Sentence examples for medicinal chemistry programme from inspiring English sources

We describe the medicinal chemistry programme that led to the identification of the EP1 receptor antagonist GSK269984A (8h).

This Letter describes the synthetic routes to challenging pyridyl analogues of 2,3-dihydro-1,4-benzodioxin-6-carbaldehyde which were key intermediates for our antibacterial medicinal chemistry programme.

Our medicinal chemistry programme in developing rapidly accessible and modifiable heterocyclic scaffolds led to the design and synthesis of novel substituted benzothiophenes, with 6-benzimidazol-1-ylbenzothiophene derivatives demonstrating significant antitrypanosomal activities (IC50 < 1 μM) against Trypanosoma brucei rhodesiense and no toxicity towards mammalian cells.

Herein we describe a medicinal chemistry programme to develop inhibitors of TbTryS, which gave rise to some potent compounds.

We recently reported the output of this screen,[ 4] and herein we discuss the medicinal chemistry programme around one of the hits, -(1 R -U504880488 (1).

Some of the fragments identified represent potential starting points for a medicinal chemistry programme to develop potent drug-like inhibitors of the enzyme.

In recent years, interleukin-1 receptor-associated kinase 4, IRAK4, has become an attractive target for many medicinal chemistry programmes.

Since the discovery of ET, intense medicinal chemistry programmes have identified receptor antagonists, ETB receptor agonists and inhibitors of the key synthetic enzyme, ECE-1.

All compounds passing these filters were regarded as, in general, valuable starting points for medicinal chemistry programmes and are used for virtual screening campaigns (VS set).

However, it is widely considered that an increasing focus on three-dimensional structures, which incorporate a greater proportion of sp carbons, is probably desirable, 1 in order for medicinal chemistry programmes to be successful against more complex drug targets.

Such lead compounds provide the chemical starting points for medicinal chemistry programmes that are designed to optimise the chemical and biological properties, and to thereby create a drug molecule that can enter clinical trials (Fig. 1).