- A facile single pot synthesis of highly functionalized tricyclic heterocycle compounds via sequential Knoevenagel-Michael addition and their α-glucosidase inhibition, antioxidants and antibacterial studies
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A facile methodology was developed which involved multicomponent single pot reaction which yielded the synthesis of highly functionalized tricyclic-heterocycle compounds (1c-6c) and (1d-7d) in good yields (60-80%). The discovered novel methodology involve
- Ahmed, Faiz,Rauf, Abdul,Sharif, Ahsan,Ahmad, Ejaz,Arshad, Muhammad,Esposito, Breno Pannia,Kaneko, Telma Mary,Qureshi, Ashfaq Mahmood
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p. 761 - 772
(2018/07/15)
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- Composition for trichogenousness
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The present invention relates to novel barbiturate and thiobarbiturate derivatives and a composition for promoting hair growth using the same. According to the present invention, the barbiturate and thiobarbiturate derivatives, in an animal model, have shown to promote hair growth and have excellent effects on hair growth by promoting regulation of Wnt/andbeta;-catenin and hair growth factor signaling and suppressing mechanism of apoptosis. Accordingly, the barbiturate and thiobarbiturate derivatives of the present invention may be used as a composition for promoting hair growth.COPYRIGHT KIPO 2017
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Paragraph 0200-0203; 0233-0234
(2017/08/08)
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- Organic synthesis by Twin Screw Extrusion (TSE): Continuous, scalable and solvent-free
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Mechanochemistry provides a method to reduce or eliminate the use of solvents by carrying out reactions through the grinding of neat reagents. Until recently a significant drawback of this form of synthesis has been the limited ability to scale up. Howeve
- Crawford, Deborah E.,Miskimmin, Clodagh K. G.,Albadarin, Ahmad B.,Walker, Gavin,James, Stuart L.
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supporting information
p. 1507 - 1518
(2017/05/10)
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- Sulfamic Acid Catalyzed Atom Economic, Eco-friendly Synthesis of Novel 7-(Aryl)-10-thioxo-7,9,10,11-tetrahedro-6H-pyrimido-[5′4′:5,6]pyrano[3,2-c]quinoline-6,8(5H)-dione and its Derivatives
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A series of novel 7-(3-chloro-phenyl)-10-thioxo-7,9,10,11-tetrahedro-6H-pyrimido-[5′4′:5,6] pyrano[3,2-c]quinoline-6,8(5H)-dione derivatives have been synthesized through the multi-component condensation of aromatic aldehydes, barbituric acid, and 2,4-dih
- Jadhav, Sunetra J.,Patil, Reshma B.,Kumbhar, Digambar R.,Patravale, Ajinkya A.,Chandam, Dattatraya R.,Deshmukh, Madhukar B.
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p. 2206 - 2215
(2017/07/25)
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- New compounds having skin whitening, antioxidant and PPAR activity, and medical use thereof
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PURPOSE: A novel compound with skin whitening, antioxidation, and PPAR activation effects, and a medical use thereof are provided to be used for a pharmaceutical composition or a cosmetic product. CONSTITUTION: A compound is denoted by chemical formula 1. A skin whitening composition contains the compound as an active ingredient. An antioxidative composition for preventing or treating oxidative diseases contains the compound of chemical formula 1 as an active ingredient. The oxidative diseases are selected among skin aging, pigmentation, wrinkling, psoriasis, or eczema. The composition prevents or treats diseases which are regulated by PPAR(peroxisome proliferator-activated receptor) activity. The PPAR includes PPAR alpha or PPAR gamma.
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Paragraph 0155; 0170
(2017/04/14)
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- NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREFOR
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Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.
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Paragraph 0139; 0147
(2014/02/16)
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- CoFe2O4 nanoparticles: An efficient heterogeneous magnetically separable catalyst for "click" synthesis of arylidene barbituric acid derivatives at room temperature
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A coprecipitation method was used to synthesize superparamagnetic CoFe 2O4 nanoparticles without using any capping agents/surfactants. The prepared nanoparticles were characterized using Fourier transform infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, X-ray diffraction, a vibrating sample magnetometer (VSM), N2 adsorption and thermogravimetric/differential thermal analysis/differential thermal gravimetry techniques. The synthesized spinel CoFe2O4 nanoparticles had an average size of 2-8 nm with a high surface area (140.9 m2/g). The field-dependent magnetization, demonstrated by VSM and saturation magnetization, was found to be 1.77 emu/g. An efficient method was used for the synthesis of arylidene barbituric acid derivatives using CoFe2O4 magnetic nanoparticles as a magnetically separable and reusable catalyst in aqueous ethanol. The attractive features of this synthetic protocol were very short reaction time, high yields, high turnover frequency, simple work-up procedure, economy, a clean reaction methodology, and chemoselectivity, as well as provision of an ecofriendly and green synthesis.
- Rajput, Jaspreet Kaur,Kaur, Gagandeep
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p. 1697 - 1704
(2013/10/21)
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- Antibacterial activities of some arylidene barbiturate derivatives
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A series of arylidene barbiturates 1-18 has been synthesized and evaluated against a number of Gram-positive and Gram-negative bacterial strains. Chromenopyrimidinedione derivatives 16 and 18 were found to be the most active against a number of Gram-positive organisms while compound 13 also showed antimicrobial activity against four Gram-positive strains. No significant activity was observed against Gram-negative bacterial strains.
- Khan, Khalid Mohammed,Ali, Muhammad,Ahmad, Aqeel,Amyn, Afroze,Karim, Aneela,Khan, Momin,Parveen, Shahnaz
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p. 890 - 893
(2013/07/26)
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- NH4Cl mediated new protocol for the synthesis of 5-arylidene barbiturates
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Eco-benign method for synthesizing arylidene barbiturates has been developed by using ammonium chloride (NH4Cl) in stoichiometric amount, as an enolization activator, in water. Execution of methodology is simple, products obtained in high yield
- Mohammed Khan, Khalid,Alia, Muhammad,Khana, Momin,Taha, Muhammad,Perveen, Shahnaz
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experimental part
p. 28 - 32
(2012/04/10)
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- Discovery of (Z)-5-(4-methoxybenzylidene)thiazolidine-2,4-dione, a readily available and orally active glitazone for the treatment of concanavalin A-induced acute liver injury of BALB/c mice
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A large amount of evidence suggests that monocytes/macrophages infiltration is implicated in a variety of inflammatory diseases including acute liver injury. Monocyte chemoattractant protein 1 (MCP-1) plays a crucial role in the process of macrophages recruitment. We herein presented a small-molecule library and a feasible quick screening method of evaluating potency of inhibition of chemotaxis of RAW264.7 cells stimulated by MCP-1. Fifty-three small molecules were synthesized and screened, and four compounds (2g, 2h, 4f, and 6h) showed inhibitory effects with IC50 values range from 0.72 to 20.47 μM, with compound 4f being the most efficient. Further in vivo studies demonstrated that oral administration of 2g, 2h, 4f, or 6h decreases, most significantly for 4f, the serum levels of alanine aminotransaminase (ALT) and asparate aminotransaminase (AST) in ConA-induced acute livery injury BALB/c mice. Histopathological evaluation liver sections confirmed 4f as a potent, orally active compound for hepatoprotective effects against ConA-induced acute liver injury in BALB/c mice.
- Luo, Youfu,Ma, Liang,Zheng, Hao,Chen, Lijuan,Li, Rui,He, Chunmei,Yang, Shengyong,Ye, Xia,Chen, Zhizhi,Li, Zicheng,Gao, Yan,Han, Jing,He, Gu,Yang, Li,Wei, Yuquan
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experimental part
p. 273 - 281
(2010/05/02)
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- Reaction of hexahydropyirimidine-2,4,6-trione with naphthalen-2-amine and benzaldehydes
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Previously unknown 12-aryl-7,8,9,10,11,12-hexahydrobenzo[f]pyrimido[4,5-b] quinoline-9,11-diones were synthesized by three-component condensation of naphthalen-2-amine with substituted benzaldehydes and barbituric acid through intermediate 5-benzylidenebarbituric acids. Nauka/Interperiodica 2007.
- Kozlov,Basalaeva
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p. 432 - 438
(2007/10/03)
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- Synthesis of arylmethylpyrimidinetriones and pyrimidoquinolinediones with fluorescent and nonlinear-optical properties
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5-Arylmethyl-2,4,6-(1H,3H,5H)pyrimidinetriones and 12-aryl-8,12- dihydrobenzo[f]pyrimido[4,5-b]quinoline-9,11-(7H,10H)diones were synthesized, and their spectral-luminescence and nonlinear-optical properties were examined.
- Kozlov,Bondarev,Odnoburtsev,Basalaeva
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p. 1101 - 1104
(2008/03/13)
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- One pot synthesis of barbiturates on reaction of barbituric acid with aldehydes under microwave irradiation using a variety of catalysts
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The condensation of barbituric acid with aldehydes under microwave irradiation in dry media has been investigated in the presence of NH 4OAc/AcOH (4/3, w/w) (41-54%), Montmorillonite K-10 (49-60%), Silica gel (52-63%), basic Al2O3 (56-67%), NaCl (57-69%), Montmorillonite KSF (62-70%), and KSF + NaCl (1:1, w/w) (70-89%).
- Dewan, Sharwan K.,Singh, Ravinder
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p. 3081 - 3084
(2007/10/03)
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- Molecular hyperpolarizabilities of barbituric acid and cyclobutene-1,2- dione derivatives. Electronic and steric effects
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A series of merocyanine dyes containing various donors and barbituric acid and cyclobutene-1,2-dione moieties as the acceptors have been synthesized and their first-order hyperpolarizabilities β were determined. The β values of barbituric acid derivatives increase as the strength of the donor is increased from 4-dimethylaminophenyl to trimethylindolinyl to benzothiazolinyl, apparently due to the gradual decrease in the bond length alternation (BLA) from a large positive value to an optimum one by a stronger donor. In contrast, the β values for the cyclobutene-1,2-dione derivatives decrease with the same variation of the donors even though the cyclobutene-1,2-dione is a poorer acceptor than the barbituric acid moiety. The results have been attributed to the electron-donating ability of the donors and the increased distortion of the chromophores from planarity.
- Cho, Bong Rae,Je, Jong Tae,Lee, Seung Jae,Lee, Sang Hae,Kim, Hyun Soo,Jeon, Seung Joon,Song, Ok-Keun,Wang
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p. 2141 - 2144
(2007/10/03)
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- Synthesis of a New Class of Uridine Phoshorylase Inhibitors
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A new series of potent uridine phosphorylase inhibitors have been prepared from barbituric acid.Among them 1--5-(m-benzyloxy)benzylbarbituric acid (37, BBBA) is the most promising having a Ki value of 1.1 +/- 0.2 nM wit
- Tzeng, Cherng-Chyi,Panzica, Raymond P.,Naguib, Fardos N.M.,Kouni, Mahmoud H. el
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p. 1399 - 1404
(2007/10/02)
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