The synthetic procedures to obtain indole derivatives with different acidic functions at position 2 of the indole are reported. The synthesised and tested derivatives comprise 5-tetrazolyl, 1,3,4-oxadiazol-5-yl-2-one, and indole-2-carboxylic acid amides with 5-aminotetrazole, methanesulphonamide and trifluoromethanesulphonamide moieties. The binding affinity was evaluated using [3H]MDL 105,519 ...

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...

Tropical parasitic diseases such as Chagas disease and leishmaniasis are considered a major public health problem affecting hundreds of millions of people worldwide. As the drugs currently used to treat these diseases have several disadvantages and side effects, there is an urgent need for new drugs with better selectivity and less toxicity. Structural modifications of naturally occurring and s...

licles pigmentation in mammals. Melanin biosynthesis or melanogenesis occurs in specialized organelles, called melanosomes, through a cascade of enzymatic reactions using the amino acid tyrosine as the initial substrate. The first two steps in the biosynthetic pathway, hydroxylation of tyrosine to L-3,4-dihydroxyphenylalanine (L-DOPA) and oxidation of L-DOPA to dopaquinone, are catalyzed by tyr...

An important event in the formation of atherosclerotic lesions is the uptake of modified low density lipoprotein (LDL) by macrophages via scavenger receptors. Modification of LDL, which results in its recognition by these receptors, can be initiated by peroxidation of LDL lipids. The first step in this process is the formation of monohydroperoxy derivatives of fatty acids, which are subsequentl...

Determination of the appropriate conditions for protein crystallization remains a highly empirical process. Preventing protein aggregation is necessary for the formation of single crystals under aggregation-prone solution conditions. Because many amino acids and amino acid derivatives offer a unique combination of solubility and stabilizing properties, they open new avenues into the field of pr...

Zinc(II) complexes with dangling functional organic groups were synthesized by reaction of zinc acetate with a series of bifunctional p-substituted benzene derivatives (a combination of carboxylate, oximate, amino, β-ketoimine, and salicylaldime groups). Selective coordination to carboxylate groups was observed when the second functional group was an oxime or β-ketoimine group. When the second ...

Benzoic acids are highly important structural motifs in drug molecules and natural products. Selective C-H bond functionalization of benzoic acids will provide synthetically useful tools for step-economical organic synthesis. Although direct ortho-C-H functionalizations of benzoic acids or their derivatives have been intensely studied, the ability to activate meta-C-H bond of benzoic acids or t...

Pills of Mefenamic acid were  employed as effective catalysts in the three component reaction of aromatic  aldehydes,  malononitrile,  as  well  as  4-hydroxycoumarin  or  barbituric  acid  in  aqueous solution,  using  reflux  conditions  in  order  to  synthesize  derivatives  of  dihydropyrano[2,3-c]chromene and pyrano[2,3-d]pyrimidine, correspondingly. Among the benefits of this technique, ...