In recent years, tools for the development of new drugs have been dramatically improved. These include genomic and proteomic research, numerous biophysical methods, combinatorial chemistry and screening technologies. In addition, early ADMET studies are employed in order to significantly reduce the failure rate in the development of drug candidates. As a consequence, the lead finding, lead optimization and development process has gained marked enhancement in speed and efficiency. In parallel to this development, major pharma companies are increasingly outsourcing many components of drug discovery research to biotech companies. All these measures are designed to address the need for a faster time to market. New screening methodologies have contributed significantly to the efficiency of the drug discovery process. The conventional screening of single compounds or compound libraries has been dramatically accelerated by high throughput screening methods. In addition, in silico screening methods allow the evaluation of virtual compounds. A wide range of new lead finding and lead optimization opportunities result from novel screening methods by NMR, which are the topic of this review article.

Drug Discovery Today

Tetrahydroquinoline is one of the most important simple nitrogen heterocycles, being widespread in nature and present in a broad variety of pharmacologically active compounds. This Review summarizes the progress achieved in the chemistry of tetrahydroquinolines, with emphasis on their synthesis, during the period from mid-2010 to early 2018.

Progress in the Chemistry of Tetrahydroquinolines.

2-Propargyl Alcohols in Organic Synthesis

The indolocarbazoles are an important class of nitrogen heterocycles which has evolved significantly in recent years, with numerous studies focusing on their diverse biological effects, or targeting new materials with potential applications in organic electronics. This review aims at providing a broad survey of the chemistry and properties of indolocarbazoles from an interdisciplinary point of view, with particular emphasis on practical synthetic aspects, as well as certain topics which have not been previously accounted for in detail, such as the occurrence, formation, biological activities, and metabolism of indolo[3,2-b]carbazoles. The literature of the past decade forms the basis of the text, which is further supplemented with older key references.

Chemistry and Properties of Indolocarbazoles

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Handbook Of Metathesis

Synthesis and biological evaluation of caffeic acid derivatives as potent inhibitors of α-MSH-stimulated melanogenesis

We describe the total synthesis of indolylquinazolinone alkaloid bouchardatine and some of the quinazolinone derivatives. The aerobic oxidation induced by copper(I) bromide, followed by Vilsmeier-Haack formylation gives the natural product bouchardatine alkaloid in good yield.

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Copper catalysed synthesis of indolylquinazolinone alkaloid bouchardatine

Biologically important quinazolinones have been synthesized from 2-aminobenzamides and DMSO. The key feature of the reaction is the utilization of DMSO as a methine source for intramolecular oxidative annulation. The CNS depressant drug methaqualone has also been synthesized by our methodology. The present method involves the synthesis of quinazolinones with a broad substrate scope and a good yield.

Transition metal-free synthesis of quinazolinones using dimethyl sulfoxide as a synthon.

A novel cyclization/oxidation strategy for a two-step synthesis of (Z)-aurone

We explored the zinc triflate catalyzed heteroannulation reaction of 3-aminocarbazoles with substituted propargyl alcohols to form pyrrolo[2,3-c]carbazoles in moderate to good yields. This transformation proceeds with good regioselectivity and without the addition of additives or ligands.

Mayavan Viji

Papers

Synthesis and biological evaluation of caffeic acid derivatives as potent inhibitors of α-MSH-stimulated melanogenesis

Copper catalysed synthesis of indolylquinazolinone alkaloid bouchardatine

Transition metal-free synthesis of quinazolinones using dimethyl sulfoxide as a synthon.

A novel cyclization/oxidation strategy for a two-step synthesis of (Z)-aurone

Zinc triflate catalyzed regioselective synthesis of pyrrolo[2,3-c]carbazoles via heteroannulation