Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines [0.03%]
一些具有支气管扩张活性的新型6-烷基/芳基-1,2,4-三氮杂萘并喹唑啉衍生物的合成及药理研究
Rajan Subramanian Kombu,Raghu Prasad Mailavaram,Harikrishna Devalapally et al.
Rajan Subramanian Kombu et al.
A series of alkyl- and aryl-1,2,4-triazino[4,3-c]quinazolines (5a-h and 8a-h) were synthesized and characterized. The title compounds were evaluated for their in vivo bronchodilator activity on guinea pigs. All the test compounds exhibited ...
The utility of oligopeptidase in brain-targeting delivery of an enkephalin analogue by prodrug design [0.03%]
通过前药设计利用寡肽酶实现脑靶向递送阿片肽类似物的功效研究
K Prokai-Tatrai,H-S Kim,L Prokai
K Prokai-Tatrai
In a brain-targeting prodrug approach for a metabolically stable enkephalin analogue DADLE, specific enzymes are utilized for in vivo prodrug activation. Prolyl oligopeptidase (POP) may be especially useful in this regard. In vitro metaboli...
Design of anticancer agents utilizing streptozocin for in silico optimization of properties and pattern recognition identification of group features [0.03%]
基于streptozocin的抗肿瘤药物设计及群体特征的模式识别研究
Ronald Bartzatt
Ronald Bartzatt
Streptozocin has been shown to be useful in the clinical treatment of malignant neuroendocrine tumors of the pancreas. The poor prognosis for patients having malignant tumors of pancreas suggests the investigation and development of new the...
The investigation of structure-activity relationships of tacrine analogues: electronic-topological method [0.03%]
电子拓扑方法研究Tacrine类似物的构效关系
Murat Saracoglu,Fatma Kandemirli
Murat Saracoglu
In this study we investigated the structure-activity relationships by using the Electron- Topological Method (ETM) for a class of AChE inhibitors related to tacrine (9-amino-1,2,3,4-tetrahydroacridine) and 11 H-Indeno-[1,2-b]-quinolin-10-yl...
A New Method for Radiosynthesis of C-Labeled Carbamate Groups and its Application for a Highly Efficient Synthesis of the Kappa-Opioid Receptor Tracer [C]GR103545 [0.03%]
一种合成C标记碳酰胺的新方法及应用于高效制备κ-阿片受体示踪剂[C]GR103545tracer的研究
B W Schoultz,E Arstad,J Marton et al.
B W Schoultz et al.
(11)C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO(2) and (11)C-methylation reagents. [(11)C]Methyl-triflate mediated methylation of carbamino adducts provides the correspo...
Transcorneal permeation in a corneal device of non-steroidal anti-inflammatory drugs in drug delivery systems [0.03%]
药物传递系统中非甾体类抗炎药在角膜装置中的角膜透入性研究
R Valls,E Vega,M L Garcia et al.
R Valls et al.
This work is focused on the ex vivo study of corneal permeation of two anti-inflammatory drugs: diclofenac, and flurbiprofen (as a model of hydrophilic and lipophilic drug, respectively) loaded to cyclodextrins or polymeric nanoparticles in...
A new concept for smart drug delivery: adhesion induced nanovector implosion [0.03%]
一种智能药物输送的新概念：粘附诱导的纳米载体崩解现象
Nicola M Pugno
Nicola M Pugno
In this paper we show that controlling adhesion in highly flexible nanovectors can help in smartly delivering the drug. The high flexibility of the nanovector is used to smartly deliver the drug only at the target site by the new concept of...
M A Abdullah,Anisa Ur Rahmah,A J Sinskey et al.
M A Abdullah et al.
Biopharmaceuticals are often produced by recombinant E. coli or mammalian cell lines. This is usually achieved by the introduction of a gene or cDNA coding for the protein of interest into a well-characterized strain of producer cells. Natu...
Identification and characterization of skin biomolecules for drug targeting and monitoring by vibrational spectroscopy [0.03%]
用于药物靶向和监测的皮肤生物分子的鉴定与特征分析——通过振动光谱法研究
Natalja Skrebova Eikje,Katsuo Aizawa,Takayuki Sota et al.
Natalja Skrebova Eikje et al.
The article discusses the application of vibrational spectroscopy techniques for in vivo identification and characterization of glucose biomolecules monitored in the skin of healthy, prediabetes and diabetes subjects; for molecular characte...
Microwave-Assisted Syntheses of Amino Acid Ester Substituted Benzoic Acid Amides: Potential Inhibitors of Human CD81-Receptor HCV-E2 Interaction [0.03%]
微波促进的氨基酸酯取代苯甲酰胺衍生物的合成及其对人CD81受体-HCV E2蛋白相互作用的抑制活性研究
Marcel Holzer,Sigrid Ziegler,Bernd Kronenberger et al.
Marcel Holzer et al.
Results from our group showed benzyl salicylate to be a moderate inhibitor of the CD81-LEL-HCV-E2 interaction. To increase the biological activity, heterocyclic substituted benzoic acids were coupled to amino acid esters via microwave assis...