alexa Synthetic peroxides as antimalarials.
Chemistry

Chemistry

Modern Chemistry & Applications

Author(s): Tang Y, Dong Y, Vennerstrom JL

Abstract Share this page

Abstract The discovery of artemisinin in 1971 initiated a new era in antimalarial chemotherapy. Although the clinically useful semisynthetic artemisinin derivatives are rapid acting and potent antimalarial drugs, they have short half-lives and must be administered over a period of 5-7 days, leading to noncompliance and recrudescence. With this in view, many synthetic antimalarial peroxides have been prepared. Yet, identification of orally active synthetic peroxide drug development candidates that are easily synthesized, inexpensive, and with good biopharmaceutical properties has been surprisingly difficult. In this review, we document the pitfalls and progress made in this endeavor. For each of 15 synthetic peroxide structural classes, we note highlights of the synthetic routes, product stereochemistry, and origin of the peroxide O atoms. Both in vitro and in vivo antimalarial data are then discussed and any SAR noted. Available data indicates that several synthetic 1,2,4-trioxanes are only marginally less effective than the semisynthetic artemisinins. Within a given peroxide chemical family, the more lipophilic members are more potent and possess better oral antimalarial activity in animal models than their more polar counterparts. This poses a challenge to identify peroxide structures with suitable "drug-like" physicochemical properties. Nonetheless, substantial progress has been made in the identification of a new generation of synthetic antimalarial peroxides. Copyright 2004 Wiley Periodicals, Inc. Med Res Rev, 24, No. 4, 425-448, 2004 This article was published in Med Res Rev and referenced in Modern Chemistry & Applications

Relevant Expert PPTs

Relevant Speaker PPTs

  • Eugene Stephane Mananga
    On Fer and Floquet-Magnus expansions: Application in solid-state nuclear magnetic resonance and physics
    PDF Version
  • Jahid Zeghiche
    Jahid-Zeghiche-Univesity-of-Al-Baha- Saudi-Arabia- Compressive- Strength-of-Concerete-filled-Thin- Steel-Stubs-Theoretical-and-Experimental-Study
    PPT Version | PDF Version
  • Beste Cubukcuoglu
    Beste-Cubukcuoglu-Antalya-International-University-Turkey-The-environmental-impact-evaluation-and-testing-of-sustainable-inorganic-binders-A-green-alternative-to-ordinary-Portland-cement
    PPT Version | PDF Version
  • Yosef Yarden
    Classically, the 3’untranslated region (3’UTR) is that region in eukaryotic protein-coding genes from the translation termination codon to the polyA signal. It is transcribed as an integral part of the mRNA encoded by the gene. However, there exists another kind of RNA, which consists of the 3’UTR alone, without all other elements in mRNA such as 5’UTR and coding region. The importance of independent 3’UTR RNA (referred as I3’UTR) was prompted by results of artificially introducing such RNA species into malignant mammalian cells. Since 1991, we found that the middle part of the 3’UTR of the human nuclear factor for interleukin-6 (NF-IL6) or C/EBP gene exerted tumor suppression effect in vivo. Our subsequent studies showed that transfection of C/EBP 3’UTR led to down-regulation of several genes favorable for malignancy and to up-regulation of some genes favorable for phenotypic reversion. Also, it was shown that the sequences near the termini of the C/EBP 3’UTR were important for its tumor suppression activity. Then, the C/EBP 3’UTR was found to directly inhibit the phosphorylation activity of protein kinase CPKC in SMMC-7721, a hepatocarcinoma cell line. Recently, an AU-rich region in the C/EBP 3’UTR was found also to be responsible for its tumor suppression. Recently we have also found evidence that the independent C/EBP 3’UTR RNA is actually exists in human tissues, such as fetal liver and heart, pregnant uterus, senescent fibroblasts etc. Through 1990’s to 2000’s, world scientists found several 3’UTR RNAs that functioned as artificial independent RNAs in cancer cells and resulted in tumor suppression. Interestingly, majority of genes for these RNAs have promoter-like structures in their 3’UTR regions, although the existence of their transcribed products as independent 3’UTR RNAs is still to be confirmed. Our studies indicate that the independent 3’UTR RNA is a novel non-coding RNA species whose function should be the regulation not of the expression of their original mRNA, but of some essential life activities of the cell as a whole.
    PPT Version | PDF Version
  • Habiba Shehu
    Habiba-Shehu-Study-of-the-selectivity-of-methane-over-carbon-dioxide-and-inert-gases-using-composite-inorganic-membranes
    PPT Version | PDF Version
  • Mark N. Callender
    Mark-N-Callender-Middle-Tennessee-State-University-USA-Theoretical-optimization-of-a-cylindrical-body-of-rotation-using-magnus-effect-lift
    PPT Version | PDF Version
  • Daniel Smith
    The editor as auteur: The modern role of editors and preditors
    PPT Version | PDF Version
  • Nadia Badr
    Application of aquatic plant phytoremediation as green technology treatment of lead in polluted water
    PPT Version | PDF Version
  • Olga V Shuvaeva
    The use of thermal release technique with atomic absorption detection for the study of mercury transformation in contaminated environment
    PPT Version | PDF Version
  • Abel E Navarro
    Improving the adsorptive properties of biomaterials for the removal of heavy metals
    PPT Version | PDF Version
  • Dequan Xiao
    Inverse molecular design of green catalysts for biomass conversion
    PPT Version | PDF Version
  • Shenghong A Dai
    Green processes to diisocyanates and polyurethane-urea elastomers via carbonate raw materials: New NPR and NIR processes
    PPT Version | PDF Version
  • J S Yadav
    Novel organic transformations in aqueous media
    PPT Version | PDF Version
  • Neha Singh
    Role of Hydrogeochemistry in the release of arsenic in 24 Parganas districts, West Bengal
    PPT Version | PDF Version
  • David Y Lai
    Mechanism-based molecular design of chemicals with low carcinogenicity potential
    PPT Version | PDF Version

Relevant Topics

Peer Reviewed Journals
 
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri & Aquaculture Journals

Dr. Krish

agriaquaculture@omicsonline.com

1-702-714-7001Extn: 9040

Biochemistry Journals

Datta A

biochemjournals@omicsonline.com

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

business@omicsonline.com

1-702-714-7001Extn: 9042

Chemistry Journals

Gabriel Shaw

chemistryjournals@omicsonline.com

1-702-714-7001Extn: 9040

Clinical Journals

Datta A

clinicaljournals@omicsonline.com

1-702-714-7001Extn: 9037

Engineering Journals

James Franklin

engineeringjournals@omicsonline.com

1-702-714-7001Extn: 9042

Food & Nutrition Journals

Katie Wilson

nutritionjournals@omicsonline.com

1-702-714-7001Extn: 9042

General Science

Andrea Jason

generalscience@omicsonline.com

1-702-714-7001Extn: 9043

Genetics & Molecular Biology Journals

Anna Melissa

geneticsmolbio@omicsonline.com

1-702-714-7001Extn: 9006

Immunology & Microbiology Journals

David Gorantl

immunomicrobiol@omicsonline.com

1-702-714-7001Extn: 9014

Materials Science Journals

Rachle Green

materialsci@omicsonline.com

1-702-714-7001Extn: 9039

Nursing & Health Care Journals

Stephanie Skinner

nursinghealthcare@omicsonline.com

1-702-714-7001Extn: 9039

Medical Journals

Nimmi Anna

medicaljournals@omicsonline.com

1-702-714-7001Extn: 9038

Neuroscience & Psychology Journals

Nathan T

neuropsychology@omicsonline.com

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

Ann Jose

pharmajournals@omicsonline.com

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

social_politicalsci@omicsonline.com

1-702-714-7001Extn: 9042

 
© 2008- 2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version
adwords