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8113959 
Journal Article 
Homologation: A versatile molecular modification strategy to drug discovery 
Lima, LM; Alves, MA; Do Amaral, DN 
2019 
Yes 
Current Topics in Medicinal Chemistry
ISSN: 1568-0266 
Bentham Science Publishers 
19 
19 
1734-1750 
English 
Homologation is a concept introduced by Gerhard in 1853 to describe a homologous series in organic chemistry. Since then, the concept has been adapted and used in medicinal chemistry as one of the most important strategies for molecular modification. The homologation types, their influence on physico-chemical properties and molecular conformation are presented and discussed. Its application in lead-identification and lead optimization steps, as well as its impact on pharmacodynamics/pharmacokinetic properties and on protein structure is highlighted from selected examples. • Homologation: definition and types • Homologous series in nature • Comparative physico-chemical and conformational properties • Application in lead-identification and lead-optimization • Impact on pharmacodynamic property • Impact on pharmacokinetic property • Impact on protein structure • Concluding remarks • Acknowledgment • References. © 2019 Bentham Science Publishers. 
Drug discovery; Homologation; Homologous; Lead optimization; Molecular modification strategy; Organic compounds