- Glycolytic inhibition and antidiabetic activity on synthesized flavanone scaffolds with computer aided drug designing tools
-
Background: Diabetes mellitus is a challengeable metabolic disorder that leads to a group of complications when the HbA1c level is not maintained. Most of the existing drugs avail-able in the market in long-term use may lead to serious adverse effects. He
- Kiruthiga, Natarajan,Saravanan, Govindaraj,Selvinthanuja, Chellappa,Sivakumar, Thangavel,Srinivasan, Kulandaivel
-
p. 574 - 592
(2021/09/30)
-
- Design, synthesis and MAO inhibitory activity of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives
-
A series of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives (aurones, 1–20) were synthesized and screened for their inhibitory activity against hMAO. Seventeen compounds (1–5, 7–17, 19) were found to be selective towards hMAO-B, while two w
- Badavath, Vishnu Nayak,Nath, Chandrani,Ganta, Narayana Murthy,Ucar, Gulberk,Sinha, Barij Nayan,Jayaprakash, Venkatesan
-
p. 1528 - 1532
(2017/07/17)
-
- The synthesis and synergistic antifungal effects of chalcones against drug resistant Candida albicans
-
To identify effective and low toxicity synergistic antifungal compounds, 24 derivatives of chalcone were synthesized to restore the effectiveness of fluconazole against fluconazole-resistant Candida albicans. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of the antifungal synergist fluconazole were measured against fluconazole-resistant Candida albicans. This was done via methods established by the clinical and laboratory standards institute (CLSI). Of the synthesized compounds, 2′-hydroxy-4′-methoxychalcone (8) exhibited the most potent in vitro (FICI = 0.007) effects. The structure activity relationship of the compounds are then discussed.
- Wang, Yuan-Hua,Dong, Huai-Huai,Zhao, Fei,Wang, Jie,Yan, Fang,Jiang, Yuan-Ying,Jin, Yong-Sheng
-
supporting information
p. 3098 - 3102
(2016/06/13)
-
- Total synthesis and assignment of the absolute stereochemistry of xanthoangelol J: Development of a highly efficient method for Claisen-Schmidt condensation Dedicated to Late (Dr.) Jadab C. Sarma on his 55th birthday on first May 2013
-
The first total synthesis of cancer chemopreventive terpenyl hydroxychalcone xanthoangelol J isolated from Angelica keiskei was accomplished with asymmetric epoxidation, aromatic C-alkylation and Claisen-Schmidt condensation via enol mode as key steps. The crucial Claisen-Schmidt condensation has been accomplished by a novel green method using KHSO 4-SiO2 as a recyclable catalyst under microwave activation. The absolute configuration of the molecule was also determined.
- Kakati, Dwipen,Barua, Nabin C.
-
p. 637 - 642
(2014/02/14)
-
- Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor
-
Central neuromedin U 2 receptor (NMU2R) plays important roles in the regulation of food intake and body weight. Identification of NMU2R agonists may lead to the development of pharmaceutical agents to treat obesity. Based on the structure of rutin, a typi
- Ma, Ming-Liang,Li, Ming,Gou, Jiao-Jiao,Ruan, Tian-Yu,Jin, Hai-Shan,Zhang, Ling-Hong,Wu, Liang-Chun,Li, Xiao-Yan,Hu, Ying-He,Wen, Ke,Zhao, Zheng
-
p. 6117 - 6123
(2015/02/02)
-
- Synthesis and cdc25B inhibitory activity evaluation of chalcones
-
A library of sixty-five chalcones was prepared for screening against the protein phosphatase, cdc25B. From this library, thirteen compounds were found having good inhibitory activity. Two compounds have excellent activity and can be used for the design of
- Zhao, Fei,Zhao, Qing-Jie,Zhao, Jing-Xia,Zhang, Da-Zhi,Wu, Qiu-Ye,Jin, Yong-Sheng
-
p. 206 - 214
(2013/07/26)
-
- The synthesis and evaluation of novel hydroxyl substituted chalcone analogs with in vitro anti-free radicals pharmacological activity and in vivo anti-oxidation activity in a free radical-injury Alzheimer's model
-
Alzheimer's disease (AD) pathogenesis involves an imbalance between free radical formation and destruction. In order to obtain a novel preclinical anti-AD drug candidate, we synthesized a series of novel hydroxyl chalcone analogs which possessed anti-free radical activity, and screened their effects on scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH free radicals in vitro. Compound C7, 4,2'-dihydroxy-3,5-dimethoxychalcone was found to have potent activity in these anti-free radical activity tests. Further research revealed that C7 could elevate glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lower malonaldehyde (MDA) level in vivo in the Alzheimer's model. The indication of C7's effect on AD needs further study.
- Pan, Ying,Chen, Yicun,Li, Qingnan,Yu, Xiaoyu,Wang, Jinzhi,Zheng, Jinhong
-
p. 1693 - 1703
(2013/04/24)
-
- Design and synthesis of 3,5-diaryl-4,5-dihydro-1H-pyrazoles as new tyrosinase inhibitors
-
In this study, twenty 3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives with hydroxyl(s) (1a-1p, 2a-2d) were synthesized and their inhibitory activity on mushroom tyrosinase was examined. The results showed that among these compounds, 1-(5-(3,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl) ethanone 1d was found to be the most potent tyrosinase inhibitor with IC 50 value of 0.301 μM. Kinetic study revealed that these compounds were competitive inhibitors of tyrosinase and their structure-activity relationships were investigated in this article.
- Zhou, Zhixuan,Zhuo, Jiaru,Yan, Sujun,Ma, Lin
-
p. 2156 - 2162
(2013/05/08)
-
- Synthesis and evaluation of novel carbamate-substituted flavanone derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents
-
This study was designed to synthesize and evaluate flavanone derivatives with phenylcarbamate moiety as potent acetylcholinesterase (AChE) inhibitors and anti-amnestic agents for management of AD. The synthesis of carbamate-substituted flavanone derivativ
- Anand, Preet,Singh, Baldev
-
p. 1648 - 1659
(2013/07/26)
-
- Mosquito larvicidal studies of some chalcone analogues and their derived products: Structure-activity relationship analysis
-
A series of chalcone analogues and some of their derivatives were synthesized and subjected to the mosquito larvicidal study. Chalcones having electron releasing group(s) on either ring A or ring B showed high toxicity. Electron withdrawing group(s), especially at ring B, reduced the activity of chalcones. The activity was abruptly decreased due to replacement of ring A by CH3, extension of conjugation or blocking of α,β- unsaturated ketone part of chalcones by derivatization. Quantitative structure-activity relationship (QSAR) studies of these compounds were performed using various spatial, electronic and physicochemical parameters. Genetic Function approximation with linear and spline options was used as the chemometric tool for developing the QSAR models.
- Begum, Naznin A.,Roy, Nayan,Laskar, Rajibul A.,Roy, Kunal
-
experimental part
p. 184 - 191
(2012/02/16)
-
- Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis
-
Drugs inhibiting the iron scarcity-induced, siderophore-mediated iron-scavenging systems of Mycobacterium tuberculosis (Mtb) and Yersinia pestis (Yp) may provide new therapeutic lines of defense. Compounds with structural similarities to siderophores were synthesized and evaluated as antimicrobials against Mtb and Yp under iron-limiting conditions, which mimic the iron scarcity these pathogens encounter and must adapt to in the host, and under standard iron-rich conditions for comparison. New antimicrobials were identified, some of which warrant exploration as initial leads against potentially novel targets and small-molecule tools to assist in the elucidation of targets specific to iron-scarcity adapted Mtb and Yp.
- Stirrett, Karen L.,Ferreras, Julian A.,Jayaprakash, Venkatesan,Sinha, Barij N.,Ren, Tao,Quadri, Luis E.N.
-
p. 2662 - 2668
(2008/12/21)
-
- Pyrazoline-based mycobactin analogues as MAO-inhibitors
-
3,5-Diaryl carbothioamide pyrazolines designed as mycobactin analogs (mycobacterial siderophore) were reported to be potent antitubercular agents under iron limiting condition in our earlier study. Clinical complications of newly introduced antibiotic Linezolid, due its MAO inhibitory activity, prompted us to evaluate our compounds for their MAO-inhibitory activity against rat liver MAO-A and MAO-B as pyrazolines were reported to be antidepressants and MAO inhibitors. The present study carried out with this pilot library of 32 compounds will provide us with necessary information for designing antitubercular molecules with reduced MAO-inhibitory activity and also help us in identifying a selective MAO-B inhibitor which has potential clinical utility in neurodegenerative disorders. Thirty-two compounds analyzed has shown spectrum of activity from selective to nonselective against two isoforms of rat liver MAO-A and MAO-B and also as competitive, reversible to non-competitive, irreversible. It is also interesting to note that anti-tubercular compound 11, 14 and 16 were also found to be selective inhibitors of rat liver MAO-B. Docking studies with human MAO shows that compound 11 interacts with the catalytic site of both the isoforms, suggesting compound 11 as nonselective inhibitor of human MAO isoforms.
- Jayaprakash, Venkatesan,Sinha, Barij N.,Ucar, Gulberk,Ercan, Ayse
-
scheme or table
p. 6362 - 6368
(2009/09/30)
-
- Synthesis of benzylideneacetophenones and their inhibition of lipid peroxidation
-
A series of benzylideneacetophenone derivatives have been synthesized and found to show potent inhibition of the lipid peroxidation (LPO) in rat liver microsomes. All 19 compounds prepared in this series are LPO inhibitors. The highest activity was found
- Arty, Indyah S.,Timmerman, Henk,Samhoedi, Mochammed,Sastrohamidjojo,Sugiyanto,Van Der Goot, Henk
-
p. 449 - 457
(2007/10/03)
-
- 3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors
-
A novel series of 3,4-dihydroxychalcones was synthesized to evaluate their effects against 5-lipoxygenase and cyclooxygenase. Almost all compounds exhibited potent inhibitory effects on 5-lipoxygenase with antioxidative effects, and some also inhibited cyclooxygenase. The 2',5'-disubstituted 3,4- dihydroxychalcones with hydroxy or alkoxy groups exhibited optimal inhibition of cyclooxygenase. We found that 2',5'-dimethoxy-3,4-dihydroxychalcone (37; HX-0836) inhibited cyclooxygenase to the same degree as flufenamic acid and 5-lipoxygenase, more than quercetin. Finally, these active inhibitors of 5- lipoxygenase inhibited arachidonic acid-induced mouse ear edema more than phenidone.
- Sogawa,Nihro,Ueda,Izumi,Miki,Matsumoto,Satoh
-
p. 3904 - 3909
(2007/10/02)
-