Substituted Acyl Thioureas and Acyl Thiosemicarbazides: Synthesis and Biological Activity (Minireview)

Acyl isothiocyanates and their functional derivatives (acyl thioureas and acyl thiosemicarbazides) are an important group of organic compounds that are widely used in the synthesis of heterocycles and in chemistry as catalysts, ligands, colorimetric hemosensors, etc. In recent years, there has been an increased interest towards this class of compounds as promising biologically active compounds, especially since the latest advances in medicinal chemistry for them are not sufficiently studied. The aim. To summarize and systematize information for the last 10 years on methods of synthesis and biological activity of substituted acyl thioureas and acyl thiosemicarbazides. Materials and methods. Web-tools for finding scientific information (Reaxys, Scopus, Google Scholar, ScienceResearch, SciFinder, Web of Science, etc.). Results and discussion. Literature sources related to the methods of synthesis of substituted acyl thioureas and acyl thiosemicarbazides were systematized and analyzed. The main approaches for the formation of these compounds are revealed: stepwise formation from carboxylic acids, through acyl chlorides and acyl isothiocyanates followed by nucleophilic addition of amines or hydrazides of carboxylic acids ("one-pot synthesis"), nucleophilic addition of amines or hydrazides of carboxylic acids directly to acyl isothiocyanates and parallel microwave synthesis using acyl isothiocyanates and amines as reagents. The possibility of their use as ligands for the formation of complex compounds with transition metal ions was discussed. In the review biological activity of these structures, namely antimicrobial, fungicidal, antitumor, antiviral, antifungal and other activities was detailazed. Conclusions. The basic approaches to the synthesis of substituted acylthuoureas and acyl thiosemicarbazides which include the application of carboxylic acids, their derivatives (acyl halides and isothiocyanates) and N-nucleophiles as initial compounds were discussed. It was shown that aforementioned class of the compounds reveals the versatile biological activity and are promising for further structural modification aimed to the search of novel drug

Representation of a Monotone Curve by a Contour with Regular Change in Curvature

The problem of modelling a smooth contour with a regular change in curvature representing a monotone curve with specified accuracy is solved in this article. The contour was formed within the area of the possible location of a convex curve, which can interpolate a point series. The assumption that if a sequence of points can be interpolated by a monotone curve, then the reference curve on which these points have been assigned is monotone, provides the opportunity to implement the proposed approach to estimate the interpolation error of a point series of arbitrary configuration. The proposed methods for forming a convex regular contour by arcs of ellipses and B-spline ensure the interpolation of any point series in parts that can be interpolated by a monotone curve. At the same time, the deflection of the contour from the boundaries of the area of the possible location of the monotone curve can be controlled. The possibilities of the developed methods are tested while solving problems of the interpolation of a point series belonging to monotone curves. The problems are solved in the CAD system of SolidWorks with the use of software application created based on the methods developed in the research work

Interpolation with Specified Error of a Point Series Belonging to a Monotone Curve

The paper addresses the problem of modeling a smooth contour interpolating a point series belonging to a curve containing no special points, which represents the original curve with specified accuracy. The contour is formed within the area of possible location of the parts of the interpolated curve along which the curvature values are monotonously increased or decreased. The absolute interpolation error of the point series is estimated by the width of the area of possible location of the curve. As a result of assigning each intermediate point, the location of two new sections of the curve that lie within the area of the corresponding output section is obtained. When the interpolation error becomes less than the given value, the area of location of the curve is considered to be formed, and the resulting point series is interpolated by a contour that lies within the area. The possibility to shape the contours with arcs of circles specified by characteristics is investigated