Ferrocenyl substitution turns valproate into a glutamate decarboxylase inhibitor [0.03%]
铁ocene取代将丙戊酸转变为谷氨酸脱羧酶抑制剂
Danijela N Nikolić,Marija S Genčić,Biljana Arsić et al.
Danijela N Nikolić et al.
2-(Ferrocenylmethyl)pentanoic acid (Fc-VPA), a ferrocenyl analog of valproic acid (VPA), was synthesized, fully characterized and its effect on glutamate decarboxylase (GAD) evaluated in mouse brain homogenates using an HPLC assay. Fc-VPA p...
Optimization of 68Ga-DOTA radiolabeling conditions for disulfide-directed multicyclic peptides and amphiphilic antimicrobial peptides [0.03%]
用于二硫键导向的多环肽和两亲性抗菌肽的68Ga-DOTA标记条件优化
Xueyao Chen,Siqi Zhang,Shuo Jiang et al.
Xueyao Chen et al.
Gallium-68 labeled peptide radiotracers have attracted significant attention in positron emission tomography (PET) imaging of various diseases. While 68Ga-DOTA radiolabeling protocols are well-established, two classes of peptides, disulfide...
Design, synthesis, and Lead optimization of novel Quinazoline-based FLT3 inhibitors with potent anti-acute myelogenous leukemia activity [0.03%]
具有抗急性髓系白血病活性的新型喹唑啉FLT3抑制剂的设计、合成及成药性优化研究
Wei Liu,Shuaibo Du,Miaomiao Wang et al.
Wei Liu et al.
FLT3 mutations, including internal tandem duplications (ITD) and tyrosine kinase domain (TKD) variants, are key drivers of acute myeloid leukemia (AML) and represent attractive therapeutic targets. Guided by a scaffold-hopping strategy base...
Design, synthesis, and anti-necroptotic activity of novel Phenylbenzothiazole receptor-interacting protein kinase 1 (RIPK1) inhibitors [0.03%]
新型苯并噻唑类受体相互作用蛋白激酶1(RIPK1)抑制剂的设计、合成及抗坏死性凋亡活性研究
Jing Tao,Yuelun Xu,Zijun Chen et al.
Jing Tao et al.
Receptor-interacting protein kinase 1 (RIPK1) is a central regulator of necroptosis and a promising therapeutic target for inflammatory and degenerative diseases. Guided by computer-aided drug design (CADD) and structure-based optimizations...
Synthesis of novel bromophenolic sulfonamides with their acetylcholinesterase and carbonic anhydrase inhibitory actions [0.03%]
具有乙酰胆碱酯酶和碳酸酐酶抑制作用的新型溴代酚磺胺类化合物的合成
Necla Öztaşkın,Pegah Etminan,Akın Akıncıoğlu et al.
Necla Öztaşkın et al.
Because of the important biological properties of halogenated benzene sulfonamides, here we report the first synthesis of bromophenolic sulfonamides and their human carbonic anhydrase I (hCA I), human carbonic anhydrase II (hCA II) and acet...
Structure-activity relationship-driven lead optimization of pyrazole hydrazide-hydrazone analogues as potent antimycobacterial agents: in vitro and in silico studies [0.03%]
基于结构活性关系的异羟肟酸衍生物抗结核药物研究：体外及分子模拟研究
Pardeep Kumar,Anuradha Singampalli,Rani Bandela et al.
Pardeep Kumar et al.
A distinct series of novel pyrazole hydrazide-hydrazone analogues, developed through a structure-activity relationship-driven lead optimization approach, and evaluated for their antitubercular activity. Among the evaluated compounds, within...
In vitro investigations of troxacitabine (TROX) and 3'-deazanepanocin (DZNep) combination for pancreatic cancer therapy [0.03%]
胰腺癌治疗的TROX和DZNep联合用药的体外研究
Joseph Manu,Uma S Singh,Elizabeth Agboluaje et al.
Joseph Manu et al.
Gemcitabine (GEM) is a first line drug to treat pancreatic cancer (PC). However, its long-term efficacy and potency is plagued with reported chemoresistance. To circumvent this issue, the novel GEM analog called troxacitabine (TROX) was eva...
Design, synthesis and antibacterial activity of novel LpxC inhibitors containing 1,2,3-triazole moieties [0.03%]
含有1,2,3-三氮唑结构的新型LpxC抑制剂的设计、合成及抗菌活性研究
Fangyi Jiang,Chenghong Zheng,Ying Wang et al.
Fangyi Jiang et al.
Two series of N-aryl-L-threonine derivatives bearing a triazole fragment are described as LpxC inhibitors targeting Gram-negative pathogens. Most compounds demonstrated stronger antibacterial activities against E. coli (MICs: ≤0.03-16 μg/...
4-Aryl-2-aminoimidazole analogues of bromoageliferin with antimicrobial activity against Acinetobacter baumannii show in vitro inhibition of translocase MraY on the peptidoglycan biosynthesis pathway [0.03%]
具有抗菌活性的4-芳基-2-氨基咪唑溴化阿格尔伊芬类似物可抑制分隔酶MraY（肽聚糖生物合成途径中的一个成分）：体外研究结果
Roisin Murphy,Julia A Fairbairn,Becca W A Baileeves et al.
Roisin Murphy et al.
A series of 4-aryl-2-imidazoles containing an ortho-substituted benzyl substituent were designed as a new peptidomimetic scaffold for an Arg-Trp-x-x-Trp motif used by lysis protein E from bacteriophage φX174 to target translocase MraY on t...
Discovery of C-9 boronated berberine derivatives with enhanced selectivity against breast cancer [0.03%]
一种选择性更强的乳腺癌治疗药物——C-9硼基小檗碱衍生物的发现
Ying-Hao Liao,Yu-Jiao Wang,Jin-Qi Wang et al.
Ying-Hao Liao et al.
A series of eighteen berberine derivatives were designed and synthesized via molecular hybridization, introducing boronic acid/ester pharmacophores at the C-9 position to improve the selectivity of the natural product against breast cancer....