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Synthesis, characterisation, biological and theoretical studies of novel pyridine derivatives
No full textDiversely functionalised pyrazolone analogues have been reported to display a wide range of biological activities. In this paper, we report the synthesis of a series of novel analogues based on piperidine fused pyrazolone core and explore its potential as novel antibacterial agents. The synthesised compounds were analysed using spectroscopic techniques such as H-1 NMR, LC-MS, and FT-IR. The major highlight involves the cyclisation reaction of tert-butyl-4-methyl 3-oxopiperidine-1,4-dicarboxylate with the hydrazine component to access the privileged piperdine fused pyrazolone scaffold. This scaffold was further treated with HCl to remove the amine protecting group and subsequently reacted with acid chlorides to deliver the final products in excellent yields. Density functional theory (DFT) calculations were performed to determine the various molecular properties of the synthesised compounds. Based on the reactive sites explored by the molecular electrostatic potential maps, the compounds were screened against two gram positive bacterial strains namely S. aureus, and M. luteus, and a gram negative bacterial strain namely E.coli
Extent of encounter with an embedded food influences how it is processed by an urbanizing macaque species
No full textRapid urbanization exerts novel adaptive pressures on animals at the interface of natural and altered environments. Urban animals often rely on synthetic foods that require skilled extraction and flexible processing. We studied how synthetic treatment of an embedded food, peanut, determined its extraction and processing across groups of bonnet macaques (Macaca radiata) differing in encounter and familiarity with peanut. The possibility of the application of processing methods to similar foods was also tested. We found encounter- and form (native/shelled/skinned)-specific familiarity to peanuts, state (raw/boiled/roasted)-specific distinction in skinning, and encounterand state-specific differences in methods of skinning. The group with the highest encounter with peanuts exhibited novel and manipulatively complex processing. Novel processing was also extended to peas and chickpeas. Our study establishes a strong relationship between familiarity with the condition of food and the processing methods used and further, demonstrates the probable role of categorization in extension of novel methods
Composition and Codon Usage Pattern Results in Divergence of the Zinc Binuclear Cluster (Zn(II)(2)Cys(6)) Sequences among Ascomycetes Plant Pathogenic Fungi
Get PDFZinc binuclear cluster proteins (ZBC; Zn(II)(2)Cys(6)) are unique to the fungi kingdom and associated with a series of functions, viz., the utilization of macromolecules, stress tolerance, and most importantly, host-pathogen interactions by imparting virulence to the pathogen. Codon usage bias (CUB) is the phenomenon of using synonymous codons in a non-uniform fashion during the translation event, which has arisen because of interactions among evolutionary forces. The Zn(II)(2)Cys(6) coding sequences from nine Ascomycetes plant pathogenic species and model system yeast were analysed for compositional and codon usage bias patterns. The clustering analysis diverged the Ascomycetes fungi into two clusters. The nucleotide compositional and relative synonymous codon usage (RSCU) analysis indicated GC biasness toward Ascomycetes fungi compared with the model system S. cerevisiae, which tends to be AT-rich. Further, plant pathogenic Ascomycetes fungi belonging to cluster-2 showed a higher number of GC-rich high-frequency codons than cluster-1 and was exclusively AT-rich in S. cerevisiae. The current investigation also showed the mutual effect of the two evolutionary forces, viz. natural selection and compositional constraints, on the CUB of Zn(II)(2)Cys(6) genes. The perseverance of GC-rich codons of Zn(II)(2)Cys(6) in Ascomycetes could facilitate the invasion process. The findings of the current investigation show the role of CUB and nucleotide composition in the evolutionary divergence of Ascomycetes plant pathogens and paves the way to target specific codons and sequences to modulate host-pathogen interactions through genome editing and functional genomics tools
Synthesis, spectral characterization, electrochemical studies of pesticide and biological evaluation of transition metal complexes of azo dye derived from substituted phenyl pyrazole
No full textDiazotization of p-nitro aniline followed by coupling with 3-methyl-1-phenyl pyrazole to procure biologically active azo-dye ligand 3-methyl-4-(E)-(4-nitrophenyl) diazenyl]-1-phenyl-1H-pyrazol-5-ol (NDP) and also the array of transition metal complexes of aforementioned azo-dye ligand has been carried off along with the use of metal complex to detect pesticides electrochemically. Structural verification of synthesized compounds was carried out via 1H and 13C NMR along with the percentage of C,H,N, molecular weights, Infra-red, UV-Visible spectra and molar conductance of ligand and its complexes was observed. Also TGA, P-XRD and CV measure-ments were noted. An antimicrobial potency was evaluated by well diffusion method and antioxidant efficacy by DPPH technique. Molecular docking studies was used and MTT tests were conducted on MCF-7 and Hela cell lines to investigate anticancer potency. Upon utilizing physical and spectroscopic techniques to characterize the novel azo-dye ligand and its transition coordinated compounds justified the bi-dentate nature of ligand. Further CV measurements showed that the synthesized Co(II) complex exhibited excellent electrocatalysis properties for the electrochemical sensing of pesticide(Ammonium salt of glyphosate 71% SG) with wider linear range of 0.1 mu M-0.8 mu M and detection limit 0.033 mu M. Mn(II) and Co(II) complex displayed good anti-microbial activity along with cytotoxic potency whereas Co(II) and Cu(II) compounds indicated good anti-oxidant activity. Thus, NDP and its complexes being structurally supported via spectral data and CV studies affirms that Co(II) is strongly useful in detecting pesticide. And lastly it was found that all metal complexes have admirable bioefficacy when compared to ligand
Synthesis and crystal structure of ebastinium hydrogen fumarate
No full textThe structure of ebastinium hydrogen fumarate {systematic name: 1-[4-(4-tert-butylphenyl)-4-oxobutyl]-4-(diphenylmethoxy)piperidin-1-ium (E)-3-carboxy-1-hydroxyprop-2-en-1-olate}, C32H40NO2+·C4H3O4−, a 1:1 salt formed in the reaction between ebastine and fumaric acid is presented. All examined crystals were found to be twinned by pseudo-merohedry. The structure is extensively disordered, with over half (20 out of 35) its non-hydrogen atoms modelled as lying over two sets of sites. In the crystal, cation–anion pairs are linked by a strong N—H⋯O hydrogen bond [N⋯O = 2.697 (11) Å]. These units interact via weaker C—H⋯O and C—H⋯π contacts to form layers lying parallel to the bc plane. The hydrogen fumarate anions are linked by a very short O—H⋯O hydrogen bond [O⋯O = 2.5402 (17) Å], augmented by weak C—H⋯O contacts into pairs of R22(6) ring motifs to form chains that extend parallel to the b-axis direction. Comparisons to similar crystal structures are presented
Isopropyl 4-aminobenzoate
No full textThe title compound, C10H13NO2, crystallizes with two molecules (A and B) in the asymmetric unit. For A, the dihedral angle between the plane of the phenyl ring and the i-propyl substituent is 65.4 (3)° while for B this angle is 67.8 (3)°. In the crystal, the molecules are linked by N—H⋯O and N—H⋯N hydrogen bonds to generate double chains propagating in the [100] direction
Synthesis of Co(II), Ni(II) and Zn(II) Metal Complexes Derived from a Hydrazone Schiff Base: Electrochemical Behavior and Comprehensive Biological Studies
No full textAbstract The present study deals with the synthesis of (E)-N’-(2,5-dimethoxybenzylidene)-2-hydroxybenzohydrazide, a hydrazone Schiff base ligand (HY) and its metal complexes Co(HY)2, Ni(HY)2, Zn(HY)2.2H2O. The structure of the synthesized ligand was characterized by physico-chemical analytical and spectral techniques. The electrochemical behavior of HY and its complexes were investigated by cyclic voltammetry. Infrared spectral data suggested that HY acts as a tridentate ligand with ONO as the donor atoms. Molar conductivity data showed that all the complexes were non-electrolytic in nature and octahedral geometry of the complexes was confirmed by UV-visible spectrum. TGA studies of the complexes gave a clear idea about the coordination sphere and the process of degradation. Further, HY and its complexes were screened for their in vitro antioxidant, antibacterial and anticancer activities. Among the synthesized complexes, Ni(II) and Zn(II) metal complexes showed prominent antioxidant activity investigated through their scavenging effect on DPPH radical, anticancer activity against MCF-7 and HeLa cancer cells. The molecular docking into P53 cancer mutant protein (PDB ID: 5AB9) was done for the optimization of the investigated compounds as potential cancer cell inhibitors. The observed data infer that all the complexes show promising antimicrobial activity against all of the tested bacterial and fungal species compared to the parent ligand HY
Antifungal Potential of Azotobacter salinestris Strain Azt 31 against Phytopathogenic Fusarium spp. Associated with Cereals
Get PDFAntifungal efficacy of Azotobacter salinestris against trichothecene-producing Fusarium spp. was investigated in maize, sorghum, and wheat. The three cereals were subjected to four treatments as control (T1), Fusarium alone (T2), combination of Fusarium and A. salinestris treatment (T3), and only A. salinestris (T4). All the treatments were evaluated for total mass of seedlings, root and shoot length, seed germination, and vigor index (VI), and extent of rhizoplane colonization by A. salinestris was investigated. Further, greenhouse studies were conducted to learn the efficacy of A. salinestris in vivo conditions. Antifungal efficacy was tested by the dual-culture method which resulted in significant reduction in Fusarium growth. Infection by Fusarium was reduced up to 50 in treated cereals such as maize, sorghum, and wheat, and there was also significant increase in seedling mass in the three hosts. Maize showed the highest VI (1859.715), followed by sorghum (1470.84), and wheat (2804.123) with A. salinestris treatment. In addition, seed germination was enhanced to 76 in maize, 69 in sorghum, and 68 in wheat, respectively. Efficacy of rhizoplane colonization showed successful isolation of A. salinestris with high CFU rate, and furthermore, significant colonization inhibition by Fusarium spp. was observed. In the greenhouse conditions, on the 45th day of the experimental set-up, the highest shoot length/root length recorded in maize was 155.70/70.0 cm, in sorghum 165.90/48.0 cm, and in wheat 77.85/56.0 cm, and the maximum root mass recorded was 17.53 g in maize, 4.52 g in sorghum, and 1.90 g in wheat. Our present study showed that seed treatment by A. salinestris, may be used as an alternate biocontrol method against Fusarium infection in maize, sorghum, and wheat
In vitro micropropagation from leaf and stem derived callus of solanum diphyllum -a potent medicinal herb
Get PDFSynthesis of Co(II), Ni(II) and Zn(II) Metal Complexes Derived from a Hydrazone Schiff Base: Electrochemical Behavior and Comprehensive Biological Studies
No full textThe present study deals with the synthesis of (E)-N'-(2,5-dimethoxybenzylidene)-2-hydroxybenzohydrazide, a hydrazone Schiff base ligand (HY) and its metal complexes Co(HY)(2), Ni(HY)(2), Zn(HY)(2)].2H(2)O. The structure of the synthesized ligand was characterized by physico-chemical analytical and spectral techniques. The electrochemical behavior of HY and its complexes were investigated by cyclic voltammetry. Infrared spectral data suggested that HY acts as a tridentate ligand with ONO as the donor atoms. Molar conductivity data showed that all the complexes were non-electrolytic in nature and octahedral geometry of the complexes was confirmed by UV-visible spectrum. TGA studies of the complexes gave a clear idea about the coordination sphere and the process of degradation. Further, HY and its complexes were screened for their in vitro antioxidant, antibacterial and anticancer activities. Among the synthesized complexes, Ni(II) and Zn(II) metal complexes showed prominent antioxidant activity investigated through their scavenging effect on DPPH radical, anticancer activity against MCF-7 and HeLa cancer cells. The molecular docking into P53 cancer mutant protein (PDB ID: 5AB9) was done for the optimization of the investigated compounds as potential cancer cell inhibitors. The observed data infer that all the complexes show promising antimicrobial activity against all of the tested bacterial and fungal species compared to the parent ligand HY