Protective effects of quercetin against inflammation and oxidative stress in a rabbit model of knee osteoarthritis [0.03%]
檞皮素对膝骨关节炎兔模型炎症及氧化应激的保护作用
Bing Wei,Yan Zhang,Lixia Tang et al.
Bing Wei et al.
Hit, Lead & Candidate Discovery This study investigated the effects of a natural phenolic compound quercetin on surgical-induced osteoarthritis (OA) in rabbits. Forty-eight New Zealand White rabbits were used to establish OA model by Hulth ...
Graph theoretical analysis, in silico modeling, prediction of toxicity, metabolism and synthesis of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl) phenyl) quinazolin-4(3H)-ones as NMDA receptor inhibitor [0.03%]
基于图论的分析、计算机建模及毒性代谢和合成一系列新的2-(甲基/苯基)-3-(4-(5-取代-1,3,4-噁二唑-2-基)苯基)喹唑啉-4(3H)-酮化合物作为NMDA受体抑制剂的性质预测
Govindaraj Saravanan,Theivendren Panneerselvam,Selvaraj Kunjiappan et al.
Govindaraj Saravanan et al.
Hit, Lead & Candidate Discovery A variety of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl)phenyl) quinazolin-4(3H)-ones have been synthesized by treating 3-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl)-2-(methyl/phenyl)-qu...
Alignment-based design and synthesis of new antimicrobial Aurein-derived peptides with improved activity against Gram-negative bacteria and evaluation of their toxicity on human cells [0.03%]
基于 alignment 的抗菌肽的设计、合成及其对革兰氏阴性菌的活性和人类细胞毒性的评价
Hamid Madanchi,Shabnam Akbari,Ali Akbar Shabani et al.
Hamid Madanchi et al.
Considering the worldwide increasing prevalence of resistance to traditional antibiotics, it is necessary to find new antibiotics to deal with this issue. Recently, antimicrobial peptides (AMPs) have been proposed as new antimicrobial agent...
Trichomonicidal activity of a new anthraquinone isolated from the roots of Morinda panamensis Seem [0.03%]
取自莫林达.panamensis Seems根部的一种新的蒽醌类化合物的特异性抗滴虫作用
David Cáceres-Castillo,Yussel Pérez-Navarro,Julio César Torres-Romero et al.
David Cáceres-Castillo et al.
Trichomoniasis, caused by the protozoan parasite Trichomonas vaginalis, is the most common nonviral sexually transmitted infection worldwide. Although drug treatment is available, unpleasant side effects and increased resistance to the nitr...
Design, synthesis, and biological evaluation of 1,8-naphthyridine glucosamine conjugates as antimicrobial agents [0.03%]
设计、合成及生物评估1,8-萘啶葡萄糖胺共轭物作为抗菌剂的研究
Aya A M Mohammed,Ghadeer A R Y Suaifan,Mayadah B Shehadeh et al.
Aya A M Mohammed et al.
In the quest for discovering potent antimicrobial agents with lower toxicity, we envisioned the design and synthesis of nalidixic acid-D-(+)-glucosamine conjugates. The novel compounds were synthesized and evaluated for their in vitro antim...
Synthesis, in vivo and in silico evaluation of novel 2,3-dihydroquinazolin-4(1H)-one derivatives as potential anticonvulsant agents [0.03%]
新型2,3-二氢喹唑啉-4(1H)-酮衍生物的合成及其体内和计算机评估作为潜在抗惊厥剂
Hend Kothayer,Samy M Ibrahim,Moustafa K Soltan et al.
Hend Kothayer et al.
In light of the pharmacophoric structural requirements for achieving anticonvulsant activity, a series of N-(1-methyl-4-oxo-2-un/substituted-1,2-dihydroquinazolin-3[4H]-yl)benzamide (4a-g) and N-(1-methyl-4-oxo-2-un/substituted-1,2-dihydroq...
Biocatalytic synthesis of diaryl disulphides and their bio-evaluation as potent inhibitors of drug-resistant Staphylococcus aureus [0.03%]
用于合成二芳基二硫化物的生物催化及作为耐药表皮葡萄球菌抑制剂的生物评价
Saima,Isha Soni,Aditya G Lavekar et al.
Saima et al.
Staphylococcus aureus is a WHO Priority II pathogen for its capability to cause acute to chronic infections and to resist antibiotics, thus severely impacting healthcare systems worldwide. In this context, it is urgently desired to discover...
Tadalafil: 15 years' journey in male erectile dysfunction and beyond [0.03%]
达拉菲尼亚：用于男性勃起功能障碍及其它适应症的15年研究历程
Nermin S Ahmed
Nermin S Ahmed
Hit, Lead & Candidate Discovery Tadalafil, Cialis, Eli Lilly & Co./ICOS, (6R,12aR)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6] pyrido[3,4-b]indole-1,4-dione, was first discovered in 2003. It was reported to...
Bedaquiline and delamanid in the treatment of multidrug-resistant tuberculosis: Promising but challenging [0.03%]
贝达喹啉和德拉马尼治疗耐多药结核病：前景与挑战共存
Yang Li,Feng Sun,Wenhong Zhang
Yang Li
Improving treatment outcomes in multidrug-resistant tuberculosis (MDR-TB) is partly hampered by inadequate effective antitubercular agents. Development of bedaquiline and delamanid has potentially changed the treatment landscape for MDR-TB....
David Gurwitz
David Gurwitz