Azaarenes are carbon-to-nitrogen transmutations
The necessary nitrogen atom in chemical biology and drug discovery: from bosentan to macitentan (Opsumit®)
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Source: Carbon-to-nitrogen single-atom transmutation of azaarenes
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Source: Carbon-to-nitrogen single-atom transmutation of azaarenes
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The nitrogen atom plays a critical role in drug discovery by mediating oxygen-to-oxygen transitions. An analysis of the structural diversity, substitution patterns, and Frequency of Nitrogen Heterocycles among US FDA approved pharmaceuticals revealed that nitrogen atom insertion increased oxygen-to-oxygen transition from bosentan to Macitentan. The nitrogen atom is also required for diversification of indole skeletons through nitrogen atom insertion.