATP合成酶抑制剂的抗结核作用
Pallavi Saha,Mohit Kumar,Deepak K Sharma
Pallavi Saha
The identification of novel anti-tubercular agents capable of eliciting lethal responses against drug-resistant tuberculosis is critically needed to address the escalating mortality from tuberculosis. Mycobacterium tuberculosis, the etiolog...
2,5-Diazabicyclo[2.2.1]heptane in medicinal chemistry: a treasure trove of therapeutic opportunities [0.03%]
二氮杂双环他平在药物化学中的研究进展:一个充满治疗潜力的研究领域
Pranav Kumar Ambast,Saumya Kapoor,Rudradip Das et al.
Pranav Kumar Ambast et al.
2,5-Diazabicyclo[2.2.1]heptane (2,5-DBH) has emerged as a valuable scaffold in medicinal chemistry owing to its conformational rigidity and favorable three-dimensional architecture. In recent years, 2,5-DBH has been increasingly incorporate...
Susanta Samajdar
Susanta Samajdar
Medicinal chemistry has driven the evolution of oncology drug discovery, transitioning from early cytotoxic agents to modern precision-guided therapies. This opinion article traces the historical trajectory of medicinal chemistry practices,...
Editorial
RSC medicinal chemistry. 2026 Jan 7. DOI:10.1039/d5md01040c 2026
Oxyprenyl-chalcones as antibacterial hits: design of experiments-optimized synthesis, antibacterial evaluation, early drug-like profiling and biodegradability prediction [0.03%]
具有抗菌活性的茋的合成优化、抗菌评价及药物早期性质评估和生物降解性预测
Ludovica Marotta,Francesca Maria Pia Rita Giammarino,Brondon Brandly Senenou Tambou et al.
Ludovica Marotta et al.
The escalating threat of antimicrobial resistance (AMR) compels the development of novel antibiotics with broad spectrum activity and environmentally responsible degradation profiles. Chalcones, naturally occurring 1,3-diaryl-2-propen-1-one...
CNS penetrant TEAD1,2,4 inhibitor MSC-4070 derived from phenotypic screening hit optimization [0.03%]
基于表型筛选 hits 优化的穿透中枢神经系统的 TEAD1,2,4 抑制剂 MSC-4070
Timo Heinrich,Carl Petersson,Jakub Gunera et al.
Timo Heinrich et al.
TEAD proteins are attractive cancer targets due to their role in cell proliferation and metastasis. We report the development of MSC-4070, a CNS-penetrant TEAD1,2,4 inhibitor derived from phenotypic screening hit optimization. Starting with...
Efficient log P determination by automated, spatially encoded 19F NMR spectroscopy [0.03%]
基于空间编码的自动化氟核磁共振光谱高效测定log P值
Susanna H Wood,Fiona Gordon,Robin S Stein et al.
Susanna H Wood et al.
We report a straightforward method for direct determination of log P by slice-selective 19F NMR spectroscopy utilising a single NMR sample. Our technique uses a partitioned NMR sample of n-octanol/water containing the compound of interest, ...
Harnessing carlina oxide scaffold for the management of vector-borne diseases: synthesis and structure-activity relationship [0.03%]
卡琳那氧化物骨架在媒介传播疾病治疗中的应用:合成及构效关系研究
Eleonora Spinozzi,Alessia Piergentili,Marta Ferrati et al.
Eleonora Spinozzi et al.
Vector-borne diseases are causes of global health concern and mosquitoes are the primary transmitters of health-threatening pathogens. Botanicals are sources of compounds structurally modifiable into versatile hits for novel plant-based ins...
Correction: Design, synthesis, and anti-plasmodial profiling of oxalamide-linked 4-aminoquinoline-phthalimide hybrids [0.03%]
纠正:4-氨基喹啉酞酰亚胺杂环的氧化胺连接体的设计、合成及抗疟活性研究
Nikita Gupta,Anu Rani,Kewal Kumar et al.
Nikita Gupta et al.
[This corrects the article DOI: 10.1039/D5MD00425J.]. This journal is © The Royal Society of Chemistry.
Published Erratum
RSC medicinal chemistry. 2026 Jan 21. DOI:10.1039/d6md90001a 2026
Recent progress of METTL3 inhibitors for cancer therapeutics: design, optimization and potential applications [0.03%]
METTL3抑制剂在癌症治疗中的最新进展:设计、优化及潜在应用
Yun Zhang,Mengxiang Quan,Qinlan Chen et al.
Yun Zhang et al.
Acute myeloid leukaemia (AML) is a clonal proliferative malignant hematologic disease of hematopoietic stem cells, characterized by the accumulation of immature progenitor cells and the inhibition of hematopoietic function due to blocked di...