Two different series of N-substituted heteroaromatic compounds related to clotrimazole structure were synthesized. In one series ortho-cholortrityl moiety of clotrimazole was replaced by trityl, mono or dimethoxy trityl (series c). In the second series the imidazole ring of clotrimazole was also replaced by benzimidazole (series d). Chemical structures of all the new compounds were confirmed by spectrophotometric methods. These compounds docked into the active site of MT-CYP51 (PDB code, 1E9X) using Autodock tools software. They showed good affinity for the enzyme comparable to clotrimazole. Antifungal activities for these compounds were evaluated against Trichophyton mentagrophytes, Microsporum gypseum and Candida albicans using PDA as media, CHCl 3 or DMSO as solvents and agar dilution assay as method. In this method 1-triphenylmethyl-imidazole (1c), 1-(bis-4-methoxyphenyl)-phenylmethyl-benzimidazole (6d) and 1-(4-methoxyphenyl)-diphenylmethyl-imidazole (2c) showed 100%, 90% and 70% activity respectively. In the second step all of the derivatives also were evaluated against Trichophyton rubrum, Microsporum canis and Epidermaphyton floccosum using PDA medium by agar dilution method. In this method 1-triphenylmethyl-imidazole (1c) and 1-(bis-4-methoxyphenyl)-phenylmethyl-benzimidazole (6d) showed 100% and 1-(4-methoxyphenyl)-diphenylmethyl-imidazole (2c) and 1-(bis-4-methoxyphenyl)-phenylmethyl-imidazole (3c) more than 75% activity against the fungi. Then the most active analogues (1c, 2c and 6d) were tested in RPMI 1640 medium which showed desirable biological activity in comparison to clotrimazole.

Herein, we report a chemoselective 1,3‐dipolar cycloaddition reaction between 5‐alkylidene‐ or 5‐arylidene rhodanine derivatives and nitrile oxide generated in situ from dibromoformaldoxime to construct 1,3‐thiazolidine‐2,4‐dione scaffold under mild conditions. This strategy exhibits a distinguished manner to afford thiazolidine derivatives in a simple, rapid and practical route. The results proved that the reaction proceeds through an unpredictable rearrangement and no spirocyclic product is generated. The structures of the target molecules were confirmed by IR, 1H NMR, 13C NMR, mass spectra and unambiguously X‐ray crystal structure analysis.

A series of new indeno[1,2‐b]quinoxaline compounds containing pyrrolopyrimidine skeleton have been synthesized in excellent yields using an improved and efficient synthetic methodology under ultrasonic irradiation in the absence of any added catalyst. The reactions were carried out under both thermal and ultrasonic irradiation condition. In general, obvious improvement in reaction time and milder conditions were observed when reactions were carried out under sonication compared with conventional silent conditions.

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The present investigation reports an easy regio-and diastereoselective access to a library of diverse polycyclic pyrrolizidine fused spiro-1,3-indandione/oxindole derivatives through a onepot sequential four-component reactions of 4-oxo-4H-chromene-3-carbaldehyde/2-chloroquinoline-3-carbaldehyde, 1-phenyl-2-(1,1,1-triphenyl-λ 5 -phosphanylidene)ethan-1-one, ninhydrin or isatin, and L-proline in EtOH at room temperature. This protocol features excellent chemical yields, high diastereoselectivity and operational simplicity.

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A convenient and effective one‐pot synthetic method for functionalized 1H‐thiopyrano[4,3‐c]quinoline scaffold via three‐component cyclization is described. This procedure contains the reaction between 2‐chloroquinoline‐3‐carbaldehyde and 2 equivalents of phenacyl thiocyanate in the presence of triethylamine in absolute ethanol at room temperature with good yield. This eco‐friendly method has advantages such as reduction of waste, short synthetic procedure, and little amount of required reagents.