RESUMO
There is a constant pressure in industry to move away from platinum group metals (PGM) and achieve more environmentally friendly and sustainable production processes in the future. Recently developed Mn-based catalysts offer an interesting opportunity to complement established catalysts based on Ru. In this article, recent achievements in the field are highlighted and recent achievements in the collaboration of Solvias AG with the group of Prof. M. Clarke towards the implementation of these catalysts on industrial scale are outlined.
RESUMO
A genetic algorithm (GA), driven by experimentally determined biological activities as a feedback fitness function, was used to propose novel small molecules as inhibitors of glucose-6-phosphate translocase (G6PT) in iterative rounds of evolutionary optimization. A straightforward polymer-supported synthetic sequence was implemented to synthesize molecules proposed by the GA, and the biological activities of the compounds were determined by a microsomal assay. Additional compound design strategies were integrated, such as Tanimoto similarity-based selection of starting materials and transfer of favored structure elements into a new chemical scaffold to identify more active and selective inhibitors.
Assuntos
Antiporters/antagonistas & inibidores , Diabetes Mellitus Tipo 2/enzimologia , Inibidores Enzimáticos/síntese química , Glucose-6-Fosfatase/antagonistas & inibidores , Hipoglicemiantes/síntese química , Proteínas de Transporte de Monossacarídeos/antagonistas & inibidores , Animais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Glucose/metabolismo , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/enzimologia , Microssomos Hepáticos/metabolismo , Estrutura Molecular , RatosRESUMO
Using a newly developed multicomponent chemistry strategy in combination with structure based drug design, a new class of HIV-1 protease inhibitors has been obtained.