CO prodrugs: A new scaffold of adamantane-fused norbornen-7-ones with tunable water solubility [0.03%]
含金刚烷并诺硼烯酮衍生物的CO前药类化合物及其制备和应用
Ce Yang,Xingyue Ji,G S Sainaga Jyothi Vaskuri et al.
Ce Yang et al.
We have had a long-standing interest in developing organic prodrugs for controlled delivery of CO for various therapeutic applications. Based on an earlier approach of taking advantage of a cheletropic extrusion reaction of norbornadienone ...
Targeting cAMP signaling and phosphodiesterase 4 for liver disease treatment [0.03%]
瞄准cAMP信号传导和磷酸二酯酶4以治疗肝病
Jingyi Ma,Dalton W Staler,Ram I Mahato
Jingyi Ma
Liver disease is a significant health burden globally and accounts for 4% of total deaths annually. Alcoholic liver disease (ALD) and metabolism-associated fatty liver disease (MAFLD) are the leading causes of cirrhosis. Extensive studies h...
Iron Porphyrin-mediated Production of Carbon Monoxide from Phenylpyruvic Acid: From Potential Therapeutic and Diagnostic Use to Physiological Implications [0.03%]
铁泊酚介导的苯丙酮酸生成一氧化碳：从潜在的治疗和诊断应用到生理意义
Wen Lu,Rujuta Ghorpade,Xiaoxiao Yang et al.
Wen Lu et al.
Because of CO's known endogenous signaling roles and its demonstrated pharmacological activity at low and safe concentrations, there is considerable interest in chemical strategies that allows for generation of carbon monoxide from organic ...
Quinazolinone-based Subchemotypes for Targeting HIV-1 Capsid Protein: Design and Synthesis [0.03%]
基于喹唑啉酮的HIV-1衣壳蛋白靶向亚化学型的设计与合成
Thamina Akther,William M McFadden,Huanchun Zhang et al.
Thamina Akther et al.
The recent FDA-approval of lenacapavir (LEN, GS-6207) and the subsequent discovery of GSK878 strongly validate HIV-1 capsid protein (CA) as a target for antiviral development. However, multiple single mutations drastically reduced the susce...
A novel class of indole derivatives: enhanced bioavailability, permeability, and antioxidant efficacy for thromboembolic disease therapy [0.03%]
吲哚衍生物的新颖类别：提高血栓栓塞性疾病疗法的生物利用度、渗透性和抗氧化功效
Srinivas Rao Mandalapu,Shanshan Hou,Steffen Jockusch et al.
Srinivas Rao Mandalapu et al.
Free radicals like reactive oxygen species (ROS) and reactive nitrogen species (RNS) cause cellular damage and contribute to thromboembolic diseases by promoting platelet activation and aggregation. Compounds that scavenge free radicals can...
Shyam Sathyamoorthi,Steven P Kelley
Shyam Sathyamoorthi
We have developed convenient protocols for alkene disulfonoxylation, which involve stirring alkene substrate with a commercial I(III) oxidant and sulfonic acid in CH2Cl2 at ambient temperature. The reactions can be performed open to air wit...
Structure-activity relationships and pharmacokinetic evaluation of L-cystine diamides as L-cystine crystallization inhibitors for cystinuria [0.03%]
L-胱氨酸二酰胺类化合物的构效关系及其抑制胱氨酸尿症中L-胱氨酸结晶的作用和药代动力学评价
Longqin Hu,Haifa Albanyan,Jeffrey Yang et al.
Longqin Hu et al.
Cystinuria is a rare genetic disorder characterized by defective l-cystine reabsorption from the renal proximal tubule, resulting in abnormally high concentrations of L-cystine and subsequent l-cystine crystallization and stone formation in...
Di Bai,Hyunjung Kim,Pengfei Wang
Di Bai
Many natural saponins demonstrate immunostimulatory adjuvant activities, but they also have some inherent drawbacks that limit their clinical use. To overcome these limitations, extensive structure-activity-relationship (SAR) studies have b...
Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction [0.03%]
作为aurora a激酶抑制剂和SARS-CoV-2刺突/宿主ACE2相互作用抑制剂的新型呫吨酮衍生物的设计、合成及生化与计算筛选
Donatus B Eni,Joel Cassel,Cyril T Namba-Nzanguim et al.
Donatus B Eni et al.
Isatin (indol-2,3-dione), a secondary metabolite of tryptophan, has been used as the core structure to design several compounds that have been tested and identified as potent inhibitors of apoptosis, potential antitumor agents, anticonvulsa...
RF-3192C and other polyketides from the marine endophytic Aspergillus niger ASSB4: structure assignment and bioactivity investigation [0.03%]
由海洋内生菌Aspergillus niger ASSB4产生的RF-3192C及其他多酮类化合物的结构鉴定及生物活性研究
Manar M Mahmoud,Ahmed S Abdel-Razek,Abdelaaty Hamed et al.
Manar M Mahmoud et al.
Chemical investigation of the methanolic extract of endophytic Aspergillus niger SB4, isolated from the marine alga Laurencia obtuse, afforded the pentacyclic polyketide, RF-3192C (1), the dimeric coumarin orlandin (2), fonsecin B (3), TMC-...