Relationship between 13C NMR Parameters and Antimalarial activity of Cryptolepine Isosteres
Authors
Abstract:
Density functional theory calculations were applied to investigate 13C Chemical Shielding (CS) tensors in cryptolepine (1) and its sulfur (2) and oxygen (3) isosteres. The results showed that the CS of carbon nuclei in these compounds may be divided into three types. First, carbons type α,are those directly bonded to X (X= NH, S, O) and σ 33 shielding component of these carbons are deshielded in O isostere compared to N and S isosteres. The second group of carbons (β-carbons) is attached to α-carbons, in which σ11 components of S isostere differs from O and N isosteres. The third carbon group, γ-carbons are positioned at a distance of three interatomic bonds or greater away from X. The replacement of N by O or S in cryptolepine isosteres has negligible influence on all components of the later carbon type. The variations of CS components could be related to the inactivity of O isostere and broad spectrum activity of S isostere.
similar resources
relationship between 13c nmr parameters and antimalarial activity of cryptolepine isosteres
full text
Cryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
full textCryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
full textthe investigation of the relationship between type a and type b personalities and quality of translation
چکیده ندارد.
Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ellipticine, olivacine, cryptolepine and a synthetic cryptolepine analog.
Indole alkaloids ellipticine (1), cryptolepine triflate (2a), rationally designed 11-(4-piperidinamino)cryptolepine hydrogen dichloride (2b) and olivacine (3) (an isomer of 1) were evaluated in vitro against Plasmodium falciparum and in vivo in Plasmodium berghei-infected mice. 1-3 inhibited P. falciparum (IC₅₀≤1.4 μM, order of activity: 2b>1>2a>3). In vitro toxicity to murine macrophages was e...
full texton the relationship between critical thinking, metacognition and translation quality of literary and economic texts
این مطالعه سعی دارد تا رابطه تفکر انتقادی و مهارت های شناختی را به عنوان دو عنصر مهم روانشناسی شناختی با کیفیت ترجمه متون ادبی و اقتصادی بررسی کند. صد دانشجوی سال آخر ترجمه که در مقطع کارشناسی مشغول به تحصیل هستند برای شرکت در این مطالعه انتخاب شدند و آزمون های تافل تفکر انتقادی و مهارت های شناختی از آنها گرفته شد. آزمون ترجمه ادبی و اقتصادی نیز برای تعیین سطح کیفیت ترجمه گرفته شد. یافته های حا...
My Resources
Journal title
volume 9 issue 3
pages 19- 26
publication date 2015-07-01
By following a journal you will be notified via email when a new issue of this journal is published.
Hosted on Doprax cloud platform doprax.com
copyright © 2015-2023