- 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 0093-0095; 0192-0193
(2017/08/08)
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- Synthesis and structure-activity relationship of thiobarbituric acid derivatives as potent inhibitors of urease
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A series of thiobarbituric acid derivatives 1-27 were synthesized and evaluated for their urease inhibitory potential. Exciting results were obtained from the screening of these compounds 1-27. Compounds 5, 7, 8, 11, 16, 17, 22, 23 and 24 showed excellent urease inhibition with IC50 values 18.1 ± 0.52, 16.0 ± 0.45, 16.0 ± 0.22, 14.3 ± 0.27, 6.7 ± 0.27, 10.6 ± 0.17, 19.2 ± 0.29, 18.2 ± 0.76 and 1.61 ± 0.18 μM, respectively, much better than the standard urease inhibitor thiourea (IC50 = 21 ± 0.11 μM). Compound 3, 4, 10, and 26 exhibited comparable activities to the standard with IC50 values 21.4 ± 1.04 and 21.5 ± 0.61μM, 22.8 ± 0.32, 25.2 ± 0.63, respectively. However the remaining compounds also showed prominent inhibitory potential The structure-activity relationship was established for these compounds. This study identified a novel class of urease inhibitors. The structures of all compounds were confirmed through spectroscopic techniques such as EI-MS and 1H NMR.
- Khan, Khalid Mohammed,Rahim, Fazal,Khan, Ajmal,Shabeer, Muhammad,Hussain, Shafqat,Rehman, Wajid,Taha, Muhammad,Khan, Momin,Perveen, Shahnaz,Choudhary, M. Iqbal
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p. 4119 - 4123
(2014/08/18)
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- Solvent-free, microwave assisted Knoevenagel condensation of novel 2,5-disubstituted indole analogues and their biological evaluation
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A rapid, efficient and environmental benign methodology for the preparation of 2,5-disubstituted indole analogues is developed. 2,5-Disubstituted indole-3-carboxaldehydes (1a-c) undergo Knoevenagel condensation with barbiturates (2 & 4), thiazolidine-2,4-dione (6) and 3-methyl-1H-pyrazol- 5(4H)-one (8) in solvent-free, NH4OAc catalyzed, microwave assisted reaction. Structures of the products thus obtained were confirmed by their m.p, Elemental analysis, IR, 1H NMR, 13C NMR and Mass spectral data. The in vitro antioxidant and cytotoxic activities against three tumor cell lines were evaluated and discussed in terms of their structural differences. Among the screened compounds 9b, 9c, 7b and 5b exhibited excellent antioxidant activity. Compounds 9b, 9c and 7b have shown strong cytotoxicity among the compounds tested.
- Biradar,Sasidhar
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experimental part
p. 6112 - 6118
(2012/01/03)
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- Facile syntheses of bioactive 5-arylidenethiobarbituric acids
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A simple and green chemistry route for the preparation of 5-arylidenethiobarbituric acids has been developed by Knoevenagel condensation of thiobarbituric acid with different aromatic and heteroaromatic aldehydes using catalytic amount of acetic acid by g
- Sharif, Ahsan,Ahmed, Ejaz,Munawar, Munawar Ali,Jabeen, Shamsa,Khan, Misbah-Ul-Ain,Begum, Robina,Farrukh, Aleeza,Ashraf, Muhammad,Arshad, Shafia,Afza, Nighat
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experimental part
p. 578 - 586
(2012/01/05)
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- Alumina Catalyzed Synthesis of Fused Thioxopyrimidine Derivatives under Microwaves
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An expeditious solventless approach for the synthesis of pyrazolino[3,4-d]/isoxazolino[3,4-d]/pyrano[2,3-d]/iminopyrimidino[4,5-d]/ thioxopyrimidino[4,5-d]/thiazino[5,4-d] pyrimidines from 2-thiobarbituric acid using supported reagents (acidic/basic alumi
- Kidwai,Mohan,Rastogi
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p. 3747 - 3759
(2007/10/03)
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- Barbituric acid analogs as therapeutic agents
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This invention pertains to active barbituric acid analogs which inhibit HIF-1 activity (e.g., the interaction between HIF-1α and p300) and thereby inhibit angiogenesis, tumorigensis, and proliferative conditions, such as cancer. The present invention also
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