Synthesis of azatricyclodiones & octahydro-benzo[f]isoindoles and their antimicrobial evaluation

A series of azatricyclodiones and octahydro-benzo[f]isoindoles have been synthesized by (4+2) Diels-Alder cycloaddition of maleimides with furfuryl amine. Reaction of azatricyclodiones with isocyanates led to the respective ureides. All of the compounds were screened against a number of bacteria and fungi. One of the compounds (2) displayed moderate antitubercular activity while two compounds (2) and (4) inhibited the fungal growth at 25 μg/mL.     

Enantiomeric impurities in chiral catalysts,auxiliaries, and synthons used in enantioselective syntheses. Part 5

The enantiomeric excess of chiral starting materials is one of the important factors determining the enantiopurity of products in asymmetric synthesis. Fifty‐one commercially available chiral reagents used as building blocks, catalysts, and auxiliaries in various enantioselective syntheses were assayed for their enantiomeric purity. The test results were classified within five impurities level (ie, <0.01%, 0.01%‐0.1%, 0.1%‐1%, 1%‐10%, >10%). Previously from 1998 to 2013, several reports have been published on the enantiomeric composition of more than 300 chiral reagents. This series of papers is necessitated by the fact that new reagents are forthcoming and that the enantiomeric purity of the same reagent can vary from batch to batch and/or from supplier to supplier. This report presents chiral liquid chromatography (LC) and gas chromatography (GC) methods to separate enantiomers of chiral compounds and evaluate their enantiomeric purities. The accurate and efficient LC analysis was done using newly introduced superficially porous particle (SPP 2.7 μm) based chiral stationary phases (TeicoShell, VancoShell, LarihcShell‐P, and NicoShell).     

Comparative liver transcriptome analysis of duck reveals potential genes associated with egg production

Molecular Biology Reports - Molecular studies on egg production in ducks were mostly focused on brain and ovaries as they are directly involved in egg production. Liver plays a vital role in...     

Synthesis, molecular modeling and bio-evaluation of cycloalkyl fused 2-aminopyrimidines as antitubercular and antidiabetic agents

An economical and efficient one step synthesis of a series of 8-(arylidene)-4-(aryl)-5,6,7,8-tetrahydro-quinazolin-2-ylamines and 9-(arylidene)-4-(aryl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-2-ylamines by the reaction of bis-benzylidene cycloalkanones and guanidine hydrochloride in presence of NaH has been developed. All the synthesized compounds were evaluated against Mycobacterium tuberculosis H₃₇Rv strain and the α-glucosidase and glycogen phosphorylase enzymes. Few of the compounds have shown interesting in vitro activity with MIC up to 3.12 μg/mL against M. tuberculosis and very good inhibition of α-glucosidase and glycogen phosphorylase enzymes. The most potent non toxic compound 40 exhibited about 58% ex vivo activity at MIC of 3.12 μg/mL. The present study opens a new gate to synthesize antitubercular agents for diabetic TB patients. In silico docking studies indicate that mycobacterial dihydrofolate reductase is the possible target of these compounds.     

Transformation and stabilization of pyrogenic organic matter in a temperate forest field experiment

Pyrogenic organic matter (PyOM) decomposes on centennial timescale in soils, but the processes regulating its decay are poorly understood. We conducted one of the first studies of PyOM and wood decomposition in a temperate forest using isotopically labeled organic substrate, and quantified microbial incorporation and physico‐chemical transformations of PyOM in situ. Stable‐isotope (¹³C and ¹⁵N) enriched PyOM and its precursor wood were added to the soil at 2 cm depth at ambient (N0) and increased (N+) levels of nitrogen fertilization. The carbon (C) and nitrogen (N) of added PyOM or wood were tracked through soil to 15 cm depth, in physically separated soil density fractions and in benzene polycarboxylic acids (BPCA) molecular markers. After 10 months in situ, more PyOM‐derived C (>99% of initial ¹³C‐PyOM) and N (90% of initial ¹⁵N‐PyOM) was recovered than wood derived C (48% of ¹³C‐wood) and N (89% under N0 and 48% under N+). PyOM‐C and wood‐C migrated at the rate of 126 mm yr^?1 with 3–4% of PyOM‐C and 4–8% of wood‐C recovered below the application depth. Most PyOM C was recovered in the free light fraction (fLF) (74%), with 20% in aggregate‐occluded and 6% in mineral associated fractions – fractions that typically have much slower turnover times. In contrast, wood C was recovered mainly in occluded (33%) or dense fraction (27%). PyOM addition induced loss of native C from soil (priming effect), particularly in fLF (13%). The total BPCA‐C content did not change but after 10 months the degree of aromatic condensation of PyOM decreased, as determined by relative contribution of benzene hexa‐carboxylic acid (B6CA) to the total BPCA C. Soil microbial biomass assimilated 6–10% of C from the wood, while PyOM contributions was negligible (0.14–0.18%). The addition of N had no effect on the dynamics of PyOM while limited effect on wood.     

Regioselective [3+2] cycloaddition of chalcones with a sugar azide: easy access to 1-(5-deoxy-d-xylofuranos-5-yl)-4,5-disubstituted-1H-1,2,3-triazoles

[3+2] Cycloaddition of 5-azido-5-deoxy-1,2-O-isopropylidene-α-d-xylofuranose with 1,3-diphenyl-prop-3-enones, followed by oxidation of the intermediate triazolines in a tandem manner, led to the regioselective formation of 4-benzoyl-1-(5-deoxy-1,2-O-isopropylidene-α-d-xylofuranos-5-yl)-5-phenyl-1H-1,2,3-triazoles in moderate to good yields.     

Salinity-Induced Attenuation in Secondary Metabolites Profile and Herbicidal Potential of Brassica nigra L. on Anagallis arvensis L.

Studies on plant defense mechanisms in stressful conditions predict that plant cope up with increasing stress for survival. Under environmental stress plants interact with problems like competition and survival under resource constraints or utilization of these resources in production of secondary compounds. In this experiment, we examined the costs of defense by evaluating variation in production of secondary compounds of Brassica nigra grown in the saline (B1?=?100 mM NaCl and B2?=?150 mM NaCl) and control (C?=?0 mM) soils and impact of its extracts on weed Anagallis arvensis L. The main allelopathic compounds in Brassica were determined using gas chromatography–mass spectroscopy (GC–MS). The results indicated that A. arvensis was adversely affected by the aqueous extracts of B. nigra. These observations might be related to extracts induced oxidative stress indicated by superoxide (O₂^?) production through nitroblue tetrazolium, cell integrity by Evans blue staining, malondialdehyde estimation by Schiff reagent, lipid peroxidation, lignin deposition, and antioxidant enzyme activities assay. We observed that soil salinity reduced the phytotoxicity of aqueous extract and decreased its potential. The presence of different bioactive compounds improved the natural herbicidal properties of B. nigra and it can be used in various medicinal and agricultural practices.

     

Preparation of poly(l-lactide) blends and biodegradation by Lentzea waywayandensis

As a biodegradable polyester, polylactide (PLA) has applications as a packaging material, in biomedical fields and tissue engineering. With the dual aim of improving its properties and biodegradability, PLA was blended with other polymers such as gum arabic, thermoplastic starch, microcrystalline cellulose, polyethylene glycol and polyhydroxy butyrate in 1:1 (w/w) by melt-blending technique. The thermal properties of the blends were compared with that of unblended PLA by thermo-gravimetric analysis. Biodegradation using Lentzea waywayandensis was in the order of PLA–gum arabic?>?PLA–thermoplastic starch?>?PLA(virgin)?>?PLA–microcrystalline cellulose?>?PLA–polyethylene glycol?>?PLA–polyhydroxy butyrate. Weight loss of 99?% (w/w) was noted within 4?days for PLA–thermoplastic starch and PLA-gum arabic blends.