Literature DB >> 20221336

A receptor-grounded approach to teaching nonsteroidal antiinflammatory drug chemistry and structure-activity relationships.

Victoria F Roche1.   

Abstract

OBJECTIVE: To describe a receptor-based approach to promote learning about nonsteroidal anti-inflammatory drug (NSAID) chemistry, structure-activity relationships, and therapeutic decision-making.
DESIGN: Three lessons on cyclooxygenase (COX) and NSAID chemistry, and NSAID therapeutic utility, were developed using text-based resources and primary medicinal chemistry and pharmacy practice literature. Learning tools were developed to assist students in content mastery. ASSESSMENT: Student learning was evaluated via performance on quizzes and examinations that measured understanding of COX and NSAID chemistry, and the application of that knowledge to therapeutic problem solving.
CONCLUSION: Student performance on NSAID-focused quizzes and examinations documented the success of this approach.

Entities:  

Keywords:  medicinal chemistry; nonsteroidal antiinflammatory drugs

Mesh:

Substances:

Year:  2009        PMID: 20221336      PMCID: PMC2828304          DOI: 10.5688/aj7308143

Source DB:  PubMed          Journal:  Am J Pharm Educ        ISSN: 0002-9459            Impact factor:   2.047


  17 in total

1.  Modeling cyclooxygenase inhibition. Implication of active site hydration on the selectivity of ketoprofen analogues.

Authors:  A Palomer; J J Pérez; S Navea; O Llorens; J Pascual; L García; D Mauleón
Journal:  J Med Chem       Date:  2000-06-01       Impact factor: 7.446

Review 2.  Cyclooxygenases 1 and 2.

Authors:  J R Vane; Y S Bakhle; R M Botting
Journal:  Annu Rev Pharmacol Toxicol       Date:  1998       Impact factor: 13.820

Review 3.  Mechanism of action of nonsteroidal anti-inflammatory drugs.

Authors:  J R Vane; R M Botting
Journal:  Am J Med       Date:  1998-03-30       Impact factor: 4.965

4.  Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents.

Authors:  R G Kurumbail; A M Stevens; J K Gierse; J J McDonald; R A Stegeman; J Y Pak; D Gildehaus; J M Miyashiro; T D Penning; K Seibert; P C Isakson; W C Stallings
Journal:  Nature       Date:  1996 Dec 19-26       Impact factor: 49.962

5.  Molecular basis of the time-dependent inhibition of cyclooxygenases by indomethacin.

Authors:  Jeffery J Prusakiewicz; Andrew S Felts; Bonnie S Mackenzie; Lawrence J Marnett
Journal:  Biochemistry       Date:  2004-12-14       Impact factor: 3.162

6.  Prostaglandin endoperoxide H synthase-1: the functions of cyclooxygenase active site residues in the binding, positioning, and oxygenation of arachidonic acid.

Authors:  E D Thuresson; K M Lakkides; C J Rieke; Y Sun; B A Wingerd; R Micielli; A M Mulichak; M G Malkowski; R M Garavito; W L Smith
Journal:  J Biol Chem       Date:  2000-12-19       Impact factor: 5.157

7.  Spatial requirements for 15-(R)-hydroxy-5Z,8Z,11Z, 13E-eicosatetraenoic acid synthesis within the cyclooxygenase active site of murine COX-2. Why acetylated COX-1 does not synthesize 15-(R)-hete.

Authors:  S W Rowlinson; B C Crews; D C Goodwin; C Schneider; J K Gierse; L J Marnett
Journal:  J Biol Chem       Date:  2000-03-03       Impact factor: 5.157

8.  Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2.

Authors:  D Riendeau; M D Percival; C Brideau; S Charleson; D Dubé; D Ethier; J P Falgueyret; R W Friesen; R Gordon; G Greig; J Guay; J Mancini; M Ouellet; E Wong; L Xu; S Boyce; D Visco; Y Girard; P Prasit; R Zamboni; I W Rodger; M Gresser; A W Ford-Hutchinson; R N Young; C C Chan
Journal:  J Pharmacol Exp Ther       Date:  2001-02       Impact factor: 4.030

9.  Improving pharmacy students' understanding and long-term retention of acid-base chemistry.

Authors:  Victoria F Roche
Journal:  Am J Pharm Educ       Date:  2007-12-15       Impact factor: 2.047

10.  A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385.

Authors:  Scott W Rowlinson; James R Kiefer; Jeffery J Prusakiewicz; Jennifer L Pawlitz; Kevin R Kozak; Amit S Kalgutkar; William C Stallings; Ravi G Kurumbail; Lawrence J Marnett
Journal:  J Biol Chem       Date:  2003-08-18       Impact factor: 5.157

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  6 in total

1.  A pharmacy practice laboratory exercise to apply biochemistry concepts.

Authors:  Marc W Harrold; Marsha A McFalls
Journal:  Am J Pharm Educ       Date:  2010-10-11       Impact factor: 2.047

2.  Active-learning exercises to teach drug-receptor interactions in a medicinal chemistry course.

Authors:  Seetharama D Satyanarayanajois
Journal:  Am J Pharm Educ       Date:  2010-10-11       Impact factor: 2.047

3.  Design and implementation of a laboratory-based drug design and synthesis advanced pharmacy practice experience.

Authors:  Ashok Philip; Mark Stephens; Sheila L Mitchell; E Blake Watkins
Journal:  Am J Pharm Educ       Date:  2015-04-25       Impact factor: 2.047

4.  Creation of medicinal chemistry learning communities through enhanced technology and interdisciplinary collaboration.

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Journal:  Am J Pharm Educ       Date:  2012-10-12       Impact factor: 2.047

5.  An Active Learning Activity to Reinforce the Design Components of the Corticosteroids.

Authors:  Stephen R Slauson; Prashant Mandela
Journal:  Pharmacy (Basel)       Date:  2018-02-05

6.  Synthesis and antiplatelet activity of antithrombotic thiourea compounds: biological and structure-activity relationship studies.

Authors:  André Luiz Lourenço; Max Seidy Saito; Luís Eduardo Gomes Dorneles; Gil Mendes Viana; Plínio Cunha Sathler; Lúcia Cruz de Sequeira Aguiar; Marcelo de Pádula; Thaisa Francielle Souza Domingos; Aline Guerra Manssour Fraga; Carlos Rangel Rodrigues; Valeria Pereira de Sousa; Helena Carla Castro; Lucio Mendes Cabral
Journal:  Molecules       Date:  2015-04-20       Impact factor: 4.411

  6 in total

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