Free Biochemistry -MEdChem-Physiology papers (look inside!)

some papers that i got on my disk drive , maybe can be useful in your research field or hobbie.All of those are pay per view...but now are for free for you

Analysis of structure–activity relationships with the N-(3-acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea template for vanilloid receptor 1 antagonism

Jeewoo Lee, , a, Su Yeon Kima, Jiyoun Leea, Myungsim Kanga, Min-Jung Kila, Hyun-Kyung Choia, Mi-Kyung Jina, Yun Wangb, Attila Tothb, Larry V. Pearceb, Daniel J. Lundbergb, Richard Tranb and Peter M. Blumbergb

a Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Shinlim-Dong, Kwanak-Ku, Seoul 151-742, South Korea
b Laboratory of Cellular Carcinogenesis and Tumor Promotion, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA

Abstract

In a continuing effort to elucidate the structure–activity relationships of the lead antagonist N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N′-[4-(methylsulfonylamino)benzyl]thiourea (1), the distances between the proposed four pharmacophores in 1 have been varied by insertion or deletion of one carbon to optimize their fit to the receptor. In addition, the acyloxy group of the C region was replaced with amide and N-hydroxy amide to identify the pharmacophoric importance of the ester group in the C2 region. The results indicated that the pharmacophoric arrangement of 1 was optimal for receptor binding affinity and antagonism, and the ester of the C2 region was significant for receptor binding. Among the derivatives, compound 19 showed distinct behavior with a 2-fold improvement in antagonism but a 13-fold reduction in binding affinity compared to 1. The partial separation of pharmacophoric requirements of these two assays has been noted before and compound 19 is thus selective for the calcium entry-linked receptor population. The conformational analysis of 1 generated three distinct conformers having different types of hydrophobic interactions, which will be utilized for exploring the active conformation of the VR1 ligand.

Bioorganic & Medicinal Chemistry
Volume 12, Issue 13 , 1 July 2004, Pages 3411-3420

http://mihd.net/z9mpij

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The proton-pump inhibitors: similarities and differences.

Horn J.

Department of Pharmacy, University of Washington School of Pharmacy, Seattle 98185, USA.

OBJECTIVE: This paper examines the clinical pharmacology of the proton-pump inhibitors (PPIs) and briefly reviews some comparative studies of these agents. BACKGROUND: PPIs have emerged as the treatment of choice for acid-related diseases, including gastroesophageal reflux disease (GERD) and peptic ulcer disease. Although these drugs-omeprazole, lansoprazole, pantoprazole, and rabeprazole-share a common structure (all are substituted benzimidazoles) and mode of action (inhibition of H+,K+-adenosine triphosphatase [ATPase]), each differs somewhat in its clinical pharmacology. RESULTS: In comparative clinical trials found in MEDLINE, PPIs administered once daily produced endoscopic evidence of healing in >90% of patients with duodenal ulcer after 4 weeks of treatment, in >90% of those with gastric ulcer after 6 weeks of treatment, and in >90% of those with ulcerative or erosive GERD after 8 weeks of treatment. Maintenance therapy with daily doses of a PPI has been shown to be an effective means of preventing GERD relapse. PPIs also inhibit the growth of Helicobacter pylori, now recognized as an important factor in peptic ulcer disease, and, when administered in combination with antibiotics, provide the best treatment for eradication of the bacterium. Rabeprazole has a more rapid onset of H+,K+-ATPase inhibition than the other PPIs and, compared with omeprazole, a greater effect on intragastric pH after the first dose. Omeprazole and lansoprazole have a greater potential for drug-drug interactions than do pantoprazole and rabeprazole. CONCLUSION: Although the individual PPIs have similar efficacy in many cases, differences between them should be considered when choosing a treatment regimen.

Clinical Therapeutics
Volume 22, Issue 3 , March 2000, Pages 266-280

http://mihd.net/4wltcq

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The Immune System— First of Two Parts

Peter J. Delves, Ph.D., and Ivan M. Roitt, D.Sc.

Since this article has no abstract, we have provided an extract of the first 100 words of the full text and any section headings.

The immune system is an organization of cells and molecules with specialized roles in defending against infection. There are two fundamentally different types of responses to invading microbes. Innate (natural) responses occur to the same extent however many times the infectious agent is encountered, whereas acquired (adaptive) responses improve on repeated exposure to a given infection. The innate responses use phagocytic cells (neutrophils, monocytes, and macrophages), cells that release inflammatory mediators (basophils, mast cells, and eosinophils), and natural killer cells. The molecular components of innate responses include complement, acute-phase proteins, and cytokines such as the interferons. Acquired responses involve the . . . [Full Text of this Article]

Three Levels of Defense

Immune Recognition

Innate Immune Responses

Cellular Components of Innate Responses

Soluble Factors in Innate Defense

The Acute Inflammatory Response

Acquired Immune Responses

The Structure of Antigen-Specific Molecules

The B-Cell Receptor and Soluble Antibodies

The T-Cell Receptor

The Diversity of Antigen Receptors

Clonal Selection

Major Populations of B Cells

T Cells and the Thymus

Tolerance Mechanisms

References

N Engl J Med. 2000 Jul 6;343(1):37-49.

http://mihd.net/yoc23k

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that's all for now , i'll post some more papers soon...and my whole lst of subscribed databases

if u want to get some biochem related paper just msg me

see ya



[Edited on 2-2-2007 by HenningBasse]

noticed that links above seems to be dead

here's the new location for the three papers cited above

biochemistry-medicinal chemistry-physiology.rar - 1.20MB

rar password : sciencemadness.org



[Edited on 8-2-2007 by HenningBasse]

[Edited on 8-2-2007 by HenningBasse]