Autor
Lídia Moreira Lima ; Angelo da Cunha Pinto
Editora
E-papers
Assunto
Ciências Exatas e da Terra
Ano
2015
Páginas
388
ISBN-13
9788576504894
Edição

Compendium of medicinal chemistry

Coletânea de artigos publicados originalmente em edição especial da Revista Virtual de Química em homenagem ao professor Antonio Monge, além de outros artigos publicados entre 2009 e 2014, selecionados e atualizados.
Tabela de conteúdo
pág. capítulo
1 Content
7 Preface
9 Opportunities and Challenges for Innovation in Pharmaceuticals Now or Never! Eliezer J. Barreiro e Angelo C. Pinto
9 1. Preamble
10 2. Historic Chronology
14 3. Pharmaceutical technological innovation: Pasteur’s Quadrant
16 4. The capacity for innovation in the Pharmaceutical Industry (PI)
17 5. Contemporary innovative pharmaceuticals
21 6. Contribution of the National Institute of Science and Technology in Drugs and Medicines (INCT-INOFAR)
24 7. Final Considerations
25 8. References
28 Molecular Modeling Methods for the Study and Design of Bioactive Compounds An Introduction Carlos Mauricio R. Sant’Anna
28 1. Introduction
31 2. Models
39 3. Comparative Methods
40 4. Modeling Bioligand-Protein Complexes
41 5. Conclusions
42 6. References
44 G Protein-Coupled Receptors - Lucas Villas Bôas Hoelz, Pedro Henrique Monteiro Torres, Guilherme Barroso Langoni de Freitas, Vinícius Fonseca Leal, Tácio Vinicio Amorim Fernandes,
44 1. Introduction
45 2. Structural Features of GPCRs
49 3. Activation Mechanism of GPCRs
53 4. Subsequent Activation of G Proteins
57 5. Classification Systems of GPCRs
59 6. Final Considerations
60 7. References
71 Protein tyrosine kinases Challenges in the development of drugs aimed at cancer therapy Carolina M. Avila e Nelilma C. Romeiro
71 1. Introduction
72 2. Structure and Function of Receptor Tyrosine Kinases (RTKs)
74 3. Structure and Function of Non-Receptor Tyrosine Kinases (NRTKs)
76 4. Tyrosine Kinase Inhibitors (TKIs)
82 5. Binding Modes Revealed by 3D Structures of PTKs Obtained by X-ray Diffraction
90 6. Monoclonal Antibodies as anti-RTKs Drugs
90 7. Sources of Information on PTKs
91 8. Conclusions
92 9. References
97 Alzheimer’s Disease Characterization, progress and implications of the neuro-inflammatory process Flávia Pereira Dias Viegas, Kris Simone Tranches Dias, Maria Cecília Rodrigues Sim
97 1. Introduction
98 2. Characterization, socioeconomic impact and progress of Alzheimer’s disease
102 3. Acetylcholinesterase Inhibitors and therapeutic arsenal available for the treatment of AD
109 4. Influence of the neuroinflammatory process on the outbreak and progress of AD
118 5. Conclusions
119 6. References
126 The Growing Importance of Carbohydrates in Medicinal Chemistry Christiane M. Nogueira, Bárbara R. Parmanhan, Patrícia P. Farias, Arlene G. Corrêa
126 1. Introduction
127 2. Antibacterial Agents
130 3. Antiviral Agents
132 4. Antineoplastic Agents
135 5. Antiprotozoal Agents
138 6. Antifungal Agents
140 7. Other Agents
143 8. References
145 Beirut Reaction and its Application in the Synthesis of Quinoxaline-N,N’-Dioxides Bioactive Compounds Lídia M. Lima Daniel N. do Amarala
145 1. Definition, application and mechanism
150 2. Quinoxaline-N,N’-dioxide derivatives
163 3. Miscellaneous
169 4. References
172 Lapachol and β-Lapachone Two Natural Naphthoquinones with Great Importance in Medicinal Chemistry Fernando C. Silva e Vitor F. Ferreira
172 1. Introduction
174 2. Quinones
179 3. Naphthoquinones
182 4. Lapachol (1)
201 5. β-Lapachone (2)
230 6. Conclusion and Final Comments
231 7. References
258 MCH-R1 Antagonists as Potential Anti-obesity Drugs. Design Strategies and Structure-activity Relationship Gildardo Rivera, Antonio Moreno, Virgilio Bocanegra-García
258 1. Introduction
260 2. Melanin-concentrating hormone (MCH)
261 3. MCH-R1 Antagonists
280 4. Conclusions
280 5. References
286 Toxoplasmosis Perspectives on the study of new therapeutic targets Daiana T. Mancini, Letícia C. Assis, Giovanna C. Gajo, Tanos C. C. França, Elaine F. F. da Cunha, Teodorico C. Ra
286 1. Toxoplasmosis
299 2. Methods
301 3. Results and discussion
315 4. Conclusions
315 5. References
320 Quinoxaline and Arylaminoalcohol Derivatives as Antiplasmodial and Leishmanicidal Agents A Review of our First Ten Years in the Field Miguel Quiliano e Ignacio Aldana
320 1. Introduction
321 2. Malaria
329 3. Leishmaniasis
332 4. Conclusions and Outlook
333 5. References
336 Quinoxaline 1,4-di-N-oxide Derivatives Interest in the Treatment of Chagas Disease Elsa Moreno-Viguri e Silvia Pérez-Silanes
336 1. Introduction
338 2. Background
340 3. Ten years of research
347 4. Complementary assays
354 5. Conclusions
358 Understanding the Solid Forms of 5E-phenylethenylbenzofuroxan with Different in vivo anti-T. cruzi Activity Sara B. Honorato, Williams Porcal, Alicia Merlino, Javier Ellena, Hugo C
358 1. Introduction
361 2. Experimental
363 3. Results
367 4. Discussion
369 5. Conclusion
369 6. References
371 Pharmaceutical Innovation A University Experience Antonio Monge
371 1. Introduction
372 2. Work approaches
377 3. Final Considerations
379 The paradigm of the lead compound in Medicinal Chemistry Eliezer J. Barreiro
379 1. Innovation in drugs: The process of rational planning
380 2. The main modern paradigm of medicinal chemistry: The discovery of the lead prototype
384 3. New lead compounds discovered in LASSBio
386 4. References
354 6. Referências

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