Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 2. Indole-3-acetamides with Additional Functionality
| العنوان: | Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 2. Indole-3-acetamides with Additional Functionality |
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| المؤلفون: | Bach Nicholas J, Dennis R. Berry, Robert D. Dillard, Edward David Mihelich, Jean-Pierre Wery, Cynthia D. Sommers, Lea M. Johnson, David W. Snyder, Donald G. Carlson, David K. Clawson, Emma R. McKinney, Amy C. Smith, Richard Walter Schevitz, Susan E. Draheim, Lawrence W. Hartley, Jennifer L. Olkowski, Noel D. Jones, Nickolay Y. Chirgadze |
| المصدر: | Journal of Medicinal Chemistry. 39:5137-5158 |
| بيانات النشر: | American Chemical Society (ACS), 1996. |
| سنة النشر: | 1996 |
| مصطلحات موضوعية: | Magnetic Resonance Spectroscopy, medicine.drug_class, Stereochemistry, Carboxamide, Crystallography, X-Ray, Chemical synthesis, Mass Spectrometry, Phospholipases A, Structure-Activity Relationship, Phospholipase A2, Drug Discovery, medicine, Humans, Indole test, chemistry.chemical_classification, Indoleacetic Acids, biology, Active site, Phospholipases A2, Enzyme, chemistry, Biochemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, Selectivity |
| الوصف: | As reported in our previous paper, a series of indole-3-acetamides which possessed potency and selectivity as inhibitors of human nonpancreatic secretory phospholipase A2(hnps-PLA2) was developed. The design of these compounds was based on information derived from x-ray crystal structures determined for complexes between the enzyme and its inhibitors. We describe here the further implementation of this structure-based design strategy and continued SAR development to produce indole-3-acetamides with additional functionalities which provide increased interaction with important residues within the enzyme active site. These efforts led to inhibitors with substantially enhanced potency and selectivity. |
| تدمد: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm960486n |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdb0858e7cadcd119a6d3f11a160b093 https://doi.org/10.1021/jm960486n |
| رقم الانضمام: | edsair.doi.dedup.....bdb0858e7cadcd119a6d3f11a160b093 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204804 00222623 |
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| DOI: | 10.1021/jm960486n |