Table 2 - uploaded by Kamal Shah
Content may be subject to copyright.
Source publication
Triazoles with different substituent groups are found to possess diverse applications in the field of medicine and industry. A series of 4-(substituted ethanoyl)amino-3-mercapto-5-(4-nitro)phenyl-1,2,4-triazoles (NU-1 to NU-15) were synthesized as novel antimicrobial agents starting from 4-nitrobenzoic acid. The chemical structures of these newly s...
Context in source publication
Similar publications
Triazoles and triazoles with different substituent groups are found to possess diverse application in the field of medicine and industry. A series of 4-(substituted) ethanoylamino-3-mercapto-5-(4-substituted) phenyl-1,2,4- triazoles were synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical stru...
Citations
... synthesized compounds were elucidated by IR, 1H NMR, 13C NMR, FAB+ -MS spectral data and elemental analysis. Their antimicrobial activities against Staphylococcus aureus (ATCC-25923), Pseudomonas aeruginosa (ATCC-27853), Escherichia coli (ATCC-8739), Bacillus substilis (ATCC-6633), Candida albicans (MTCC-227), Aspergillus niger (MTCC-3323) and Fusarium oxysporum (MTCC-2087) were investigated20 . 5d, h using thionyl chloride. ...
Antimicrobial resistance represents a serious threat to human health across the globe. The cost of bringing a new antibiotic from discovery to market is high and return on investment is low. Furthermore, the development of new antibiotics has slowed dramatically since the 1950s’ golden age of discovery. Medicinal compounds synthesis produce a variety of bioactive compounds that could be used to build a new way for the future discovery pipeline. While many studies have focused on specific aspects of synthetic compounds with antibacterial properties, a comprehensive review of the antibacterial potential of compounds has never before been attempted. This review aims to evaluate reports on some derivatives with significant antimicrobial activities.
... One such pharmaceutically important moiety, NH-triazole, serves as integral component of many biologically essential compounds such as anti-bacterial, anti-allergic, anti-cancer, and anti-malarial agents. [36][37][38][39] Due to their attractive physical and chemical properties such as hydrogen bonding ability, strong dipole moment, and chemical stability, NH-triazoles are of utmost importance in the current areas of research and development. 40,41 In this work, we have reported a cost-effective, effortless, and environmentally benign protocol for the synthesis of different phases of copper sulde NPs by varying the sulfur precursor concentration. ...
A series of copper sulfide (CS) nanoparticles (NPs) were synthesized just by varying the amount of the sulfur precursor and have been explored for the first time as a three-way heterogeneous catalyst in the photocatalytic oxidation of a number of aromatic alcohols, photocatalytic degradation and the reduction of water pollutants, and the facile synthesis of pharmaceutically important moiety 4-aryl-NH-1,2,3-triazoles. The green and novel protocol was successfully developed for the synthesis of covellite (CuS, Cu2+) and the covellite-villamaninite (CuS-CuS2) (copper in Cu2+, Cu1+) phases of copper sulfide, employing EDTA both as the chelating and capping agent via a simple precipitation method at room temperature using water as the solvent. A blue shift in the absorption spectra and band gap in the range of 2.02-2.07 eV prompted the investigation of the as-synthesized CS nanoparticles as the photocatalyst under visible light irradiation. In the absence of any oxidizing or reducing agent, covellite CuS nanoparticles showed the highest photocatalytic efficiency for the degradation of methylene blue (MB) and the reduction of carcinogenic and mutagenic Cr(vi) to non-toxic Cr(iii). Interestingly, the mixed phase of CS (CuS-CuS2), where Cu is present in both +1 and +2 oxidation states, was found to be the most efficient catalyst compared to CuS toward the visible light-mediated selective oxidation of various benzyl alcohols to their corresponding aldehydes. However, in the synthesis of substituted NH-1,2,3-triazoles, single-phase CS nanoparticles (i.e., CuS) provided the best catalytic result. This significant outcome certainly opens up the scope for realizing the present demand of low-cost multifunctional semiconductor nano-materials, which will have a huge impact on the economy and environment when they show more than two potential applications.
... antimicrobial, anticancer, anticonvulsant, anti-inflammatory, antioxidant) 1 and can undergo various types of reactions. 2 These reaction could involve the amino group, 3 the mercapto group, [4][5][6] or the endocyclic NH in the thione tautomer. 4,7 In addition, the proximity of the aforementioned reactive sites in 4-amino-1,2,4-triazole-3-thiones is inducive of ring closure reactions in which both amino and mercapto groups are involved. ...
4-Amino-5-(thiophen-2-ylmethyl)-2,4-dihydro-3 H -1,2,4-triazole-3-thione was synthesized and converted into the corresponding Schiff bases using several aromatic aldehydes. Reaction of this aminotriazolethione with phenacyl bromides lead to triazolothiadiazines, which were subsequently reduced with NaBH 4 to dihydrotriazolothiadiazines. The latter type of fused heterocycle has been also obtained directly by reacting one of the previously obtained Schiff base with phenacyl bromides. NMR analysis confirmed the structures of the synthesized compounds.
... Compound 191 was found similarly effective against Candida albicans as compared to reference drug Ketoconazole [136]. [137]. ...
Triazole is a valuable platform in medicinal chemistry, possessing assorted pharmacological properties, which could play a major role in the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still a lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has captured the attention of medicinal chemists to synthesize novel triazole derivatives. The authors amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of the triazole nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to provide insights to designing and synthesizing novel triazole derivatives with advanced and unexplored pharmacological implications.
... Once hydrotalcite based catalysts were modified to become ordered mesoporous hydrotalcite like compounds, the catalysts would contain not only acid and base sites, but also ordered mesoporous structure. This structure could highly enhance activity and selectivity of these kinds of catalysts in the decarboxylation of vegetable oil containing fatty acids, leading to produce a high-quality product of rich hydrocarbon composition [4][5][6]. Our paper published elsewhere [7] also proved this ability of preparation of the catalysts which could be assigned as mesohydrotalcite catalysts. ...
... Two of the most important characteristics of the mesohydrotalcite catalysts were their acidity and basicity, and pore width distribution [1,2,4]. Once getting these good properties including suitable acidity and high basicity, and relative medium-sized mesopores, the activity and selectivity of these catalysts in the decarboxylation could be greatly improved. ...
Vietnamese jatropha oil was converted to rich green hydrocarbon products under batch decarboxylation conditions using novel mesoporous Mg-Al-Co hydrotalcite based catalyst (mesohydrotalcite catalyst). The catalyst having pore width of 130Å was modified to other ones with pore width of 38Å by changing its preparation method from co-condensation-evaporation to hydrothermal treatment. The narrower pore width of the catalyst greatly contributed to its selectivity with free fatty acids in the decarboxylation process, which positively enhanced the hydrocarbon products. The decarboxylation parameters including temperature, time, catalyst loading and stirring speed were investigated in order to improve productivity of hydrocarbons within boiling range of diesel fraction. Results of the decarboxylation process showed a very high yield of ~70% of the diesel fraction strongly proving great activity and selectivity of the mesohydrotalcite catalyst. Some other techniques including WAXRD, TEM, BET, CO 2-TPD and NH 3-TPD were also applied to characterize some important properties of the mesohydrotalcite catalyst. They were all evidences for convincing the catalyst ability in the production of biofuel from renewable sources. Graphical Abstract Adsorption-desorption isotherm and pore distribution against pore area of MHT-HT catalyst Highlights Preparing mesoporous hydrotalcite based catalyst containing both homogeneous pore channels. Narrowing the catalyst pore width from 130Å to 38Å by changing preparation method from 1652 co-condensation evaporation to hydrothermal treatment. Establishing decarboxylation of jatropha oil in batch process obtaining green hydrocarbons. Yielding 70% of high purity green hydrocarbons in diesel fraction.
... This has led to increased pressure on the need for the newer 2 Bioinorganic Chemistry and Applications molecules which may have potentials to curb the spread of this problem. Particularly, 1,2,4-triazole and its derivatives have been reported to possess antioxidant activities [10][11][12][13]. The 1,2,4-triazole derivatives have also been known to possess many biological activities (antifungal, analgesic, antiviral, anti-inflammatory, antitumor, anti-HIV properties, etc.) [14,15]. ...
Density functional calculations were used to explore the complexation of 3-alkyl-4-phenylacetylamino-4,5-dihydro-1h-1,2,4-triazol-5-one (ADPHT) derivatives by first-row transition metal cations. Neutral ADPHT ligand and mono deprotonated ligands have been used. Geometry optimizations have been performed in gas-phase and solution-phase (water, benzene, and N,N-dimethylformamide (DMF)) with B3LYP/Mixed I (LanL2DZ for metal atom and 6-31+G(d,p) for C, N, O, and H atoms) and with B3LYP/Mixed II (6-31G(d) for metal atom and 6-31+G(d,p) for C, N, O, and H atoms) especially in the gas-phase. Single points have also been carried out at CCSD(T) level. The B3LYP/Mixed I method was used to calculate thermodynamic energies (energies, enthalpies, and Gibb energies) of the formation of the complexes analyzed. The B3LYP/Mixed I complexation energies in the gas phase are therefore compared to those obtained using B3LYP/Mixed II and CCSD(T) calculations. Our results pointed out that the deprotonation of the ligand increases the binding affinity independently of the metal cation used. The topological parameters yielded from Quantum Theory of Atom in Molecules (QTAIM) indicate that metal-ligand bonds are partly covalent. The significant reduction of the proton affinity (PA) observed when passing from ligands to complexes in gas-phase confirms the notable enhancement of antioxidant activities of neutral ligands.
... Specifically, 1,2,4-triazoles and their heterocyclic derivatives represent an interesting class of compounds possessing a wide spectrum of biological activities. A large number of 1,2,4,-triazole derivatives containing ring systems exhibit antibacterial (Gabriela et al., 2010;Upmanyu et al., 2011;Prasad et al., 2012;Taj et al., 2013;Kumar et al., 2014;Gupta et al., 2015), antifungal (Sangshetti et al., 2009;Zoumpoulakis et al., 2012;Barbuceanu et al., 2009Barbuceanu et al., , 2012Sahu et al., 2014;Gupta et al., 2015) antitubercular (Gill et al., 2008;Kumar et al., 2010;Cristophe et al., 2011;Godhani et al., 2015), analgesic (Amir et al., 2008;Tozkoparan et al., 2012;Khanage et al., 2013;Sarigol et al., 2015), anti-inflammatory (Pattan et al., 2012;Ayse et al., 2012;Ashour et al., 2013;Sarigol et al., 2015), anticancer (Romagnoli et al., 2010;Wang et al., 2011;Bai et al., 2012), anticonvulsant (Siddiqui et al., 2010;Dayanand et al., 2011;Botros et al., 2013;Plech et al., 2013;Kamboj et al., 2015), antiviral (Abdel-Aal et al., 2008;Jordao et al., 2009;El-Etrawy et al., 2010), antimalarial (Mishra et al., 2008;Gujjar et al., 2009) central nervous system (Kamboj et al., 2015) and other activities (Puthiyapurayil et al., 2012;Iqbal et al., 2012). ...
As a part of our ongoing studies in developing new derivatives as antimicrobial agents we describe the synthesis of novel substituted 5- benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6(5H)ones.The twenty five newly synthesized compounds were tested for their antimicrobial and antifungal activity. All compounds have shown antibacterial properties with compounds 1-9 showing the lowest activity, followed by compounds 10-14 while compounds 15-25 the highest antibacterial activity. Specific compounds appeared to be more active than ampicillin in most studied strains and in some cases more active than streptomycin. Antifungal activity in most cases also was better than that of reference drugs ketoconazole and bifonazole. Elucidating the relation of molecular properties to antimicrobial activity as well as generation of pharmacophor model for antifungal activity of two fungal species A. fumigates and C.albicans were performed.
... The 1,3,4-oxadiazole compounds often display antifungal, herbicidal [10], and insecticidal [11,12] effects. 1,2,4-Triazoles have attracted particular attention due to the wide range of their biological properties such as antibacterial and antifungal [13][14][15][16], anticancerantitumour [17], antidepressant [18]. Strains of the Rhizobium species (formerly Agrobacterium, which was reclassified based on 16S rDNA analyses) are aerobic, motile, oxidase-positive, and non-spore-forming gramnegative bacilli. ...
... The pathway of synthesis of the new 1,4disubstituted pyrrolidinones is shown in Scheme 1 (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13) and Scheme 2 (14)(15)(16)(17)(18)(19)(20)(21)(22)(23). ...
4-Substituted 1-(4-methoxyphenyl)pyrrolidin-2-ones containing azole, diazole, oxadiazole, thiadiazole, and triazole fragments have been synthesized, and the characterization of the obtained products is presented. The study compounds have been analyzed for antioxidant and antibacterial activities. Two types of hetero systems – 5-thioxo-4,5-dihydro-1,3,4-oxadiazole and [1,2,4]triazolo[3,4- b ][1,3,4]thiadiazine – showed a moderate activity against Rhizobium radiobacter , Xanthomonas campestris , and Escherichia coli microorganisms. Some compounds were tested for their antioxidant activity. DOI: http://dx.doi.org/10.5755/j01.ct.65.1.8881
... In the last few decades, the chemistry of 1,2,4-traiazole compounds and their fused heterocyclic derivatives have received considerable attention owing of their synthetic and effective biological importance, for example, a large of 1,2,4-traiazole containing ring systems have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, CNS stimulation sedatives, antianxiety and antimicrobial agents [1,2]. The mercapto and thione-substituted 1,2,4-traizole ring systems have been reported for a large number of their derivatives [1]. ...
... Propenyl-1,2,4-Triazole(L) A. Synthesis of methyl ester of 4nitrobenzoic acid (I) [2,5] To 4-nitrobenzoic acid (0.1 mol) in (100ml) of methanol in a round bottomed flask conc. sulfuric acid (5.7 ml) was added. ...
In the present work, we synthesized a series of metal complexes of Co(II), Ni(II), Cu(II), Zn(II) and Au(III) from newly synthesized ligand 5-(4-Nitro Phenyl)-4-Amino-3-Mercapto Propenyl-1,2,4-Triazole (L) in alcoholic medium. These compounds were characterized by several techniques using FT-IR, UV-Visible spectrophotometer, thermal gravimetric TG analyses, magnetic susceptibility, Flame Atomic Absorption technique, elemental analysis and conductivity measurements. From the spectral studies, an octahedral monomer structure was proposed for all complexes except Cu(II) complex has dinuclear structure. The nature of the complexes formed in ethanolic solution has been studied following the molar ratio method and the result recorded 1:1 molar ratio for all complexes. Semi-empirical methods (ZINDO/1, ZINDO/S and PM3) were carried out to evaluate the heat of formation ∆H˚f, binding energy ∆Eb, and dipole moment for all complexes expect Au(III) complex that used AMBER method, also the vibration frequencies and electronic transitions were calculated for prepared ligand to make comparison with experimental results. Electrostatic potential, HOMO and LUMO energies for ligand were calculated to determine the reactive sites of new ligand.
... In the last few decades, the chemistry of 1,2,4-traiazole compounds and their fused heterocyclic derivatives have received considerable attention owing of their synthetic and effective biological importance, for example, a large of 1,2,4-traiazole containing ring systems have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, CNS stimulation sedatives, antianxiety and antimicrobial agents [1,2]. The mercapto and thione-substituted 1,2,4-traizole ring systems have been reported for a large number of their derivatives [1]. ...
... Propenyl-1,2,4-Triazole(L) A. Synthesis of methyl ester of 4nitrobenzoic acid (I) [2,5] To 4-nitrobenzoic acid (0.1 mol) in (100ml) of methanol in a round bottomed flask conc. sulfuric acid (5.7 ml) was added. ...
In the present work, we synthesized a series of metal complexes of Co(II), Ni(II), Cu(II), Zn(II) and Au(III) from newly synthesized ligand 5-(4-Nitro Phenyl)-4-Amino-3-Mercapto Propenyl-1,2,4-Triazole (L) in alcoholic medium. These compounds were characterized by several techniques using FT-IR, UV-Visible spectrophotometer, thermal gravimetric TG analyses, magnetic susceptibility, Flame Atomic Absorption technique, elemental analysis and conductivity measurements. From the spectral studies, an octahedral monomer structure was proposed for all complexes except Cu(II) complex has dinuclear structure. The nature of the complexes formed in ethanolic solution has been studied following the molar ratio method and the result recorded 1:1 molar ratio for all complexes. Semi-empirical methods (ZINDO/1, ZINDO/S and PM3) were carried out to evaluate the heat of formation ∆H˚f, binding energy ∆Eb, and dipole moment for all complexes expect Au(III) complex that used AMBER method, also the vibration frequencies and electronic transitions were calculated for prepared ligand to make comparison with experimental results. Electrostatic potential, HOMO and LUMO energies for ligand were calculated to determine the reactive sites of new ligand.
