- COMPOSITIONS IN THE FORM OF AN INJECTABLE AQUEOUS SOLUTION COMPRISING AMYLIN AN AMYLIN RECEPTOR AGONIST OR AN AMYLIN ANALOG, AT LEAST ONE IONIC SPECIES AND AN AMPHOIPHILIC COMPOUNDS CONTAINING HYDRIPHOBIC RADICALS
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A composition in the form of an injectable solution includes: amylin, an amylin receptor agonist or an amylin analog; at least one ionic species; and an amphiphilic compound having a hydrophilic skeleton HB, substituted by at least one hydrophobic radical -Hy according to formula (I). A composition further is characterised in that it also has prandial insulin. In one embodiment, the composition also has GLP-1, GLP-1 analogs, and GLP-1 receptor agonists, commonly called GLP-1 RA.
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- Synthesis, molecular docking, cytotoxicity and antioxidant activity evaluation of isoindoline-1,3-dione derivatives
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A variety of amines have been employed to functionalize isobenzofuran-1,3-dione to obtain isoindoline-1,3-dione derivatives in the base free conditions. All the synthesized compounds are screened for their bioactivity through molecular docking, cytotoxicity (against HeLa) and antioxidant activity. ABTS and DPPH are employed to assess the antioxidant activity. Among the synthesized isoindoline-1,3-dione derivatives (3a-k), compound 3e has showed the best antioxidant activity and also exhibited better binding energy when docked with caspase-3 protein. Cytotoxicity of the synthesized compounds was studied against cervical cancer cell line (HeLa) and compound 3e has displayed better activity than other isoindoline derivatives.
- Kumar, Palanichamy Santhosh,Kumar, Kuruba Bharath,Obadiah, Asir,Kumar, Suluvoy Jagadish,Mohanapriya, Raman,Durairaj, Arulappan,Ramanathan, Subramanian,Vasanthkumar, Samuel
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p. 2548 - 2556
(2019/10/02)
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- Asymmetric aluminum complex containing acetylacetone derivative as well as preparation method and application thereof
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The invention discloses an asymmetric aluminum complex containing an acetylacetone derivative as well as a preparation method and application thereof. The asymmetric aluminum complex has a structuralformula shown as a formula I, wherein R1 is trifluoromethyl or methyl and R2 is phenyl, trifluoromethyl or methyl. The asymmetric aluminum complex catalyst containing the acetylacetone derivative disclosed by the invention is prepared from a ligand and trimethyl aluminum through reaction and has the advantages of simple preparation method, low cost and high product yield; the complex has a specialstructure and metal central aluminum is coordinated with divalent N, N, O and O of the ligand; the complex can be used as a catalyst for cyclic lactone ring-opening polymerization reaction and has the advantages of high catalytic activity, good stereoselectivity and rapid reaction speed; the polymerization reaction is simple to operate and an obtained polymerized product has narrow molecular weight distribution, controllable molecular weight and high yield; the asymmetric aluminum complex can be widely used for cyclic lactone ring-opening polymerization and is a very ideal catalyst. (The formula I is shown in the description.).
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Paragraph 0033
(2018/05/16)
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- Asymmetric ligand containing acetylacetone derivative as well as preparation method and application thereof
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The invention discloses an asymmetric ligand containing an acetylacetone derivative as well as a preparation method and application thereof. The ligand disclosed by the invention can be coordinated with N, N, O and O four teeth and can be complexed with trimethylaluminum to form a complex. According to the ligand disclosed by the invention, the structure is special, the preparation method is simple, and the formed aluminum complex can serve as a catalyst for a ring-opening polymerization reaction of cyclic lactone; the catalyst is high in catalytic activity, the stereoselectivity is high, thereaction rate is very high, the polymerization reaction is simple in operation, products of different molecular weights can be controllably obtained, and the selectivity is broad, so that the ligand has a good market prospect.
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Paragraph 0034
(2018/06/15)
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- Aluminum complexes containing salicylic aldehyde group as well as preparation method and application of complexes
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The invention discloses aluminum complexes containing a salicylic aldehyde group as well as a preparation method and application of the complexes. The complexes have a structural formula shown in a formula I in the description, wherein R is hydrogen, a C1-C4 alkane or a halogen. The aluminum complex catalyst containing the salicylic aldehyde group provided by the invention is obtained by reactinga ligand with trimethylaluminum, the preparation method is simple, the costs are low, and the product yield is high; the compounds have a special structure, the structure is various, and metal centralaluminum and divalent N, N, O and O of the ligand are subjected to coordination; the complexes can be used as a catalyst for a ring-opening polymerization reaction of a cyclic lactone and has high catalytic activity, good stereoselectivity and a high reaction speed, and the polymerization reaction is simple to operate; and the obtained polymer product has narrow molecular weight distribution, a controllable molecular weight and a high yield, can be widely used in ring-opening polymerization of the cyclic lactone, and is an ideal catalyst.
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Paragraph 0033
(2018/07/30)
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- Ligands containing salicylic aldehyde group as well as preparation methods and application of ligands
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The present invention discloses ligands containing a salicylic aldehyde group as well as preparation methods and an application of the ligands. The ligands provided by the present invention can implement N, N, O and O tetradentate coordination, and can separately be complexed with trimethylaluminum to form a complex. The ligands provided by the present invention have a special structure and the preparation methods are simple; the formed aluminum complex can be used as a catalyst of a ring-opening polymerization reaction of a cyclic lactone, and the catalyst has high catalytic activity, high stereoselectivity and a high reaction speed; and the polymerization reaction is simple to operate, products with different molecular weights can be obtained controllably, and the catalyst has wide selectivity and good market prospects.
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Paragraph 0034
(2018/07/30)
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- Development of unsymmetrical dyads as potent noncarbohydrate-based inhibitors against human β-N-acetyl-D-hexosaminidase
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Human β-N-acetyl-D-hexosaminidase has gained much attention due to its roles in several pathological processes and been considered as potential targets for disease therapy. A novel and efficient skeleton, which was an unsymmetrical dyad containing naphthalimide and methoxyphenyl moieties with an alkylamine spacer linkage as a noncarbohydrate-based inhibitor, was synthesized, and the activities were valuated against human β-N-acetyl-D- hexosaminidase. The most potent inhibitor exhibits high inhibitory activity with Ki values of 0.63 μM. The straightforward synthetic manners of these unsymmetrical dyads and understanding of the binding model could be advantageous for further structure optimization and development of new therapeutic agents for Hex-related diseases.
- Guo, Peng,Chen, Qi,Liu, Tian,Xu, Lin,Yang, Qing,Qian, Xuhong
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p. 527 - 531
(2013/07/26)
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- Design, synthesis and biological evaluation of novel nitrogen and sulfur containing hetero-1,4-naphthoquinones as potent antifungal and antibacterial agents
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A series of 2-Arylamino-3-chloro-1,4-naphthoquinones (3), 2-Amino-3-arylsulfanyl-1,4-naphthoquinones (5), 2-Arylamino-3-arylsulfanyl-1,4-naphthoquinones (6), Dihydrobenzo[f]naphtho[2,3-b][1,4]thiazepine-6,11-diones (9) (via Pictet-Spengler cyclization), Isoindoline-1,3-dione derivatives of 1,4-naphthoquinone (13), 2,2′-(1,4-Dioxo-1,4-dihydronaphthalene-2,3-diyl)bis(methylene)dibenzonitrile (14), 13-Amino-12-substituted-6H-benzo[e]naphtho [2,3-b][1,4]diazepine-6,11(12H)-diones (15-16), 2-Chloro-3-arylsulfanyl-1,4-naphthoquinones (17-18) and 3-Methyl-6H-benzo[b]phenothiazine-6,11(12H)-dione (19) were synthesized and studied for their antifungal and antibacterial activities. The results indicate that compounds 3b, 5a and 5b have potent antifungal activity. Amongst the most promising antifungal compounds, 3b showed better antifungal activity than clinically prevalent antifungal drug Fluconazole (MIC50 = 2.0 μg/mL) against Sporothrix schenckii (MIC50 = 1.56 μg/mL), significant profile against Candida albicans (MIC50 = 1.56 μg/mL), Cryptococcus neoformans (MIC50 = 0.78 μg/mL) and Trichophyton mentagraphytes (MIC50 = 1.56 μg/mL) and same antifungal activity when compared with Amphotericin-B against C. neoformans (MIC50 = 0.78 μg/mL). Compounds 3b, 5a and 5b also showed promising antibacterial activity.
- Tandon, Vishnu K.,Maurya, Hardesh K.,Mishra, Nripendra N.,Shukla, Praveen K.
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experimental part
p. 3130 - 3137
(2009/10/17)
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- Facile synthesis of 3-(diarylmethylene)isobenzofuranones, 4-(diarylmethyl)-1(2H)-phthalazinones and diarylmethanes
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Reflux of 2,2-diaryl-1,3-indanediones in ethyleneglycol with a catalytic amount of triethylamine affords 3-(diarylmethylene)isobenzofuranones in very good yields. The latter produces 4-diarymethyl-1(2H)-phthalazinones under reflux in hydrazine hydrate (99%), and diarylmethanes upon stirring in ethylenediamine.
- Das, Suven,Froehlich, Roland,Pramanik, Animesh
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- 6-(α-hydroxy-α-aryl/naphthyl)methyl-3,4-dihydro-2, 5-benzodiazocin-1(2H)-ones and diphenylmethanes from C-2 arylated 1,3-indanediones
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Stirring 2-hydroxy-2-aryl-1,3-indanediones in ethylenediamine at room temperature for 1-2 h produces 6-(α-hydroxy-α-aryl/naphthyl)methyl- 3,4-dihydro-2,5-benzodiazocin-1(2H)-ones in high yields. Under similar reaction conditions 2,2-diaryl-1,3-indanediones furnish diphenylmethanes.
- Kundu, Sandip Kumar,Das, Suven,Pramanik, Animesh
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p. 781 - 783
(2007/10/03)
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