Abstract:The series of novel Mannich bases were synthesized and evaluated for their in vitro antibacterial activity against Gram‐positive and Gram‐negative bacterial strains. The results showed that all compounds were less active than the drugs used as reference, but some of them had moderate potency against Staphylococcus epidermidis ATCC 12228 and Bacillus subtilis ATCC 6633. The presence of a phenyl ring in the position 4 of piperazine seems to be necessary for antibacterial activity in this class of compounds.
“…Several studies show that a common compound that is carried out in the numerous fields of biology and medicine is a five-membered heterocyclic compound, and its nitrogen-containing structure with high activities against several pathogens like antifungal, antibacterial, antiviral, and others could be found in 1,2,4-triazoles Mannich bases 20 .…”
Biological evaluation of a 1,2,4-triazole mannich base that has been synthesized for interesting behavior in medicinal chemistry, so it’s interesting to synthesize triazole derivatives and investigate their biological properties to evaluate their capacity in medicine. The aim of this study evaluate the antimicrobial, anticancer, and antioxidant activities of a 1,2,4-triazole Mannich base derivative and its power in the treatment of diseases. For antimicrobial activity four bacterial strains and one fungal strain based on the agar disc diffusion. While used two cancer cell lines for anticancer activity which are known as Hep-G2 and MCF-7; the antioxidant activity of the compound used three different radical species include OH•, ABTS•+, and DPPH•, and also determine the antioxidant activity of the compound after extracting vitamins A, C, E, and MDA in the S. cerevisiae yeast cell by HPLC. The results of this study show the positive role of a derivative 1,2,4-triazole mannich base as antimicrobial and antiradical assays, particularly when treated with C. albicans and OH• radical that significantly reduced growth of the fungal and the radical compared to others. In addition, it didn’t exhibit any cytotoxicity to reduce both cancer cell lines. In conclusion, the compound's ability is different from one assay to another, increasing its concentration efficiency affects the radical scavenging, and inhibits microorganism growth.
“…Several studies show that a common compound that is carried out in the numerous fields of biology and medicine is a five-membered heterocyclic compound, and its nitrogen-containing structure with high activities against several pathogens like antifungal, antibacterial, antiviral, and others could be found in 1,2,4-triazoles Mannich bases 20 .…”
Biological evaluation of a 1,2,4-triazole mannich base that has been synthesized for interesting behavior in medicinal chemistry, so it’s interesting to synthesize triazole derivatives and investigate their biological properties to evaluate their capacity in medicine. The aim of this study evaluate the antimicrobial, anticancer, and antioxidant activities of a 1,2,4-triazole Mannich base derivative and its power in the treatment of diseases. For antimicrobial activity four bacterial strains and one fungal strain based on the agar disc diffusion. While used two cancer cell lines for anticancer activity which are known as Hep-G2 and MCF-7; the antioxidant activity of the compound used three different radical species include OH•, ABTS•+, and DPPH•, and also determine the antioxidant activity of the compound after extracting vitamins A, C, E, and MDA in the S. cerevisiae yeast cell by HPLC. The results of this study show the positive role of a derivative 1,2,4-triazole mannich base as antimicrobial and antiradical assays, particularly when treated with C. albicans and OH• radical that significantly reduced growth of the fungal and the radical compared to others. In addition, it didn’t exhibit any cytotoxicity to reduce both cancer cell lines. In conclusion, the compound's ability is different from one assay to another, increasing its concentration efficiency affects the radical scavenging, and inhibits microorganism growth.
“…Liu et al reported a novel substituted 3,5-diamine-1,2,4-triazole from isothiocynate and mono-substituted hydrazines and sodium hydrogen cyanamide (Scheme 6 ) [ 27 ]. Scheme 6 Novel substituted 3,5-diamine-1,2,4-triazole …”
Background
A large number of studies have recently reported that, because of their significant biological and pharmacological properties, heterocyclic compounds and their derivatives have attracted a strong interest in medicinal chemistry. The triazole nucleus is one of the most important heterocycles which has a feature of natural products as well as medicinal agents. Heterocyclic nitrogen is abundantly present in most medicinal compounds. The derivatization of triazole ring is based on the phenomenon of bio-isosteres in which substituted the oxygen atom of oxadiazole nucleus with nitrogen triazole analogue.
Main text
This review focuses on recent synthetic procedure of triazole moiety, which comprises of various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc..
Conclusion
This review highlights the current status of triazole compounds as different multi-target pharmacological activities. From the literature survey, triazole is the most widely used compound in different potential activities.
“…[48] Extensive literature reports have highlighted the potency of Mannich base-linked 1,2,4-triazole derivatives as antibacterial, [49][50][51] antifungal, [52,53] antitubercular, [54] anti-cancer agents. [55,56] As existing drugs on the market often face challenges such as drug resistance, undesirable toxic side effects, and incompatibility with other drugs, there is an urgent need for the synthesis of novel biologically active compounds. These new candidates should possess safety profiles, exhibit strong biological activity, have rapid action, and be non-toxic, thereby meeting the current medical demands.…”
Section: Introductionmentioning
confidence: 99%
“…Additionally, by selecting the appropriate amine reagent, the Mannich reaction can also contribute to enhancing the lipophilic properties of a drug [48] . Extensive literature reports have highlighted the potency of Mannich base‐linked 1,2,4‐triazole derivatives as antibacterial, [49–51] antifungal, [52,53] antitubercular, [54] anti‐cancer agents [55,56] . As existing drugs on the market often face challenges such as drug resistance, undesirable toxic side effects, and incompatibility with other drugs, there is an urgent need for the synthesis of novel biologically active compounds.…”
Over the past twenty years (1998–2023), extensive research has focused on the synthesis and biological activity of Mannich base derivatives of flavonoids (FMBD), which have demonstrated exceptional properties towards organic and bioorganic molecules. Several research groups have reported the pharmacological potential of these flavonoid derivatives, including antioxidant and antiviral activities, as well as their ability to inhibit AChE and exhibit anticancer properties. Moreover, the unique characteristic of forming stable complexes with biomolecules positions flavonoid derivatives as valuable assets in the realm of biology and drug discovery. In this extensive review, we′ve meticulously analyzed over seventy six distinct research studies on this subject. Our aim is to provide a succinct overview of the wide‐ranging applications of flavonoid derivatives coupled with amines. Furthermore, we explore the promising horizons and potential innovations in this field. It's essential to highlight that these derivatives display no discernible signs of toxicity or eliciting immune responses, making them even more attractive for biopharmaceutical applications. Undoubtedly, the utilization of flavonoid derivatives combined with amines as crucial biopharmaceutical agents is poised for significant expansion in the forthcoming years.
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