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978-3-8439-4452-6, Reihe Medizinische Chemie

Michael Christopher Böck
Development of new mGAT4 inhibitors by variation of the amino acid subunit and lipophilic domain of (S)-SNAP-5114

333 Seiten, Dissertation Ludwig-Maximilians-Universität München (2020), Hardcover, A5

Zusammenfassung / Abstract

Diseases related to deficient GABAergic neurotransmission, such as epilepsy, depression, Alzheimer´s disease and anxiety disorders, respresent a major world health issue, hence requiring effective and tolerable medication. In this context, the GABA transporter subtype mGAT4 has come into focus as potentially promising pharmacological target. As the currently available mGAT4 inhibitors can be regarded as not really satisfying with regard to inhibitory potency and subtype selectivity, there exists a strong demand for the development of more efficient inhibitors. For this to be achieved, a deeper understanding of the structure activity relationship (SAR) of mGAT4 inhibitors is required. Hence, the objective of this dissertation aimed at broadening the knowledge in this respect and, as a consequence thereof, at identifying mGAT4 inhibitors with higher potency and subtype selectivity. To this end, a variety of analogues of the lead compound (S)-SNAP-5114 were synthesized and examined for their inhibitory effects. In this context, several mGAT4 inhibitors with potencies comparable to or higher than the lead compound were developed. Also, promising new structural motifs for the lipophilic domain of (S)-SNAP-5114 analogues were identified.