A number of N-arylmethyl substituted indole derivatives have been synthesized and their effectiveness against ADP and arachidonic acid induced platelet aggregation in human plasma was determined. The desired compounds were synthesized by reacting the appropriate aniline derivative with isatin (or substituted isatin) to form the corresponding imine structures. The so formed compound was then act...

In recent years, indole derivatives have acquired conspicuous significance due to their wide spectrum of biological activities. It is well known fact that the indole nucleus is present as a structural unit in many natural products. Synthesis and biological evaluation of indole derivatives have been a topic of special interest to organic and medicinal chemists. A number of indole derivatives hav...

A concise synthesis of spiro-cyclopropane compounds from indole derivatives and sulfur ylides has been developed via a dearomatization strategy. Moreover, the spiro-cyclopropane compounds could be conveniently transformed to rearomatized indole derivatives in the presence of acids.

A variety of highly functionalized indole-based [n.3.3]propellane derivatives is described. The synthesis of the propellane derivatives involves a Weiss-Cook condensation, a Fischer indole cyclization, and a ring-closing metathesis as key steps.

Indole is a benzopyrrole in which the benzene and pyrrole rings are fused through the 2-and 3-positions of the pyrrole nucleus. The indole derivatives are very much used as anticonvulsant agents. In the same context, several indole derivatives were prepared by the reaction between indole-3carboxaldehyde and various p-substituted phenylsemicarbazides, in the presence of glacial acetic acid. The ...

A series of N-(aminoiminomethyl)-1H-indole carboxamide derivatives were synthesized and their inhibitory potencies against the Na+/H+ exchanger were measured. Variation of the carbonylguanidine group at the 2- to 7-position of the indole ring system showed that a substitution at the 2-position improved the Na+/H+ exchanger inhibitory activity the most in vitro. This led to the synthesis and eva...

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

Although several methods for the preparation of 4o propargyl indole derivatives have been published, this synthetic transformation is complicated by the tendency of 3o propargyl alcohols to form allenium intermediates in acidic media.  It is therefore a challenge to find an efficient method for the C-3 propargylation of indoles with 3° propargylic alcohols.  In this pa...

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

The addition of an allenyl indium intermediate to chiral N-tert-butanesulfinyl imines 7 proceeds with high levels of diastereocontrol. The resulting homopropargylic amine derivatives 10 were transformed into 2-(2-aminoalkyl)benzofuran and indole derivatives 13 and 19, after Sonogashira coupling with o-iodophenol or o-iodoaniline, followed by formation of the heteroaromatic ring through an intra...