Samuel A Kirby,Cynthia S Dowd
Samuel A Kirby
Phosphoryl prodrugs are key compounds in drug development. Biologically active phosphoryl compounds often have negative charges on the phosphoryl group, and as a result, frequently have poor pharmacokinetic (PK) profiles. The use of lipophi...
Design and discovery of a high affinity, selective and β-arrestin biased 5-HT7 Receptor Agonist [0.03%]
高选择性、偏向性的五羟色胺7受体激动剂的设计与发现
Edem K Onyameh,Edward Ofori,Barbara A Bricker et al.
Edem K Onyameh et al.
Compound 1c, 5-chloro-2-(2-(3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing high affinity binding to the 5-HT7 receptor (Ki = 0.5 nM). However, compound 1c racemizes read...
Michael S Wolfe
Michael S Wolfe
Familial Alzheimer's disease (FAD) is a rare early-onset genetic form of a common dementia of old age. Striking in middle age, FAD is caused by missense mutations in three genes: APP (encoding the amyloid precursor protein) and PSEN1 and PS...
Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues [0.03%]
lifitegrast类似物的设计、合成及LFA-1/ICAM-1拮抗活性评价
Guoxin Du,Weiwei Du,Yuanlong An et al.
Guoxin Du et al.
The interaction between Lymphocyte function-associated antigen 1 (LFA-1) and intercellular-adhesion molecule-1 (ICAM-1) plays important roles in the cell-mediated immune response and inflammation associated with dry eye disease. LFA-1/ICAM-...
Synthesis and antitumor activity of novel silibinin and 2,3-dehydrosilybin derivatives with carbamate groups [0.03%]
具有碳酰胺基团的新木犀草素和2,3-去氢木犀草素衍生物的合成及抗肿瘤活性研究
Qiuchan Wu,Jiang Zeng,Jinfu Dong
Qiuchan Wu
A novel series of silibinin and 2,3-dehydrosilybin derivatives bearing carbamate groups were designed, synthesized and their in vitro anticancer activities were screened against human cancer cell lines including MCF-7, NCI-H1299, HepG2 and ...
Synthesis and antiplasmodial assessment of nitazoxanide and analogs as new antimalarial candidates [0.03%]
硝唑尼德及其类似物的合成与抗疟活性评估
Camila Irabuena,Laura Scarone,Guilherme Eduardo de Souza et al.
Camila Irabuena et al.
During the last years, the progression to control malaria disease seems to be slowed and WHO (World Health Organization) reported a modeling analysis with the prediction of the increase in malaria morbidity and mortality in sub-Saharan Afri...
Isatin derivatives as broad-spectrum antiviral agents: the current landscape [0.03%]
异丙薁衍生物作为广谱抗病毒药物：现状分析
Tilal Elsaman,Malik Suliman Mohamed,Eyman Mohamed Eltayib et al.
Tilal Elsaman et al.
In recent decades, several viruses have resulted in large outbreaks with serious health, economic and social consequences. The current unprecedented outbreak of the new coronavirus, SARS-COV-2, necessitates intensive efforts for delivering ...
Synthesis and biological evaluation of (20 S,24 R)-epoxy-dammarane-3β,12β,25-triol derivatives as α-glucosidase and PTP1B inhibitors [0.03%]
(20 S,24 R)-环氧齐墩果烷-3β,12β,25-三醇衍生物作为α-葡萄糖苷酶和PTP1B抑制剂的合成及生物活性评价
Xiao-Tong Yang,Tian-Ze Li,Chang-An Geng et al.
Xiao-Tong Yang et al.
The dammarane triterpenoid (20S,24R)-epoxy-dammarane-3β,12β,25-triol obtained from Cyclocarya paliurus in our previous study showed inhibitory activity on α-glucosidase in vitro with an inhibitory ratio of 32.2% at the concentration of 2...
Review on molnupiravir as a promising oral drug for the treatment of COVID-19 [0.03%]
莫努匹拉韦治疗新冠肺炎潜力口服药物研究进展及相关思考综述
Elham Zarenezhad,Mahrokh Marzi
Elham Zarenezhad
During the COVID-19 pandemic, various drug candidates have been developed, molnupiravir (MK-4482 and EIDD-2801), which is a new orally anti-viral agent under development for the treatment of COVID-19, is under study in the final stage of th...
A review of natural products, their effects on SARS-CoV-2 and their utility as lead compounds in the discovery of drugs for the treatment of COVID-19 [0.03%]
天然产物的综述：其对SARS-CoV-2的影响及其作为先导化合物在COVID-19治疗药物发现中的应用价值
Robert L Chapman,Shridhar V Andurkar
Robert L Chapman
During the COVID-19 pandemic lasting now for well more than a year, nearly 247 million cases have been diagnosed and over 5 million deaths have been recorded worldwide as of November 2021. The devastating effects of the SARS-CoV-2 virus on ...