Presence Of Potassium Carbonate Research Articles

Aqueous dispersions of ‘green’ silver nanoparticles for eco-applications: Synthesis, structure and biosafety

Sustainable agriculture requires the use of intelligent compounds with multifaceted effect on soil and plants. Such conditioners can be hydrogels enriched with nanoparticles, but only those synthesized using ‘green chemistry’ methods. Therefore, the main aim of the study was to synthesize and characterize innovative ‘green’ silver nanoparticles (AgNPs) for agricultural applications. AgNPs were created using water or alcohol extracts of eucalyptus (Eucalyptus viminalisLabill) and aloe (Aloë arborescens Mill) as well as tannin to reduce silver ions (Ag+) to zero valent form (Ag0). The synthesis was conducted under autoclave conditions or at room temperature, in the presence of potassium carbonate. The AgNPs characterization was performed by X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and dynamic light scattering (DLS) method, whereas stability of the AgNPs suspensions under various conditions was estimated using turbidimetry. Biosafety of the formed species was determined based on genotoxicity (comet test) and cytotoxicity (study with crystal violet and MTT) assays. The obtained results confirmed the presence of zero valent silver phase in the nanoparticles and showed that their crystallite size was 14–24 nm, with different degrees of polydispersity depending on the synthesis conditions. Hydrodynamic diameter of AgNPs and their aggregates in the aqueous dispersions varied from 6 nm to 103 nm, and the smallest aggregation degree was noted for the nanoparticles synthesized using tannin. All synthesized nanoparticles were biosafe. Thus, they can be applied in agro-industrial processes without damaging the environment.

Construction and characterization of Fe3O4@SiO2-Dop/Amide-BTA-pd(0) nanocomposite as a novel and efficient nanomagnetic recoverable catalyst for synthesis of 5-substituted 1h-tetrazoles in water

The development of efficient, and environmentally friendly catalytic systems for synthesis of 5-substituted 1H-tetrazoles is an important challenge in organic synthesis because tetrazole derivatives are well known in medicinal chemistry with many biological activities such as anti-bacterial, anti-fungal, anti-allergic, anti-viral, anti-cancer, reducing blood pressure, and so on. In this research, we fabricated a palladium(0) complex stabilized on magnetic Fe3O4 nanoparticles modified with dopamine and benzo[d]thiazole-2-carbonyl chloride [Fe3O4@SiO2-Dop/Amide-BTA-Pd(0)] (1) and evaluated its catalytic behavior in the synthesis of 5-substituted 1H-tetrazoles through one-pot tandem reactions of aryl halides with K4[Fe(CN)6] and sodium azide under eco-friendly conditions. One-pot tandem reactions of aryl halides with K4[Fe(CN)6] and sodium azide were conducted using a catalytic amount of 1 in the presence of potassium carbonate in water at 100 °C for 2 h the 5-substituted 1H-tetrazole products were obtained in high to excellent yields. At the end of the reaction, 1 can be easily recycled and the products obtained had high purity.

A Novel Synthesis and Quantitation Route of Belinostat

Introduction: This research article describes the production, quantification, and purification of belinostat from 3-nitrobenzaldehyde as the starting material. A cascade-step process produces higher yields when compared to all previous existing methodologies. Method: The procedure involved the following: Horner–Wadsworth–Emmons (HWE) reaction of aromatic aldehydes with triethylphosphonoacetate in the presence of potassium carbonate, reduction of the nitro group to the amino group, sulfochlorination by thionyl chloride, aniline-mediated sulfonamidation, and hydroxylamine amidation as the last step. Results: The prepared solid belinostat was purified, and an acceptable yield of 56-60% was obtained. Conclusion: The approach has several key benefits, including low-cost beginning materials, straightforward techniques, safer and more reliable results, and substantial environmental advantages.

Synthesis of 1,3‐oxazepine derivatives via tandem reaction of 5‐benzylidine Meldrum's acids with TosMIC in presence of potassium carbonate

Synthesis of 1,3‐oxazepine derivatives via tandem reaction of 5‐benzylidine Meldrum's acids with <scp>TosMIC</scp> in presence of potassium carbonate

A Novel Bis-Trifluoromethylated Compound Demonstrates High Efficacy as a Nematicide Against Root-Knot Nematodes on Pistachio, Supported by Docking Studies.

Three novel trifluoromethylated compounds were designed and synthesized by reacting trifluoroacetimidoyl chloride derivatives with acetamidine hydrochloride or thiourea in the presence of potassium carbonate or sodium hydrogen carbonate as a base. In vitro and in vivo assays demonstrated the efficacy of the tested compounds in controlling root-knot nematode disease on pistachio rootstocks caused by Meloidogyne incognita. Bis-trifluoromethylated derivatives, namely N,N''-thiocarbonylbis(N'-(3,4-dimethylphenyl)-2,2,2-trifluoroacetimidamide) (compound A1), showed high efficacy as novel and promising nematicides, achieving up to 78.28% control at a concentration of 0.042 mg/liter. This effect is attributed to four methyl and two trifluoromethyl groups. In the pre-inoculation application of compound A1, all three concentrations (0.033, 0.037, and 0.042 mg/liter, and Velum) exhibited a higher level of control, with 83.79, 87.46, and 80.73% control, respectively. In the microplot trials, compound A1 effectively reduced population levels of M. incognita and enhanced plant growth at a concentration of 0.037 mg/liter. This suggests that compound A1 has the potential to inhibit hedgehog protein and could be utilized to prevent the progression of root-knot disease. Furthermore, the molecular docking results revealed that compounds A1 and A3 interact with specific amino acid residues (Gln60, Asp530, Glu70, Arg520, and Thr510) located in the active site of hedgehog protein. Based on the experimental findings of this study, compound A1 shows promise as a lead compound for future investigations.

In-silico Studies, Design, and Synthesis of Pyrimidine-linked Benzothiazoles for its Anticonvulsant Potential.

The objective of the study was to design and synthesize a series of N-(6-substituted-1,3-benzothiazole- 2-yl)-2-{[6-(3-substitutedphenyl)-5-cyano-2-sulfanylpyrimidine-4-yl)]amino}acetamide derivatives BPD (1-15) that contains key pharmacophores required for anticonvulsant action. The titled compounds (BPD 1-15) were synthesized by reacting 2-substituted-N-(6-chlorobenzo[d]thiazol2-yl)acetamide with 4-amino-6-(4-substituted phenyl)-2-mercapto pyrimidine 5-carbonitrile in the presence of potassium carbonate and dry acetone. The synthesized compounds BPD (1-15) were assessed in vivo by the maximum electric shock (MES) test and the subcutaneous pentylenetetrazol (scPTZ) test in mice. The neurotoxicity test was performed by the rotarod test. A molecular docking study of title compounds with a sodium channel receptor (PDB ID: 1BYY) was carried out using the SP Docking protocol of the Glide module of the Maestro. Pharmacophore modeling was used to qualitatively identify the chemical characteristics for ligand binding and their spatial configurations in the 3D space of the active site. Among the studied compounds, BPD-15 and BPD-5 compounds showed significant action in both the MES and scPTZ models, with no neurotoxicity. BPD-15 & BPD-5 were relatively safe in acute toxicity testing. Compounds BPD-15 and BPD-5 showed good dock scores of -6.434 and -6.191, respectively. Thus, the compounds BPD-15 and BPD-5 have shown a considerable affinity towards the sodium channel as compared to the standard drug Riluzole. Compound BPD-14 showed good drug compatibility, and compounds BPD-1, BPD-2, BPD-11, BPD-12, BPD-13, BPD-14, BPD-15 showed good ADME values.

New Synthesis of 2-Aminopyrimidines by Amination of Biginelli Reaction Products — Oxadiazocines

Abstract Previously, we synthesized methanobenzo[g][1,3,5]oxadiazocines and methanonaphtho[2,3-g]­[1,3,5]oxadiazocines via the Biginelli reaction using thiourea with acetoacetic ester or acetylacetone and salicylaldehyde or 2-hydroxy-1-naphthaldehyde under acidic catalysis and microwave irradiation. These compounds were then subjected to alkylation reaction with ethyl bromide in the presence of potassium carbonate in dimethylformamide. Under these mild reaction conditions, possible thione-thiol tautomerism of the oxadiazocines, as well as their structural analogs of cyclic thioureas, predominantly yielded in S-alkylation products with minor amounts of N-alkylation products. Further nucleophilic substitution reactions of S-ethyl-methanobenzo[g][1,3,5]oxadiazocines and S-ethyl-methanonaphtho[2,3-g][1,3,5]oxadiazocines revealed that alongside nucleophilic substitution by morpholine, elimination of phenol or naphthol occurred, followed by aromatization of the dihydropyrimidinone ring into an aromatic pyrimidine ring, resulting in the formation of 2-morpholinyl-substituted pyrimidines. Only a few examples and multi-step syntheses for obtaining such 2-amino-substituted pyrimidines are presented in the literature. Therefore, our newly discovered method for obtaining widely demanded derivatives of 2-aminopyrimidines is presented both relevant and promising.

Synthesis of N-heterocyclic carbene gold(I) complexes from the marine betaine 1,3-dimethylimidazolium-4-carboxylate.

The marine natural product norzooanemonin (1,3-dimethylimidazolium-4-carboxylate) has been used to prepare a series of carboxyl- or carboxylate-functionalized N-heterocyclic carbene (NHC) gold(I) complexes from [(Me2S)AuCl] in the presence of potassium carbonate. The potential of the resulting mono- and dicarbene complexes to act as cytotoxic or antibacterial drugs was investigated.

Directional transformation and migration pathways of nitrogen during pig manure supercritical water gasification

Nitrogen is a valuable nutrient element in pig manure. This work focuses on investigating the distribution, directional transformation, and migration pathways to facilitate the recovery of nitrogen from supercritical water gasification products. Results indicated that no nitrogen-containing gas was detected and 12.65 % of nitrogen remained in solid products. 82.49 % of nitrogen migrated into liquid products, which are predominated by ammonia. Catalysts were employed to promote the conversion of solid nitrogen to liquid nitrogen and organic nitrogen to ammonia. Finally, 85 % of nitrogen is enriched into liquid products and ammonia predominated the liquid nitrogen. The percentage of ammonia increased to 97.51 % at 620 °C in the presence of potassium carbonate. The migration pathways indicated that nitrogen was transformed into ammonia by various intermediates such as indole. The rest of the nitrogen remained in solid products with stable quaternary-nitrogen. These findings provide valuable insights into nitrogen management and recovery.

Synthesis and Biological Evaluation of 1-Substituted (R)-6-(2?-Cyano-1?-Pyrrolidin-yl)-4-(3?- Hydroxyadamantan-1?-yl)-3-phenyl-1,2,4-triazines

A series of various 1-substituted (R)-6-(2?-cyano-1?-pyrrolidin-yl)-4-(3?-hydroxy adamantan-1?-yl)-3-phenyl- 1,2,4-triazines (5a-i) was synthesized by the reaction of (R)-6-(2?-cyano-1?-pyrrolidin-yl)-4-(3?-hydroxy adamantan-1?- yl)-3-phenyl-1,4-dihydro-1,2,4-triazine (4) with heterocyclic halogenated compounds (R-X) in the presence of potassium carbonate. All the synthesized compounds were evaluated biologically and also determined In vitro cytotoxicity of compounds 5a, 5c, 5d, 5e, 5g, and 5h against human cervical cancer cell line (HeLa). Among all the synthesized compounds, some compounds exhibited potent antimicrobial activity as well as cytotoxicity.. KEYWORDS :1,2,4-Triazine, Adamantanol, Biological activities, Pyrrolidine.

Microwave Synthesized Hydrophilic 4‐Oxo‐2‐phenylquinazoline‐3(4H)–carboximidamide and –Carboxamide as Privileged Small Molecule Scaffolds with Anti‐HIV‐1 Activities

AbstractOpportunistic infections like tuberculosis (TB) are prevalent in HIV‐infected individuals. In an approach to introducing an industrial‐scale microwave‐assisted production of agents having both antiviral and antibacterial properties, a set of hydrophilic 2,3‐substituted quinazolinones, 4‐oxo‐2‐phenylquinazoline‐3(4H)‐carboximidamide (Qg) and 4‐oxo‐2‐phenylquinazoline‐3(4H)‐carboxamide (Qu), were afforded in encouraging yields. They were obtained by treating 2‐benzamidobenzoyl chloride with guanidine hydrochloride or urea in the presence of potassium carbonate in DMF. DFT calculations were employed for geometrical optimization and vibrational frequency analysis of the compounds. Free energies of solvation (ΔGsol) of Qg, and Qu calculated using DFT lend evidence in support of their hydrophilicity The anti‐HIV‐1 activities of the small‐molecule quinazolinone derivatives Qg and Qu were investigated. The synthons under in vitro conditions inhibit the entry of HIV in receptor cells with low cytotoxicity (EC50=50.53 nM for Qu and EC50=97.92 nM for Qg). The study identifies the antiviral properties of the two benzo‐fused pyrimidine derivatives, which were earlier reported to have antitubercular activity. Our findings indicate the scope for further synthetic explorations of these quinazolinone scaffolds that can lead to developing promising alternatives in drug design, pharmaceutics, and clinical research.

Synthesis of Bis‐Nicotinonitrile Derivatives and Investigations of Antimicrobial and Antibiofilm Activities

AbstractIn this study aimed to the synthesis of novel bis‐nicotinonitrile derivatives starting from 1,3‐bis‐chalcones and investigate their antimicrobial activity potentials. Bis‐nicotinonitrile derivatives were synthesized from 1,3‐bis‐chalcone derivatives reacted with malononitrile in ethanol in the presence of potassium carbonate. Characterization of the obtained compounds was carried out by spectroscopic methods. In total, 12 new 1,3‐phenylene‐bis‐nicotinonitrile derivatives were synthesized. Finally, the antimicrobial and antibiofilm activities of synthesized 1,3‐phenylene‐bis‐nicotinonitrile derivatives were tested against 5 microorganisms. As a result, it was observed that the synthesized new nicotinonitrile derivatives were quite active especially in terms of antibiofilm activity.

Enhanced LC-ESI-MS/MS Sensitivity by Cationic Derivatization of Organophosphorus Acids.

The chemical derivatization to enhance the signal intensity and signal-to-noise (S/N) of several organophosphorus (OP) acids in liquid chromatography tandem mass spectrometry (LC-ESI-MS/MS) is illustrated. The OP class of compounds represents the environmental degradants of OP nerve agents and pesticides. N-(2-(bromomethyl)benzyl)-N,N-diethylethanaminium bromide (CAX-B) was utilized to derivatize a panel of eight acids consisting of five alkyl methylphosphonic acids (ethyl-, isopropyl-, isobutyl-, cyclohexyl-, and pinacolyl-methylphosphonic acid) along with three dialkylphosphate analogs (diethyl-, dibutyl-, and diethyl thio-phosphate). The derivatization reaction with CAX-B was conducted in acetonitrile in the presence of potassium carbonate at 70 °C for 1 h. The resulting acid derivatives were analyzed with an LC-Orbitrap-ESI-MS/MS, and their dissociation processes were investigated. It was found that the derivatization procedure increased the limits of identification (LOIs) by one to over two orders of magnitude from the range of 1 to 10 ng/mL for the intact OP-acids to the range of 0.02-0.2 ng/mL for the derivatized acids utilizing an LC-MS(QqQ) in MRM mode, regardless of the sample matrix (hair, concrete, or plant extracts). The interpretation of the corresponding ESI-MS/MS spectra for each type of derivatized sub-OP family revealed the formation of characteristic neutral losses and a characteristic ion for the organophosphorus core. This derivatization is beneficial and useful for screening and identifying target and "unknown" OP acids.

Synthesis of 4-(Phenylchalcogenyl)tetrazolo[1,5-a]quinolines by Bicyclization of 2-Azidobenzaldehydes with Phenylchalcogenylacetonitrile.

A general methodology to access valuable 4-(phenylchalcogenyl)tetrazolo[1,5-a]quinolines was developed by the reaction of 2-azidobenzaldehyde with phenylchalcogenylacetonitriles (sulfur and selenium) in the presence of potassium carbonate (20 mol%) as a catalyst. The reactions were conducted using a mixture of dimethylsulfoxide and water (7:3) as solvent at 80 °C for 4 h. This new methodology presents a good functional group tolerance to electron-deficient and electron-rich substituents, affording a total of twelve different 4-(phenylchalcogenyl)tetrazolo[1,5-a]quinolines selectively in moderate to excellent yields. The structure of the synthesized 4-(phenylselanyl)tetrazolo[1,5-a]quinoline was confirmed by X-ray analysis.

Syntheses, crystal structures and Hirshfeld surface analysis of 2-(benzyl-sulfan-yl)-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole and 2-[(2-chloro-6-fluoro-benz-yl)sulfan-yl]-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole.

The title compounds were synthesized by alkyl-ation of 5-[(4-di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole-2-thiol with benzyl chloride or 2-chloro-6-fluoro-benzyl chloride in the presence of potassium carbonate. The yields of 2-(benzyl-sulfan-yl)-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole, C17H17N3OS (I), and 2-[(2-chloro-6-fluoro-benz-yl)sulfan-yl]-5-[4-(di-methyl-amino)-phen-yl]-1,3,4-oxa-diazole, C17H15ClFN3OS (II), were 96 and 92%, respectively. In the crystal structures of (I) and (II), C-H⋯π inter-actions are observed between neighboring mol-ecules. Hirshfeld surface analysis indicates that H⋯H and H⋯C/C⋯H inter-actions make the most important contributions to the crystal packing.

Synthesis, Antibacterial, and Antifungal Evaluation of Some New Quinazolinone-Azole Hybrids

Nowadays, the need to replace the existing drugs is felt more than ever by increasing drug resistance. Quinazoline is one of the major heterocyclic compounds in biological activity. This research was done to synthesize new derivatives of quinazolin-4(3H)-one and evaluation of their antibacterial and antifungal properties. Ten new quinazolin-4(3H)-one derivatives (5(a–d), 6(a–d), and 7(a,b)) were synthesized by using the nucleophilic substitution reaction of 2-(chloromethyl)-3-(4-chlorophenyl) quinazolin-4(3H)-one (4) and the heterocyclic moieties of 1,3,4-oxadiazole I(a–d) or 1,2,4-triazole (II(a–d), III(a,b)) in the presence of potassium carbonate as base and in acetone as solvent. The chemical structures of the products were approved using 1H-NMR, 13 C-NMR, IR, and Mass spectroscopy. The antimicrobial activity of the compounds was assessed against a panel of Gram-positive and Gram-negative bacteria and species of Candida and Aspergillus fungal. Minimum inhibitory concentration (MIC), minimum bactericidal/fungicidal concentration (MBC/MFC), and inhibition zone (IZ) of these compounds were determined. As results shown, 7a showed better effects against Staphylococcus epidermidis, Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, and Pseudomonas aeruginosa than the other compounds. However, 5d showed better effects against Proteus vulgaris. Compound 6b showed better effects against Candida albicans, Aspergillus fumigatus, and Aspergillus niger, also compound 5a showed better effects against Candida glabrata.

2-(3-Bromophenyl)imidazo[2,1-b]oxazole

The microwave-assisted reaction of 2-nitroimidazole with 3-bromophenacyl bromide in the presence of potassium carbonate as a base and dimethylformamide as a solvent afforded 2-(3-bromophenyl)imidazo[2,1-b]oxazole. The formation of this compound was explained via a domino mechanism comprising an initial N-alkylation reaction of the imidazole substrate, followed by the base-promoted deprotonation of the position adjacent to the carbonyl to give an enolate anion that finally cyclizes via an intramolecular SNAr reaction, with the loss of the nitro group as potassium nitrite. Then, the proposed 1-(3-bromophenacyl)-2-nitroimidazole intermediate could be isolated by reducing the reaction time and was shown to be a precursor of the imidazo[2,1-b]oxazole final product.

Microwave-assisted Synthesis of 3-amino-2-phenylquinazolin-4(3H)-one (QH) and 4-oxo-2-phenylquinazoline-3(4H)-carbothioamide (QTh)

Background: Microwave synthesis has developed as a powerful tool for the cost-effective and greener synthesis of organic molecules, including quinazolines. Irradiation with microwave leads to the excitation of molecules and equitable distribution of thermal energy in a much shorter time than conventional synthesis. This results in shorter reaction time and, more often than not, higher efficiency Objective: The primary objective of the work presented in this article was to prepare hydrazine hydrate or thiourea derivative of quinazolines through microwave synthesis as small-molecule scaffolds for fur-ther need-based functionalisation, isolation, and characterisation. We, herein, report the synthesis of two quinazolinone derivatives of thiourea and hydrazine, 3-amino-2-phenylquinazolin-4(3H)-one (QH) and 4-oxo-2-phenylquinazoline-3(4H)-carbothioamide (QTh), respectively. Method: A multi-step synthetic strategy starting from anthranilic acid was employed to synthesise the small molecule quinazolinones 3-amino-2-phenylquinazolin-4(3H)-one (QH) and 4-oxo-2-phenylquinazoline-3(4H)-carbothioamide (QTh). The compounds were synthesised by reacting hydra-zine and thiourea with 2-benzamidobenzoyl chloride in DMF under microwave irradiation (800 W at 135 °C for 4 min) in the presence of potassium carbonate. The acid chloride was prepared by chlorination of 2-benzamidobenzoic acid, which in turn was synthesised from anthranilic acid by benzoylation. This method is an efficient alternative approach to synthesising quinazolinones from benzoxazin-4-ones. Results: We have successfully synthesised, isolated, and characterised the quinazolinone derivative QH (yield: 81%) and QTh (yield: 85%). The structures of the compounds were established through spectro-scopic techniques. Theoretical optimisation of the structures was also achieved using DFT. The HOMO-LUMO difference for QH and QTh was calculated to be 4.60 and 4.47 eV, respectively. Conclusion: The reported protocol is advantageous over conventional methods of quinazoline synthesis from benzoxazin-4-ones. The time required for the reaction is much less (4 min) as compared to the usual requirements of reflux (&gt; 4 h); the higher energy gap of QH indicates greater stability than that of QTh.

A novel, swift, and effective green synthesis of morpholino-pyridine analogues in microwave irradiation conditions

We report a facile, efficient, and environmentally benign approach for preparing morpholino-linked 1,4-dihydropyridine derivatives. The four-component fusion of morpholin-4-amine, diethyl acetylene dicarboxylate, malononitrile, and chosen substituted benzaldehydes occurred under microwave irradiation under mild conditions in the presence of potassium carbonate as a catalyst. This protocol offers remarkable benefits such as excellent yields (92–98 %), easy handling, simple workup, economy, cleaner reaction profile, green conditions, shorter reaction time (≤10 min), and avoiding column chromatography for purification.

Search for fungistatics in the imidazole series

New imidazole derivatives with fungistatic activity were synthesized at the NCRSRVI branch of FSBSC Federal Rostov Agrarian Scientific Center. The initial compound 4,5-dichlorimidazole was obtained according to the method described in the literature [3]. Structures 1, 4, 6, 7, 8 - 11, 14 - 17, 19, 20, 22, 24 they were synthesized by alkylation of 4,5-dichlorimidazole with corresponding halide alkyls in an alkaline medium. Alcohol 5 was obtained by reducing ketone with sodium borohydride in ethanol. Bigeterocycles 10, 13 were obtained by the reaction of 4,5-dichlorimidazole with corresponding chloronitropyridines by boiling in dimethylformamide in the presence of potassium carbonate. Compound 10 was obtained under similar conditions, but ortho-chloronitrobenzene was used as an aryl derivative. The preparation 23 was obtained by acylation using a chlorocarbon ester of the corresponding N-(4-aminophenylmethyl) 4,5-dichlorimidazole, which, in turn, was synthesized from a nitro derivative by reduction with iron in ethanol in the presence of a catalytic amount of hydrochloric acid. Preparation 18 is obtained from the methyl ester of 4,5-dichlorimidazole and acetic acid and hydrazine in an alcoholic medium. The study of fungistatic activity showed that the size of the culture growth retardation zone crucially depends on the type of substituents in the nitrogen atom of the imidazole cycle. First of all, this applies to the lipophilicity of the substituent: the higher the lipophilicity (of the compound 1, 4, 6, 7, 20, 22-24), the higher the activity of the connection. However, lipophilicity obviously should not exceed certain limits: the most lipophilic compounds 2 and 3 are significantly inferior in activity to slightly less lipophilic compounds 1, 4, 6, 7, 20, 22-24. Polar substituents of the nitrogen atom (compounds 5, 8, 11, 16-18, 23) completely suppress fungistatic activity. The aryl substituent of the nitrogen atom of the imidazole ring (compound 10), as well as the nitrogetaryl substituents (compounds 12 and 13) have significant fungistatic activity.