Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent [0.03%]
一种新型1,2,4-三唑-吲哚杂化分子抗真菌剂的生物研究
Fabrice Pagniez,Nicolas Lebouvier,Young Min Na et al.
Fabrice Pagniez et al.
(2-(2,4-Dichlorophenyl)-3-(1H-indol-1-yl)-1-(1,2,4-1H-triazol-1-yl)propan-2-ol (8 g), a new 1,2,4-triazole-indole hybrid molecule, showed a broad-spectrum activity against Candida, particularly against low fluconazole-susceptible species. I...
N-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation [0.03%]
N-单芳基乙酰噻二脲类尿素酶抑制剂：合成、结构活性关系及生物评价
Wei-Yi Li,Wei-Wei Ni,Ya-Xi Ye et al.
Wei-Yi Li et al.
A urease inhibitor with good in vivo profile is considered as an alternative agent for treating infections caused by urease-producing bacteria such as Helicobacter pylori. Here, we report a series of N-monosubstituted thioureas, which act a...
Design, synthesis and biological evaluation of carbohydrate-based sulphonamide derivatives as topical antiglaucoma agents through selective inhibition of carbonic anhydrase II [0.03%]
基于糖类的磺酰胺衍生物的设计、合成及生物学评价作为通过选择性抑制碳酸酐酶II的抗青光眼药物研究
Zhuang Hou,Chuanchao Li,Yichuang Liu et al.
Zhuang Hou et al.
A series of new carbohydrate-based sulphonamide derivatives were designed, synthesised by employing the so-call 'sugar-tail' approach. The compounds were evaluated in vitro against a panel of CAs. Compared to their parent compound p-sulfamo...
A potentiated cooperation of carbonic anhydrase IX and histone deacetylase inhibitors against cancer [0.03%]
碳酐酶IX与组蛋白脱乙酰酶抑制剂联合用于癌症治疗
Jessica Ruzzolini,Anna Laurenzana,Elena Andreucci et al.
Jessica Ruzzolini et al.
The emergence of tumour recurrence and resistance limits the survival rate for most tumour-bearing patients. Only, combination therapies targeting pathways involved in the induction and in the maintenance of cancer growth and progression mi...
Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1 H- pyrazole derivatives as a novel selective inhibitor scaffold of JNK3 [0.03%]
一类新型的选择性JNK3抑制剂骨架3-烷基-5-芳基-1-吡啶甲酰基-1H-吡唑衍生物的发现
Youri Oh,Miyoung Jang,Hyunwook Cho et al.
Youri Oh et al.
3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives were designed and synthesised as selective inhibitors of JNK3, a target for the treatment of neurodegenerative diseases. Following previous studies, we have designed JNK3 inhibitors to redu...
Inhibition survey with phenolic compounds against the δ- and η-class carbonic anhydrases from the marine diatom thalassiosira weissflogii and protozoan Plasmodium falciparum [0.03%]
用酚类化合物抑制海洋羽纹纲藻塔花束藻和疟原虫科恶性疟原虫的δ-η碳酸酐酶
Siham A Alissa,Hanan A Alghulikah,Zeid A ALOthman et al.
Siham A Alissa et al.
The inhibition of δ- and η-class carbonic anhydrases (CAs; EC 4.2.1.1) was poorly investigated so far. Only one δ-CA, TweCA from the diatom Thalassiosira weissflogii, and one η-CA, PfCA, from Plasmodium falciparum, have been cloned and ...
Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer's disease [0.03%]
设计、合成及体内外评价新型苯基哌啶类乙醇胺衍生物作为治疗阿尔茨海默病的胆碱酯酶抑制剂
Jun Mo,Tingkai Chen,Hongyu Yang et al.
Jun Mo et al.
Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer's disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the s...
Development of a cheminformatics platform for selectivity analyses of carbonic anhydrase inhibitors [0.03%]
碳酸酐酶抑制剂选择性分析的化学信息学平台开发
Giulio Poli,Salvatore Galati,Adriano Martinelli et al.
Giulio Poli et al.
The selectivity for a specific human Carbonic Anhydrase (hCA) isoform is an important property a hCA inhibitor (CAI) should be endowed with, in order to constitute a valuable therapeutic tool for the treatment of a desired pathology. In thi...
New flavonoid - N, N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic properties [0.03%]
新的黄酮-N,N-二苄基（N-甲基）胺杂化物：具有神经发生特性的阿尔茨海默病多靶向药物
Martín Estrada-Valencia,Clara Herrera-Arozamena,Concepción Pérez et al.
Martín Estrada-Valencia et al.
The design of multi-target directed ligands (MTDLs) is a valid approach for obtaining effective drugs for complex pathologies. MTDLs that combine neuro-repair properties and block the first steps of neurotoxic cascades could be the so long ...
Towards discovery of novel scaffold with potent antiangiogenic activity; design, synthesis of pyridazine based compounds, impact of hinge interaction, and accessibility of their bioactive conformation on VEGFR-2 activities [0.03%]
具有强抗血管生成活性的新型支架的发现；基于吡嗪类化合物的设计与合成，铰链相互作用以及其生物活性构象对VEGFR-2活性的可及性的影响
Maiy Y Jaballah,Rabah A T Serya,Nasser Saad et al.
Maiy Y Jaballah et al.
Pyridazine scaffolds are considered privileged structures pertaining to its novelty, chemical stability, and synthetic feasibility. In our quest towards the development of novel scaffolds for effective vascular endothelial growth 2 (VEGFR-2...