The present study describes palladium-catalyzed one pot Suzuki cross-coupling reaction to synthesize a series of novel pyridine derivatives 2a–2i, 4a–4i. In brief, Suzuki cross-coupling reaction of 5-bromo-2-methylpyridin-3-amine (1) directly or via N-[5-bromo-2-methylpyridine-3-yl]acetamide (3) with several arylboronic acids produced these novel pyridine derivatives in moderate to good yield. Density functional theory (DFT) studies were carried out for the pyridine derivatives 2a–2i and 4a–4i by using B3LYP/6-31G(d,p) basis with the help of GAUSSIAN 09 suite programme. The frontier molecular orbitals analysis, reactivity indices, molecular electrostatic potential and dipole measurements with the help of DFT methods, described the possible reaction pathways and potential candidates as chiral dopants for liquid crystals. The anti-thrombolytic, biofilm inhibition and haemolytic activities of pyridine derivatives were also investigated. In particular, the compound 4b exhibited the highest percentage lysis value (41.32%) against clot formation in human blood among all newly synthesized compounds. In addition, the compound 4f was found to be the most potent against Escherichia coli with an inhibition value of 91.95%. The rest of the pyridine derivatives displayed moderate biological activities.
Four new 5 alpha-pregnane-type steroidal alkaloids, hookerianamides L(1), M(2), N(3), and O(4), and a known N-formylchonemorphine (5) have been isolated by acid-base extraction of the dichloromethane extract of Sarcococca hookeriana. The structures of all compounds were determined with spectroscopic techniques and by comparison with literature data. All compounds displayed antileishmanial and antibacterial properties. Compounds 1, 4, and 5 were found to be more potent than standard pentamidine (IC (50) = 9.59 microg/mL) with respect to leishmanicidal activity. The minimum inhibitory concentration of most of the compounds against Bacillus subtilis, Streptococcus minor, and Streptococcus ferus was lower than that of the standard ampicillin.
Dietary fiber has gained greater attention owing to their positive and potential health perspectives. Cereals are the most important and enriched source of dietary fiber with more insoluble dietary fiber than soluble. For dietary fiber modification, chemical treatment with various techniques is considered as significant approach owing to its safety point of view and involves less damage to the molecular structure of the dietary fiber through chemical reagents and content of soluble dietary fiber is increased more efficiently. The current study was aimed to nutritionally characterize the cereal grains and to partially convert insoluble dietary fiber into soluble dietary fiber through chemical treatments in combination with extrusion. For the purpose, two varieties of each cereal were characterized for their chemical composition, mineral profile, and dietary fiber content according to the respective methods. Then, dietary fiber ratio in cereals was modified through chemical treatments, that is, acid, alkaline, and consecutive acid–alkaline followed by extrusion. Results regarding dietary fiber content of cereal grains exhibited that wheat (12.03–12.20 g/100 g) contained higher total dietary fiber followed by sorghum (6.70–6.90 g/100 g). Additionally, modification of SDF (1.97%) and IDF (11.48%) ratio in wheat and SDF (1.19%) and IDF (24.25%) ratio in sorghum through extrusion processing was nonsignificant while acid–alkaline treatment showed highly significant results, that is, 768.2% increase in SDF and 56.5% decrease in IDF in wheat and 952.38% increase in SDF and 71.17% decrease in IDF in sorghum. Among chemical treatments, higher result was given by acid–alkaline method and the lower outputs were observed in case of extrusion in both cereals. Conclusively, soluble dietary fiber was significantly increased through chemical treatments alone or in combination with twin‐screw extrusion.
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