Abstract
Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or more nitrogen atoms within the (fused) rings). In a constant quest for new chemical entities in drug discovery, a few novel heterocycles have emerged in recent years as promising building blocks for the obtainment of bioactive modulators. In this context, pyrrolotriazinones have attracted attention, and some show promising biological activities. Here, we offer an extensive review of pyrrolo[2,1-f][1,2,4]triazin-4(1H)-one and pyrrolo[1,2-d][1,2,4]triazin-4(3H)-one, describing their biological properties en route to drug discovery.
Highlights
Whereas biologics are emerging as a new concept in the therapeutic arsenal, small molecules are still needed either to identify probes to decipher biological processes or to get potential starting points for drug discovery
Devasthale et al [13] have designed a series of pyrrolotriazinones that were assayed for their antagonistic activity, and the reduction in weight gain in a rat model after 4 days of once-daily oral treatment
Sepiapterin reductase plays an important role in the biosynthesis of tetrahydrobiopterin (BH4), which is a key cofactor for a set of enzymes, including nitric oxide synthases (NOSs), aromatic amino acid hydroxylases, and alkylglycerol monooxygenase
Summary
Whereas biologics are emerging as a new concept in the therapeutic arsenal, small molecules are still needed either to identify probes to decipher biological processes or to get potential starting points for drug discovery. In order to narrow the number of scaffolds to explore, one can focus on nitrogen-containing compounds and, more precisely, on nitrogen-based heterocycles. This makes sense since more than 75% of drugs approved by the Food and Drug Administration currently available on the market (β-lactams, quinazolines, benzodiazepines) are nitrogen-containing heterocycle moieties. Whereas many nitrogen-based heterocycles have been explored in drug design, there are still some families that are underrepresented [6]. Due to the growing interest in biological applications of pyrrolotriazinones, new synthetic strategies should be explored in the future in order to offer a quicker access to more complex analogs, a highly challenging task for organic chemists. We focus on pyrrolotriazinones (A) and (C) published or patented to date and present their biological activities as well as their targets when available
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