Challenges and Rewards in Medicinal Chemistry Targeting Cardiovascular and Metabolic Diseases.
Chimia (Aarau)
; 69(7): 407-413, 2015 Aug 19.
Article
en En
| MEDLINE
| ID: mdl-28482972
ABSTRACT
Medicinal chemistry has been transformed by major technological and conceptual innovations over the last three decades structural biology and bioinformatics, structure and property based molecular design, the concepts of multidimensional optimization (MDO), in silico and experimental high-throughput molecular property analysis. The novel technologies advanced gradually and in synergy with biology and Roche has been at the forefront. Applications in drug discovery programs towards new medicines in cardiovascular and metabolic diseases are highlighted to show impact and advancement the early discovery of endothelin antagonists for endothelial dysfunction (Bosentan), 11-beta hydroxysteroid dehydrogenase (11ß-HSD1) inhibitors for dysregulated cellular glucocorticoid tonus (type 2 diabetes and metabolic syndrome) and non-covalent hormone sensitive lipase (HSL) inhibitors to study the scope of direct inhibition of lipolysis in the conceptual frame of lipotoxicity and type 2 diabetes.
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Banco de datos:
MEDLINE
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En
Revista:
Chimia (Aarau)
Año:
2015
Tipo del documento:
Article
País de afiliación:
Suiza