In this research the goal was to produce novel pyrimidine triazole compounds in high yields using triethylamin as an efficient catalyst. These new compounds were synthesized by using multicomponent reaction of aldehydes, guanidine, electron deficient acetylenic compounds, tert-butyl isocyanide and hydrazonoyle chloride in aqueous media. Due to the presence of an NH group, which was assessed using two different methodologies, newly synthesized pyrimidine triazoles have antioxidant properties. Additionally, the antibacterial activity of newly created pyrimidine triazoles was assessed using the disk distribution method with two different types of Gram-positive bacteria and Gram-negative bacteria, demonstrating that the use of these compounds prevented the growth of bacteria. Applied to the preparation of pyrimidine triazole derivatives, this method has short reaction times, high product yields, and the ability to separate catalyst and product using simple procedures.
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http://dx.doi.org/10.1007/s11030-023-10754-z | DOI Listing |
Biomed Chromatogr
January 2025
Department of Pharmaceutical Sciences, School of Biotechnology and Pharmaceutical Sciences, Vignan's Foundation for Science, Technology and Research, Guntur, India.
Vactosertib, an inhibitor of transforming growth factor β-receptor type-1 (TGFBR1) effective in preventing tumor cell proliferation, is approved for treating various cancers by FDA. The literature revealed that no LC-MS/MS method was reported for the quantification of vactosertib. To develop a validated LC-MS/MS method for the quantification of vactosertib in rat plasma, vactosertib and cabozantinib (internal standard [IS]) were detected using Waters LC-MS/MS system in MRM positive ionization mode, with a mixture of 0.
View Article and Find Full Text PDFMol Divers
December 2024
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, India.
Acquired immunodeficiency syndrome (AIDS) poses a significant threat to life. Antiretroviral therapy is employed to diminish the replication of the human immunodeficiency virus (HIV), extending life expectancy and improving the quality of patients' lives. These HIV-1 integrase inhibitors form robust covalent interactions with Mg ions, contributing to their tight binding, thereby inhibiting the integration of viral DNA into the CD4 cell DNA.
View Article and Find Full Text PDFBioorg Chem
November 2024
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
Front Plant Sci
November 2024
Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing, China.
Recently, due to the widespread use of the acetolactate synthase (ALS)-inhibiting herbicide penoxsulam in paddy fields in China, (L.) P. Beauv.
View Article and Find Full Text PDFPLoS One
December 2024
Department of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Virginia Polytechnic Institute and State University, Blacksburg, Virginia, United States of America.
Aspergillus fumigatus is a widely distributed pathogen responsible for severe infections, particularly in immunocompromised individuals. Triazoles are the primary treatments options for Aspergillus infections; however, the emergence of acquired resistance to this antifungal class is becoming a growing concern. In this study, we investigated the potential of the antiviral drug, lopinavir (LPV) to restore the susceptibility of A.
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