- New compounds having skin whitening activity and medical use thereof
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The present invention relates to novel compounds having skin whitening activity and a medical use thereof, wherein the novel compounds are represented by chemical formula 1. The compounds according to the present invention have skin whitening activity tha
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Paragraph 0070; 0072; 0074; 0078; 0079
(2017/11/23)
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- Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity
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Some novel indolizine derivatives were synthesized by bioisosteric modification of imidazo[1,2-a]pyridine for anti-inflammatory activity. The physicochemical characterization and structure of compounds were elucidated by state of the art spectroscopic technique. Induced fit docking was performed for initial screening to elucidate the interactions with corresponding amino acids of cyclooxygenase (COX-1, COX-2) and lipoxygenase (LOX) enzymes. The target compounds 53–60 were then evaluated against in vivo carrageenan and arachidonic acid induced rat paw edema models for anti-inflammatory activity. Amongst all the synthesized derivatives, compound 56 showed the significant anti-inflammatory activity in both rat paw edema models with very less ulcerogenic liability in comparison to standard diclofenac, celecoxib, and zileuton. The compounds 56 was further assessed to observe in vitro enzyme inhibition assay on both cyclooxygenase and lipoxygenase enzyme where it showed a preferential and selective non-competitive enzyme inhibition towards the COX-2 (IC50?=?14.91?μM, Ki?=?0.72?μM) over COX-1 (IC50?>?50?μM) and a significant non-competitive inhibition of soybean lipoxygenase enzyme (IC50?=?13.09?μM, Ki?=?0.92?μM). Thus, in silico, in vivo, and in vitro findings suggested that the synthesized indolizine compound 56 has a dual COX-2 and LOX inhibition characteristic and parallel in vivo anti-inflammatory activity in comparison to the standard drugs.
- Shrivastava, Sushant K.,Srivastava, Pavan,Bandresh, Robin,Tripathi, Prabhash Nath,Tripathi, Avanish
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p. 4424 - 4432
(2017/07/22)
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- Laccase-catalyzed oxidative phenolic coupling of vanillidene derivatives
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The laccase-catalyzed oxidative phenolic coupling of vanillidene derivatives using aerial oxygen as the oxidant has been developed. Depending on the substitution pattern of the vanillidene double bond of the substrate, either dilactones, dihydrobenzo[b]furans or biphenyls are formed.
- Constantin, Mihaela-Anca,Conrad, Juergen,Beifuss, Uwe
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supporting information
p. 2375 - 2379
(2013/02/21)
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- First bovine serum albumin-promoted synthesis of enones, cinnamic acids and coumarins in ionic liquid: An insight into the role of protein impurities in porcine pancreas lipase for olefinic bond formation
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During studies on exploiting the catalytic promiscuity of crude porcine pancreas lipase (PPL) in ionic liquid for C=C bond formations, bovine serum albumin (BSA) was found to be competing for these reactions. After a detailed investigation, we establish that these transformations are possible by unspecific protein catalysis rather than catalytic promiscuity of "PPL" - a first insight into the role of protein impurities in crude enzyme. Thus, a novel and highly efficient, environmentally friendly approach involving synergistic catalysis by bovine serum albumin-1-butyl-3- methylimidazolium bromide (BSA-[bmim]Br) has been developed for the synthesis of (E)-α,β-unsaturated compounds including a one-pot cascade synthesis of cinnamic acids and coumarins via aldol, Knoevenagel and Knoevenagel-Doebner condensations.
- Sharma, Nandini,Sharma, Upendra K.,Kumar, Rajesh,Katoch, Nidhi,Kumar, Rakesh,Sinha, Arun K.
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scheme or table
p. 871 - 878
(2011/06/19)
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- METHODS FOR PHOTOSTABILIZING INGREDIENTS WITHIN COSMETICS, PERSONAL CARE AND HOUSEHOLD PRODUCTS AND COMPOSITIONS OBTAINED THEREFROM
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The present invention relates to methods and compositions for using photostabilizer compounds for stabilizing formulation ingredients, like flavors, fragrances, colors, antioxidants, polymers, within cosmetics, personal care and household products, against degradation from sun light, heat and air oxidation resulting in improvement in storage stability, viscosity, and maintenance of color of the formulated products.
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