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A new family of mono‐ (3a‐h) and bis‐ (4a‐g) isoxazole‐bridged silatranes has been synthesized by the reaction of 3‐aminopropylsilatrane (1) and 3‐substituted 5‐chloro‐methylisoxazoles (2a‐h). The structure of the isoxazole‐silatrane hybrids is characterized by elemental analysis, FT‐IR, UV, NMR (1H, 13C,29Si and 15N) spectroscopy, high‐resolution mass spectrometry, and X‐ray diffraction analysis. The in silico ADME (absorption, distribution, metabolism, excretion) assessment reveals that properties of mono‐adducts (3a‐h) are similar to those of drugs obeyed to the Lipinski's rule. The calculated screening of potential pharmacological activity profiles (in silico PASS program) of isoxazole‐silatranes shows that all synthesized compounds (both mono‐ and bis‐substituted) may have high antitumor action, unlike starting isoxazoles. The preliminary screening of the synthesized silatranes for antimicrobial activity against Enterococcus durans, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa indicates that all test samples are active only against gram‐positive microorganisms. Silatrane 3f displays minimal inhibitory concentration (MIC 12.5 and 6.2 μg ml−1) against E. durans and B. subtilis as compared with standard drug gentamicin (MIC 25 and 50 μg ml−1).

This review article summarizes the data on the synthesis, physicochemical properties, structure, reactivity and actual or potential pharmacological activity novel atranes and their analogs synthesized based on biogenic 2‐hydroxyethylamines (and other amines containing the NCH2CH2OH structural unit), biologically active (het)arylchalcogenylacetic acids, and essential metals.

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A general method for the synthesis of 1 alkyl(allyl)(benzyl) substituted (indol 3 yl) sulfanylalkanecarboxylic acids and hexane 1,6 diyl(1,4 phenylenemethylene)bisindol 3 yl sulfanylalkanecarboxylic acids from the corresponding N substituted indoles and bisindoles, thiourea, iodine, and halogencarboxylic acids was developed. The oxidation of substituted (indol 3 yl)sulfanylalkanecarboxylic acids for the first time afforded their analogs containing the sulfonyl group. New (2 hydroxyethyl)ammonium salts of 1 R indol 3 ylsulfanyl(sulfonyl) alkanecarboxylic acids, which are structural analogs of highly active immunomodulators of indacetamin and VILIM, were synthesized. Among the studied (2 hydroxyethyl)ammonium salts of 1 R indol 3 ylsulfanylacetic and sulfonylalkanecarboxylic acids, the compounds exhi biting high dose dependent antiproliferative activity by the ability to affect the spontaneous and mitogen stimulated splenocyte proliferation of mice in vitro were found.Tris(2 hydroxyethyl)ammonium salts of aroxyacetic acids, whose cation has the compact tricyclic atrane (2,8,9 trihydroprotatrane) structure favoring the penetra tion of a substance through cell membranes, are a new class of pharmacologically active substances. 1 They pos sess 2-12 anti aggregation, membrane stabilizing, antiox idant, antisclerotic, antiphlogistic, cardiotropic, analge sic, hypocholesterolemic, immunomodulating, and anti tumor activity considerably exceeding or different from the effect of the initial biologically active acids and trieth anolamine.Earlier synthesized analogs of these compounds, viz., alkanolammonium salts of (het)arylsulfanyl (sulfonyl)acetic acids (Het)ArS(SO 2 )CH 2 COO -• •N + R 1 R 2 (CH 2 CH 2 OH) n (R 1 , R 2 = H, Alk, CH 2 CH 2 OH; n = 1-3), 13-15 and their complexes with salts of biomicroelements 16,17 are lowly toxic (LD 50 = = 1300-6000 mg kg -1 ), also exhibit high and diverse bio logical activity, such as hemo and immunotropic, car diotropic, antiphlogistic, antithrombotic, antioxidant, adaptogenic, hypocholesterolemic, etc., and are highly ef ficient growth stimulating preparations for biotechnolog ical processes. 18,19 Biological activity of alkanolammonium salts of sulfur containing acids is not inferior and often exceeds the activity of related alkanolammonium salts of aroxyacetic acids. The activity is enhanced with an increase in the oxidation state of the sulfur atom and depends on the structure of the (2 hydroxyethyl)ammonium fragment. 14, 15 Indole derivatives, 20 in particular, (indol 3 yl)sulfanyl alkanecarboxylic acids and their salts, are worthy of spe cial attention as biologically active substances, 21 interme diates for the synthesis of medical preparations 22-24 and technically valuable products. 25 We have earlier found by screening efficient non toxic (LD 50 = 1300-3000 mg kg -1 ) immunoactive compounds, viz., tris(2 hydroxyethyl)ammonium indol 3 yl and 1 benzylindol 3 ylsulfanyl acetates (indacetamin and VILIM, respectively).Indacetamin has a wide range of biological activity and is an e...