Considering Rotatability of Hydroxyl Groups for the Active Site Residues of MMP-13 in Retrospective Virtual Screening Campaigns [0.03%]
考虑MMP-13活性位点残基的羟基旋转性以进行回顾性虚拟筛选研究
Jamal Shamsara
Jamal Shamsara
Considering different orientation of hydroxyl and thiol groups of receptor residues such as Thr, Tyr, Ser and Cys is an option available on Glide docking software. This is an attempt that can provide more realistic ligand-receptor interacti...
Design and Synthesis of Novel Arylketo-containing P1-P3 Linked Macro-cyclic BACE-1 Inhibitors [0.03%]
新型芳基酮类P1-P3连接环肽类BACE-1抑制剂的设计与合成
Veronica Sandgren,Oscar Belda,Ingemar Kvarnström et al.
Veronica Sandgren et al.
A series of arylketo-containing P1-P3 linked macrocyclic BACE-1 inhibitors were designed, synthesized, and compared with compounds with a previously known and extensively studied corresponding P2 isophthalamide moiety with the aim to improv...
Use & Misuse of Water-filtered Tobacco Smoking Pipes in the World. Consequences for Public Health, Research & Research Ethics [0.03%]
关于水过滤烟草烟斗的使用与误用及其对全球公共卫生、研究和科研伦理的影响
Kamal Chaouachi
Kamal Chaouachi
Background: The traditional definition of an "epidemic" has been revisited by antismoking researchers. After 400 years, Doctors would have realized that one aspect of an ancient cultural daily practice of Asian and Africa...
Recent Progress in the Use of Glucagon and Glucagon Receptor Antago-nists in the Treatment of Diabetes Mellitus [0.03%]
近期有关胰高血糖素和胰高血糖素受体拮抗剂在糖尿病治疗中的应用进展
Mohamed Lotfy,Huba Kalasz,Gyorgy Szalai et al.
Mohamed Lotfy et al.
Glucagon is an important pancreatic hormone, released into blood circulation by alpha cells of the islet of Langerhans. Glucagon induces gluconeogenesis and glycogenolysis in hepatocytes, leading to an increase in hepatic glucose production...
Synthesis and Biological Evaluation of Macrocyclized Betulin Derivatives as a Novel Class of Anti-HIV-1 Maturation Inhibitors [0.03%]
茋类茋生物碱茋茋茋茋茋抗HIV-1成熟抑制剂的研究
Jun Tang,Stacey A Jones,Jerry L Jeffery et al.
Jun Tang et al.
A macrocycle provides diverse functionality and stereochemical complexity in a conformationally preorganized ring structure, and it occupies a unique chemical space in drug discovery. However, the synthetic challenge to access this structur...
Basic aspects of the pharmacodynamics of tolperisone, a widely applicable centrally acting muscle relaxant [0.03%]
托吡酯的药理学基本方面研究——一种广泛应用的中枢性肌肉松弛剂
Kornelia Tekes
Kornelia Tekes
Tolperisone (2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydro-chloride) was introduced in the clinical practice more than forty years ago and is still evaluated as a widely applicable compound in pathologically elevated skelet...
Nitropropenyl benzodioxole, an anti-infective agent with action as a protein tyrosine phosphatase inhibitor [0.03%]
硝基丙烯基苯并二氧六环一种具有蛋白质酪氨酸磷酸酶抑制作用的抗感染剂
Kylie S White,Gina Nicoletti,Robert Borland
Kylie S White
We report on the activities of a broad spectrum antimicrobial compound,nitropropenyl benzodioxole (NPBD) which are of relevance to its potential as an anti-infective drug. These investigations support the proposal that a major mechanism of ...
Synthesis of Some 4,5-Dihydrothieno[3,2-e][1,2,4]Triazolo[4,3-a] Pyrimi-dine-2-Carboxamides as Anti-Inflammatory and Analgesic Agents [0.03%]
合成一些具有抗炎和止痛作用的4,5-二氢噻唑并[3,2-e][1,2,4]三氮唑并[4,3-a]嘧啶-2-甲酰胺类化合物
Omaima G Shaaban,Ola H Rizk,Aida E Bayad et al.
Omaima G Shaaban et al.
A new series 4,5-dihydrothieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidine-2-carboxamide was synthesized. Twenty one newly synthesized compounds were investigated for their anti-inflammatory and analgesic activity using acute and subacute formal...
Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors [0.03%]
N4-磺胺基-琥珀酸、酞酰、丙烯酰和苯甲酰乙酸衍生物的设计、合成及作为潜在二肽基肽酶IV抑制剂的药理评价
Reema Abu Khalaf,Ghassan Abu Sheikha,Mahmoud Al-Sha&#x;er et al.
Reema Abu Khalaf et al.
As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein in...
Docking Studies of Methylthiomorpholin Phenols (LQM300 Series) with Angiotensin-Converting Enzyme (ACE) [0.03%]
甲基硫霉素酚(LQM300系列)与血管紧张素转换酶(ACE)对接研究
Víctor H Vázquez-Valadez,V H Abrego,Pablo A Martínez et al.
Víctor H Vázquez-Valadez et al.
A main target in the treatment of hypertension is the angiotensin-converting enzyme (ACE). This enzyme is responsible for producing angiotensin II, a potent vasoconstrictor. Therefore, one of the targets in the treatment of hypertension is ...