ABSTRACT
It is the first report of the novel amalgamation of 1,2,3-triazoles, piperidines, thieno pyridine rings and evaluation of their antifungal activity. The synthesized compounds showed interesting moderate to good antifungal activity, wherein they were able to discriminate between the two species Aspergillus flavus and Aspergillus niger of the same genus. In addition, the main highlight of this series is the sensitivity of the fungal strain Cryptococcus neoformans to the compounds having p-chlorobenzoyl (9h), methane sulfonyl (9i) and p-methylbenzene sulfonyl (9j) attached to the piperazine nitrogen.
Subject(s)
Antifungal Agents/pharmacology , Piperidines/pharmacology , Pyridines/pharmacology , Triazoles/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Aspergillus flavus/drug effects , Aspergillus niger/drug effects , Cryptococcus neoformans/drug effects , Dose-Response Relationship, Drug , Microbial Sensitivity Tests , Molecular Structure , Piperidines/chemical synthesis , Piperidines/chemistry , Pyridines/chemical synthesis , Pyridines/chemistry , Structure-Activity Relationship , Triazoles/chemical synthesis , Triazoles/chemistryABSTRACT
It is the first report of 1,3,4,5-tetrasubstituted 1,2,3,6-tetrahydropyrimidines derivatives, catalyzed by ZrOCl2. The mild reaction conditions, excellent yields in shorter reaction time and evasion of cumbersome workup procedures make this process economically lucrative for industrial application. The novelty and highlight of the present method is the promising antibacterial and antifungal activity shown by compounds (4a, 4b, 4e, 4f, 4h and 4l) compared to standard.
Subject(s)
Anti-Infective Agents/chemical synthesis , Green Chemistry Technology , Pyrimidines/chemistry , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Aspergillus/drug effects , Bacillus subtilis/drug effects , Candida albicans/drug effects , Catalysis , Escherichia coli/drug effects , Microbial Sensitivity Tests , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Staphylococcus aureus/drug effects , Zirconium/chemistryABSTRACT
Combined nano zinc oxide and titanium dioxide [nano (ZnO-TiO(2))] has been reported first time for the synthesis of novel series of 4,5,6,7-tetrahydro-6-((5-substituted-1,3,4-oxadiazol-2-yl)methyl)thieno[2,3-c]pyridine. All the synthesized compounds (7a-7m) are novel and were screened for their antimicrobial activity against four different strains like Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis and antifungal activity was determined against two strains Candida albicans and Aspergillus niger. SAR for the newly synthesised derivatives has been developed by comparing their MIC values with ampicillin, ciprofloxacin and miconazole for antibacterial and antifungal activities, respectively. Among the synthesized compounds, 2,6 dichlorophenyl analogue (7f), 4 fluorophenyl analogue (7k) and 2,6 dichlorophenyl analogue (7l) shows promising antibacterial as well as antifungal activity whereas thiophene substituted compound (7j) shows promising antibacterial activity.
