Design, synthesis, molecular docking study and molecular dynamics simulation of new coumarin-pyrimidine hybrid compounds having anticancer and antidiabetic activity [0.03%]
设计、合成及分子对接和动力学模拟新型香豆素-嘧啶杂化抗肿瘤及抗糖尿病化合物
Duong Ngoc Toan,Nguyen Dinh Thanh,Mai Xuan Truong et al.
Duong Ngoc Toan et al.
Coumarin-pyrimidine hybrid compounds were synthesized by condensation reaction of α,β-unsaturated ketones of 6-acetyl-5-hydroxy-4-methylcoumarin with guanidine. The reaction yields were of 42-62%. The antidiabetic and anticancer activitie...
N-arylated oxathiazinane heterocycles are convenient synthons for 1,3-amino ethers and 1,3-amino thioethers [0.03%]
N-芳基化氧噻嗪烷杂环是1,3-氨基醚和1,3-氨基硫代醚的合成子
Anand H Shinde,Someshwar Nagamalla,Shyam Sathyamoorthi
Anand H Shinde
This communication describes a variety of nucleophilic ring openings of N-arylated oxathiazinane heterocycles. We find that this reaction is compatible with phenoxides, naphthoxides, and thiolates and allows for the rapid assembly of N-aryl...
Novel MreB inhibitors with antibacterial activity against Gram (-) bacteria [0.03%]
具有抗革兰氏阴性菌活性的新MreB抑制剂
Hye Yeon Sagong,Jesus D Rosado-Lugo,Eric J Bryan et al.
Hye Yeon Sagong et al.
MreB is a cytoskeleton protein present in rod-shaped bacteria that is both essential for bacterial cell division and highly conserved. Because most Gram (-) bacteria require MreB for cell division, chromosome segregation, cell wall morphoge...
Combination with a FtsZ inhibitor potentiates the in vivo efficacy of oxacillin against methicillin-resistant Staphylococcus aureus [0.03%]
新型抗生素组合可增强苯唑西林对耐甲氧西林金黄色葡萄球菌的体内疗效研究
Malvika Kaul,Edgar Ferrer-González,Lilly Mark et al.
Malvika Kaul et al.
Oxacillin is a first-line antibiotic for the treatment of methicillin-sensitive Staphylococcus aureus (MSSA) infections but is ineffective against methicillin-resistant S. aureus (MRSA) due to resistance. Here we present results showing tha...
Synthesis and biological evaluation of esculetin derivatives as potential anti-HBV agents [0.03%]
一种新型Esculetin衍生物的合成及其抗HBV活性研究
Zhen Ye,Tong-Shi-Yao Zhao,Shan-Bin Li et al.
Zhen Ye et al.
Previous in vivo and in vitro studies revealed that esculetin (Fig. 1) has anti-hepatitis B virus (anti-HBV) activity as well as a protective effect on liver damage caused by duck hepatitis B virus. We designed and synthesized a series of e...
Design, synthesis, and biological evaluation of new 2-(4-(methylsulfonyl)phenyl)- N-phenylimidazo[1,2- a]pyridin-3-amine as selective COX-2 inhibitors [0.03%]
新型选择性环氧化酶-2抑制剂2-[4-(甲磺酰基)苯基]-N-苯基咪唑并[1,2-a]吡啶-3-胺的设计、合成及药理学研究
Mahsa Azami Movahed,Fatemeh Khadem Abbasi,Mahsa Rajabi et al.
Mahsa Azami Movahed et al.
Cyclooxygenase (COX), which plays a role in converting arachidonic acid to inflammatory mediators, could be inhibited by non-steroidal anti-inflammatory drugs (NSAIDs). Although potent NSAIDs are available for the treatment of pain, fever, ...
Design, synthesis and anti-breast cancer properties of butyric ester tethered dihydroartemisinin-isatin hybrids [0.03%]
丁香酸素连接双氢青蒿素-异咯嗪衍生物的设计、合成及其抗乳腺癌活性研究
Shijia Zhao,Xiaoyan Zhang,Min Tang et al.
Shijia Zhao et al.
Fifteen novel butyric ester tethered dihydroartemisinin-isatin hybrids 4a-d and 5a-k were designed, synthesized, and evaluated for cytotoxicity against four human breast cancer cell lines, including MCF-7, MDA-MB-231, MCF-7/ADR and MDA-MB-2...
Novel Benzo[4,5]imidazo[1,2- a]pyrimidine derivatives as selective Cyclooxygenase-2 Inhibitors: Design, synthesis, docking studies, and biological evaluation [0.03%]
新型苯并[4,5]咪唑[1,2-a]嘧啶衍生物作为选择性环氧合酶-2抑制剂：设计、合成、对接研究及生物活性评价
Maryam Bayanati,Mona Khoramjouy,Mehrdad Faizi et al.
Maryam Bayanati et al.
The present study was aimed at the synthesis and evaluation of a new series of benzo[4,5]imidazo[1,2-a]pyrimidine having a methylsulfonyl group as COX-2 (cyclooxygenase-2) inhibitor pharmacophore. Molecular modeling studies were performed u...
M Dhanalakshmi,D Sruthi,K R Jinuraj et al.
M Dhanalakshmi et al.
There are a plethora of antibiotic resistance cases and humans are marching towards another big survival test of evolution along with drastic climate change and infectious diseases. Ever since the first antibiotic [penicillin], and the myri...
Evaluation of a series of nucleoside analogs as effective anticoronaviral-2 drugs against the Omicron-B.1.1.529/BA.2 subvariant: A repurposing research study [0.03%]
核苷类似物系列作为有效抗冠状病毒-2药物对Omicron-B.1.1.529/BA.2亚变体的评价：一种新药研究
Amgad M Rabie,Mohnad Abdalla
Amgad M Rabie
Mysterious evolution of a new strain of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the Omicron variant, led to a new challenge in the persistent coronavirus disease 2019 (COVID-19) battle. Objecting the conserved SARS...