Synthesis and anti-microbial screening of some substituted 1, 2, 3-triazole derivatives

• Published in: Journal of pharmaceutical sciences and research 2019-08, Vol.11 (8), p.2797-2801
• Main Authors: Ibraheem, Tareq K, Al-azawi, Suad Turky Ali, Mohammed, A
• Format: Article
• Language: English
• Subjects: Antimicrobial agents; Azide; Bacteria; Chemistry; Cytotoxicity; Ethanol; Financial disclosure; Gram-positive bacteria; Potassium
• ISSN: 0975-1459

Generally, 1,2,3,4-tetrazole and derivatives possess broad spectrum of biologicalactivates[1].1,2,3-Triazoles are Nheterocyclic compounds not present in natural products, which display different biological properties such as potential antitumor [1] anti-fungal[2] anti-hypertensive [3] anti-bacterial activity against Gram-positive bacteria in addition to Gram-negative bacteria[4], anti-inflammatory [5] cytotoxic activity against human cancer cell lines[6] and anti-viral activity against many viruses [7]. such as antiHIV) [8], anti-epileptic activities [9], anti-diabetic [10] and cholinesterase inhibitors [11]. [...]members of this class in as dyes, corrosion inhibitars photostabilizers and photographic materials. [...]to the best of our knowledgoe knowledge there are no report of the use of this five-membered ring in liquid crystals except for few examples containing the regioisomeric [1,2,4]-triazole [12]. [...]the aim of current study was the synthesis of some new 1,2,3-triazol derivatives and screening them for potential antimicrobial activities. Yield dark brown (85 %), m.p. 156-158°C Synthesis of N,N-([1,1-biphenyl-4,4-diyl)bis(2azidoacetamide)][II] An amount of compound [I] (0.001mol) was dissolved in (5mL) DMF added to the mixture sodium azide (0.002mol) then added ammonium chloride (0.002mol) and refluxed for (5h) and cooled then added to ice water filtered and recrystallized from ethanol Synthesis of 4-(prop-2-yn-1-yloxy)benzaldehyde [III] To a solution of 4-hydroxybenzaldehyde (0.0008mol) and potassium carbonate (0.0007mol) in (5mL) DMF was slowly added propargylbromide (0.0008mol) was added to the solution in bath ice if an ice water mixture was stirred for (24h) and filtered Synthesis of N,N'-(1,4-phenylene)bis(2-(4-(4(formylphenoxy)-1H-1,2,3-triazol-1-yl)acetamide [V] An amount of compound [III] (0.01 mol) was dissolved in ethanol (50 mL). The solution stirred for (3h) then then mixture cooled and filtered Antimicrobial Screening The antibacterial activity of the synthesized compounds was tested against four Gram-positive bacteria (, Staphylococcus epidermidis, Staphylococcus aureus Micrococcus luteus and Bacillus cereus) and two Gramnegative bacteria (Pseudomonas aeruginosa and Escherichia coli) using nutrient agar medium.