In vivo- and in silico-driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors [0.03%]
体内和计算机辅助的新喹唑啉类抗惊厥和AMPA受体抑制剂的设计合成与活性研究
Hamada S Abulkhair,Salwa Elmeligie,Adel Ghiaty et al.
Hamada S Abulkhair et al.
The lack of effective therapies for epileptic patients and the potentially harmful consequences of untreated seizure incidents have made epileptic disorders in humans a major health concern. Therefore, new and more potent anticonvulsant dru...
A triple-targeting inhibitory activity of Rose Bengal on polysaccharide biosynthesis of Burkholderia pseudomallei [0.03%]
玫瑰精通过三重抑制作用抑制贝氏疏螺旋体多糖生物合成活性
Suwon Kim,Seri Jo,Mi-Sun Kim et al.
Suwon Kim et al.
Sugar nucleotidyltransferases (SNTs) participate in various biosynthesis pathways constructing polysaccharides in Gram-negative bacteria. In this study, a triple-targeting inhibitory activity of Rose Bengal against SNTs such as d-glycero-α...
Discovery of novel triazolophthalazine derivatives as DNA intercalators and topoisomerase II inhibitors [0.03%]
新型三唑菲唑啉类DNA嵌入剂和拓扑异构酶II抑制剂的发现
Helmy Sakr,Rezk R Ayyad,Ali A El-Helby et al.
Helmy Sakr et al.
A new series of triazolophthalazine derivatives was designed and synthesized as topoisomerase II (Topo II) inhibitors and DNA intercalators. The synthesized derivatives were evaluated in vitro for their cytotoxic activities against three hu...
Synthesis, docking studies, and pharmacological evaluation of 2-hydroxypropyl-4-arylpiperazine derivatives as serotoninergic ligands [0.03%]
2-羟丙基-4-芳基哌嗪衍生物作为血清素受体配体的合成、对接研究和药理学评价
Elisa Magli,Ewa Kędzierska,Agnieszka A Kaczor et al.
Elisa Magli et al.
A new series of norbornene and exo-N-hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboximide derivatives was prepared, and their affinities to the 5-HT1A , 5-HT2A , and 5-HT2C receptors were evaluated and compared with a previously synthesi...
Design, synthesis, molecular docking, and some metabolic enzyme inhibition properties of novel quinazolinone derivatives [0.03%]
新型喹唑啉酮衍生物的设计、合成、分子对接及其部分代谢酶抑制性能研究
Feyzi S Tokalı,Parham Taslimi,İbrahim H Demircioğlu et al.
Feyzi S Tokalı et al.
3-Amino-2-ethylquinazolin-4(3H)-one (3) was synthesized in two steps from the reaction of amide (2), which was obtained from the treatment of methyl anthranilate (1) with propionyl chloride, with hydrazine. From the reaction of 3-amino-2-et...
Natural cyclic polypeptides as vital phytochemical constituents from seeds of selected medicinal plants [0.03%]
来源于药用植物种子的天然环肽类植化成分研究进展
Rajiv Dahiya,Sunita Dahiya,Jyoti Shrivastava et al.
Rajiv Dahiya et al.
Cyclopolypeptides are among the most predominant biomolecules in nature, especially those derived from plant seeds. This category of compounds has gained extraordinary attention due to remarkable variety of structures and valuable biofuncti...
Design, synthesis, and biological evaluation of new urolithin amides as multitarget agents against Alzheimer's disease [0.03%]
设计、合成及生物活性评价新型鞣皮素酰胺类化合物作为抗阿尔茨海默病多功能靶向药物
Karar T Shukur,Tugba Ercetin,Chiara Luise et al.
Karar T Shukur et al.
A series of urolithin amide (i.e., URO-4-URO-10 and THU-4-THU-10) derivatives was designed and synthesized, and their chemical structures were confirmed with spectroscopic techniques and elemental analysis. The title compounds and synthesis...
Synthesis of N-alkylated pyrazolo[3,4-d]pyrimidine analogs and evaluation of acetylcholinesterase and carbonic anhydrase inhibition properties [0.03%]
N-烷基化吡唑并[3,4-d]嘧啶类似物的合成及乙酰胆碱酯酶和碳酸酐酶抑制作用评价
Busra O Aydin,Derya Anil,Yeliz Demir
Busra O Aydin
Fused pyrimidines, especially pyrazolo[3,4-d]pyrimidines, are among the most preferred building blocks for pharmacology studies, as they exhibit a broad spectrum of biological activity. In this study, new derivatives of pyrazolo[3,4-d]pyrim...
Synthesis and in vitro antileishmanial efficacy of novel benzothiadiazine-1,1-dioxide derivatives [0.03%]
新型苯并噻二嗪-1,1-二氧化物衍生物的合成及其体外抗利什曼病活性研究
Daisy K Mangwegape,Nonkululeko H Zuma,Janine Aucamp et al.
Daisy K Mangwegape et al.
Leishmaniasis is a major vector-borne parasitic disease that affects thousands of people in tropical and subtropical developing countries. In 2019 alone, it killed 26,000-65,000 individuals. Leishmaniasis is curable, yet its eradication and...
Phytochemical characterization and effects on cell proliferation of Pinus nigra Arn. bark [0.03%]
Pinus nigra Arn.树皮的植化分析及其对细胞增殖的影响
Nataša Milić,Maja Milanović,Dragana Četojević-Simin et al.
Nataša Milić et al.
Pinus nigra Arn. bark extracts from Mokra gora (MG) and Tara mountains were analyzed with regard to their polyphenolic profile and antioxidative and antiproliferative activity. The ethanol extract from MG showed the highest phenolic, flavon...