A3 Adenosine Receptors: Protective vs. Damaging Effects Identified Using Novel Agonists and Antagonists [0.03%]
A3腺苷受体：利用新型激动剂和拮抗剂确定其保护作用与损伤作用
Kenneth A Jacobson,Stefano Moro,Yong-Chul Kim et al.
Kenneth A Jacobson et al.
Investigation of the physiologic role of the A3 adenosine receptor has been facilitated by the availability of selective agonists and antagonists. Selective agonists include IB-MECA and the 2-chloro derivative Cl-IB-MECA. Selective antagoni...
Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization [0.03%]
药剂学结晶中初级异质形核的新兴作用
Samarth D Thakore,Aaruti Sood,Arvind K Bansal
Samarth D Thakore
Crystallization is an important and difficult to control unit operation in the pharmaceutical industry. Crystallization can control molecular (i.e., polymorphism) and particulate (i.e., particle size and crystal habit) properties of active ...
Synthesis and antimicrobial evaluation of piperic acid amides and their lower homologues [0.03%]
毕拔酸酰胺及其低级同类物的合成及抗菌活性评价
Prabhakar S Achanta,Sneha Raj,Soyar Horam et al.
Prabhakar S Achanta et al.
Seven piperic acid amides along with their lower homologs (12) were synthesized using HATU-DIPEA coupling reagent. All the synthesized derivatives were evaluated for their antibacterial activities against Staphylococcus aureus, Pseudomonas ...
Comparative Study
Drug development research. 2020 May;81(3):366-373. DOI:10.1002/ddr.21630 2020
New 3-unsubstituted isoxazolones as potent human neutrophil elastase inhibitors: Synthesis and molecular dynamic simulation [0.03%]
一类新的3-位未取代异噁唑酮类人中性粒细胞弹性蛋白酶抑制剂的分子动力学模拟及其合成研究
Maria Paola Giovannoni,Letizia Crocetti,Niccolò Cantini et al.
Maria Paola Giovannoni et al.
Human neutrophil elastase (HNE) is a proteolytic enzyme belonging to the serine protease family and is involved in a variety of pathologies. Thus, compounds able to inhibit HNE represent promising therapeutics for the treatment of inflammat...
Substituted chloroacetamides as potential cancer stem cell inhibitors: Synthesis and biological evaluation [0.03%]
氯乙酰胺类癌症干细胞抑制剂的合成和生物活性研究
Komal N Padhariya,Maithili Athavale,Sangeeta Srivastava et al.
Komal N Padhariya et al.
Cancer kills, irrespective of geographical and cultural origin. Novel modalities for treating cancer are desperately needed. Cancer stem cells (CSCs), main culprits behind chemoresistance and tumor relapse, are one of the few logical choice...
Molecular signaling of G-protein-coupled receptor in chronic heart failure and associated complications [0.03%]
慢性心力衰竭及其相关并发症中的G蛋白偶联受体分子信号通路
Mohammad Altamish,Vijaya Paul Samuel,Rajiv Dahiya et al.
Mohammad Altamish et al.
The well-known condition of heart failure is a clinical syndrome that results when the myocardium's ability to pump enough blood to meet the body's metabolic needs is impaired. Most of the cardiac activity is maintained by adrenoceptors, ar...
Folic acid-conjugated raloxifene hydrochloride carbon nanotube for targeting breast cancer cells [0.03%]
叶酸偶联的人纤细碳纳米管载氯甲他香抗乳腺癌细胞的研究
Nadrajan Jawahar,Aninidta De,Selveraj Jubee et al.
Nadrajan Jawahar et al.
Breast cancer is one of the leading causes of mortality specifically for the women. The existing therapy is not sufficient due to the lack of target specificity and drug resistance. Carbon nanotubes (CNTs) are one of the promising formulati...
Comparative Study
Drug development research. 2020 May;81(3):305-314. DOI:10.1002/ddr.21620
Eran Schmukler,Ronit Pinkas-Kramarski
Eran Schmukler
A growing body of evidence indicates that autophagy, an intracellular degradation pathway, profoundly affects Alzheimer's disease (AD) pathogenesis. Autophagy mediates the degradation of neurotoxic material and damaged organelles, allowing ...
Synthesis, evaluation, molecular docking, and molecular dynamics studies of novel N-(4-[pyridin-2-yloxy]benzyl)arylamine derivatives as potential antitubercular agents [0.03%]
新型N-(4-[吡啶-2-基氧]苯甲基)芳胺衍生物作为潜在抗结核剂的合成、评估、分子对接及分子动力学研究
Ruchi Verma,Helena I M Boshoff,Kriti Arora et al.
Ruchi Verma et al.
A new series of novel triclosan (2,4,4'-trichloro-2'-hydroxydiphenylether) analogues were designed, synthesized, and screened for their in vitro antimycobacterial and antibacterial activities. Most of the compounds showed significant activi...
Comparative Study
Drug development research. 2020 May;81(3):315-328. DOI:10.1002/ddr.21623
Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification [0.03%]
基于结构改造设计的新酰基异噻唑啉酮的合成及其抗结核活性研究
Roberto Martínez,Clara I Espitia-Pinzón,Mayra Silva Miranda et al.
Roberto Martínez et al.
Acylthiosemicarbazides 8a-n were designed by structural modification of lead Compound 7. The syntheses of 8a-n involve a five-step procedure starting from carboxylic acids. Compounds 8a-n were tested against three Mycobacterium tuberculosis...