Keywords
Abstract
Due to its chemical reactivity, indole was modified to obtain a large number of new molecules, which were later successfully used as drugs for various diseases. In recent years, many studies have been con- ducted on the synthesis and investigation of the therapeutic prospects of this compounds, focused on the structure-activity relationship to identify active pharmacophores and offer a platform for the development of new indole derivatives.
The purpose of the study is to consider the pharmacological properties and use of known drugs and new remedies among indole derivatives.
To achieve the goal, literary sources devoted to the structure, pharmacodynamics, mechanisms of action and indications of indole derivatives used in the clinic or undergoing clinical trials were analyzed.
In pharmacology, indole alkaloids are widely known, in particular, alkaloids of rauwolfia (reserpine, aimaline), ergot (ergometrine, ergotamine), yohimbe (yohimbine), passionflower (as part of the drugs «Novopasit», «Central-B»), pink periwinkle (vinblastine and vincristine), minor periwinkle (vincamine), iboga ( (ibogaine). Chemical substitutes create a wide selection of structures of indole derivatives (oxoin- doles, isoindoles, pyridoindoles). Among them, there is a large number of agents that affect effector organs and metabolism, exerting anti-inflammatory, broncholytic, hypoglycemic or osteoprotective action, regulating the functions of the gastrointestinal tract. These drugs include indomethacin, pravadolin, zafirlukast, ecopladib, varespladib, lidorestat, bazedoxifene, and tegaserod. There are substituted indoles with antitumor properties (sunitinib, lenalidomide, apaziquone and others), which associated with induc- tion of apoptosis, inhibition of aromatase, regulation of estrogen receptors, inhibition of tyrosine kinase, or tubulin assembly. There are many neurotropic agents among indole derivatives, and these are not only indole alkaloids. These include ziprasidone (an atypical antipsychotic), roxindol (an anxiolytic and antide- pressant with antiparkinsonian action), siramesin (an anxiolytic and antidepressant), tropisetron (anti- emetic), pindolol (beta-adrenergic blocker). Indole derivatives are characterized not only by their effect on the macroorganism, but also by antimicrobial, in particular, antiviral activity: for example, delavirdine and atevirdine are used for the treatment of HIV infection.
Therefore, indole derivatives represent an important class of molecules for pharmacology, are actively studied and have significant clinical potential. The search for promising substances with pronounced phar- macological activity and low toxicity is still going on both among natural compounds and synthetic homo- logues of indole to replenish the list of existing drugs.