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1,2,4-Triazole-3-one prepared from tryptamine was converted to the corresponding carbotioamides by several steps. Their treatment with ethyl bromoacetate or 4-chlorophenacyl bromide produced the corresponding 5-oxo-1,3-thiazolidine or 3-(4-chlorophenyl)-1,3-thiazole derivatives. Acetohydrazide derivative that was obtained starting from tryptamine, was converted to the corresponding Schiff basis and sulfonamide by the treatment with suitable aldehydes and benzensulphonyl chloride, respectively. 2-[(4-Amino-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-3-yl)methyl]-4-[2-(1H-indole-3-yl)ethyl]-5-methyl-2,4-dihydro-3H-1,2,4-triazole-3-one was synthesized starting from hydrazide via the formation of the corresponding 1,3,4-oxadiazole compound, while the other bitriazole compounds were obtained by intramolecular cyclisation of carbothioamides in basic media. The treatment of 1,2,4-triazole or 1,3,4-oxadiazole compound with several amines generated the corresponding Mannich bases. Ethyl (2-amino-1,3-thiazole-4-yl)acetate was converted to the corresponding 1,3,4-oxadiazole derivative, arylidenehydrazides, 1,2,4-triazole-3-one and 5-oxo-1,3-oxazolidine derivatives by several steps. The structural assignments of new compounds were based on their elemental analysis and spectral (FT IR, 1H NMR, 13C NMR and LC-MS) data. The antimicrobial, antilipase and antiurease activity studies revealed that some of the synthesized compounds showed antimicrobial, antilipase and/or antiurease activity.

4-Aryl-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-(thi)oles 5-7, obtained starting from nicotinic acid hydrazide were converted to the corresponding Mannich bases 12-24 by the reaction with several heterocyclic amines in the presence of formaldehyde. The synthesis of S-alkylated compounds 8-11 was performed from the reaction of the corresponding triazol-5-thioles with various alkyl halides. The condensation of carbo(thio)amides 2-4 with 4-chlorophenacyl bromide afforded the corresponding 1,3-thia(oxa)zol-2(3H)-ylidene]pyridine-3-carbohydrazides 25-27. 1,3-Thia(oxa)zolidine derivatives 28-30 were obtained from the cyclization reaction between compounds 2-4 and ethyl bromoacetate. All newly synthesized compounds were screened for their antimicrobial, antiurease, and antilipase activities. The biological activity studies revealed that all the compounds screened showed good or moderate antimicrobial, antiurease, and/or antilipase activity., (© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

1,2,4‐Triazole‐fluoroquinolone and 1,2,4‐triazole–conazole hybrids are designed, synthesized, and investigated in vitro against a variety of common diseases. The structure of the newly synthesized compounds are characterized from spectral data (IR, 1H NMR, 13C NMR, and LC–MS). The antibacterial activity against both Gram‐positive and Gram‐negative bacteria is shown to be enhanced by many of the produced compounds. Also, some of the products are found to have strong antiproliferative effects aganist HeLa cervical cancer cells, whilst demonstrating cytotoxic effects toward normal cells. [ABSTRACT FROM AUTHOR]

Abstract Schiff base derivatives were synthesized in this study via conventional, microwave irradiation and ultrasound sonication methods. Optimization conditions were examined for several parameter such as solvent, reaction time and yield. After determining the optimization conditions, the compounds were synthesized by using ultrasound sonication. The structures of the synthesized compounds were examined by spectral data, and the antiurease, antioxidant and antimicrobial activities of the Schiff bases derivatives were investigated due to the imine group (-C N-) and promising results were obtained. The enzyme inhibitory potentials of these compounds were further validated through molecular docking studies. Also, In Silico ADME prediction studies were calculated for compounds. Highlights • Urease inhibition of newly synthesized Schiff base derivatives. • Screening antimicrobial and antioxidant activity and in silico ADME prediction study of novel drug-like compounds. • Docking studies were performed for the most active compounds and interaction modes with enzyme active sites were determined. • Conventional, microwave and ultrasound prompted synthesis of new Schiff base derivatives. [ABSTRACT FROM AUTHOR]