scholarly journals Synthesis and Biological Evaluation of New Substituted 3-[4-(Phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one Derivatives asα-Glucosidase Inhibitors

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Yu-ling Wang ◽  
Ting-jian Zhang ◽  
Jing-wei Liang ◽  
Fan-hao Meng ◽  
Shao-jie Wang
Keyword(s):  
Inhibitory Activity ◽  
Methoxy Group ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Glucosidase Inhibitors ◽  
Further Development ◽  
Synthesis And Biological Evaluation

A series of new substituted 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives bearing groups methoxy,tert-butyl, and atoms of halogens at thepara-position of the A-ring were synthesized andin vitrobiological activities were evaluated as nonsugarα-glucosidase inhibitors. Most of the test compounds demonstrated significantα-glucosidase inhibitory activity relative to that of Acarbose (IC50= 29.26 μM). Thepara-substitution with a methoxy group or halogens could notably increase the potency. Compounds17,18, and23, with IC50values of 0.025 μM, 0.014 μM, and 0.018 μM, respectively, may be of significance for the further development of new nonsugarα-glucosidase inhibitors.

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

Synthesis and biological evaluation of oleanolic acid derivative–chalcone conjugates as α-glucosidase inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (21) ◽  
pp. 10862-10874 ◽  
Author(s):  
Chu Tang ◽  
Linhui Zhu ◽  
Yu Chen ◽  
Rui Qin ◽  
ZhiNan Mei ◽  
...  
Keyword(s):  
Acid Derivative ◽  
Oleanolic Acid ◽  
Biological Evaluation ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Oleanolic Acid Derivative

Series of oleanolic acid derivative–chalcone conjugates were designed, synthesized and their α-glucosidase inhibitory activities were investigatedin vitro.

Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles

2019 ◽  
Vol 15 (5) ◽  
pp. 521-536 ◽  
Author(s):  
Natalya Agafonova ◽  
Evgeny Shchegolkov ◽  
Yanina Burgart ◽  
Victor Saloutin ◽  
Alexandra Trefilova ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Antipyretic Activity ◽  
Starting Point ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Synthesis And Biological Evaluation ◽  
Cox 1

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices. Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds. Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2. Conclusion: The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.

Design, synthesis and biological evaluation of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives as potential BRAFV600E inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (95) ◽  
pp. 52702-52711 ◽  
Author(s):  
Ya-Juan Qin ◽  
Man Xing ◽  
Ya-Liang Zhang ◽  
Jigar A. Makawana ◽  
Ai-Qin Jiang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Methyl Benzoate ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Potent Inhibitory Activity ◽  
Benzoate Derivatives

A series of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives (6a–10d) were designed and synthesized and evaluated as BRAFV600 inhibitors. Among them, compound 10a showed the most potent inhibitory activity against A375, WM266.4 and BRAFV600Ein vitro with IC50 values of 1.36 μM, 0.94 μM and 0.11 μM, respectively.

Total synthesis and biological evaluation of oscillatoxin D, E, and F

2021 ◽  
Author(s):  
Yusuke Araki ◽  
Yusuke Hanaki ◽  
Masaki Kita ◽  
Koutaro Hayakawa ◽  
Kazuhiro Irie ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Cell Line ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Marine Cyanobacteria ◽  
Methyl Group ◽  
Synthetic Strategy ◽  
Target Molecules ◽  
Synthesis And Biological Evaluation

Abstract Oscillatoxins (OTXs) and aplysiatoxins (ATXs) are biosynthetically related polyketides produced by marine cyanobacteria. We previously developed a synthetic route to phenolic O-methyl analogs of OTX-D and 30-methyl-OTX-D during collective synthesis of these natural products. According to our synthetic strategy, we achieved total synthesis of OTX-D, 30-methyl-OTX-D, OTX-E, and OTX-F by deprotecting the O-methyl group in an earlier intermediate, and determined their biological activities. Although OTX-D and 30-methyl-OTX-D have been reported to show anti-leukemic activity against L1210 cell line, we found that their cytotoxicity in vitro against this cell line is relatively weak (IC50: 29–52 μM). In contrast, OTX-F demonstrated cell line-selective anti-proliferative activity against DMS-114 lung cancer cells, which implies that OTXs target as yet unknown target molecules as part of this unique activity.

scholarly journals BIOLOGICAL ACTIVITIES OF NOVEL IN VITRO RAISED STEVIA PLANT

2017 ◽  
Vol 10 (8) ◽  
pp. 240 ◽  
Author(s):  
Neeta Raj Sharma ◽  
Vineet Meshram ◽  
Mahiti Gupta
Keyword(s):  
Pancreatic Lipase ◽  
Staphylococcus Epidermidis ◽  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Gram Negative Bacteria ◽  
Herbal Formulation ◽  
Further Development

  Objective: This communication explores a lead fraction from methanolic extract of novel Stevia species raised under in vitro conditions for its various biological activities.Methods: The dried Stevia leaves were crushed in methanol to get the polar extract. This methanol extract was tested for pancreatic lipase and alpha-amylase inhibitory activity using quantitative plate assays. Antibacterial property of the extract was also evaluated against Staphylococcus epidermidis, Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. Further, the antioxidant potential was evaluated using 1,1-diphenyl-2-picrylhydrazyl.Results: The methanolic extract inhibited pancreatic lipase with IC50 of 5.74 μg/ml in a similar manner to a well-known anti-obesity drug in the market orlistat. The methanolic extract also showed a better pancreatic α-amylase inhibitory activity (IC50=88 μg/ml) than acarbose. Further, the lead fraction exhibited 88.48% antioxidant activity. It also exhibited broad spectrum antimicrobial activity against the spectrum of Gram-positive and Gram-negative bacteria tested under laboratory conditions with a minimal inhibitory concentration ranging from 1.95 to 31.25 μg/ml.Conclusion: Thus, this study signifies the vast potential of the lead fraction from a novel Stevia species for further development into a herbal formulation for prevention of various infectious and non-infectious diseases.

scholarly journals Synthesis and biological evaluation of geldanamycin–ferulic acid conjugate as a potent Hsp90 inhibitor

RSC Advances ◽  
2019 ◽  
Vol 9 (72) ◽  
pp. 42509-42515
Author(s):  
Zhenyu Li ◽  
Lejiao Jia ◽  
Hui Tang ◽  
Yuemao Shen ◽  
Chengwu Shen
Keyword(s):  
Breast Carcinoma ◽  
Antitumor Activity ◽  
Ferulic Acid ◽  
Inhibitory Activity ◽  
Hsp90 Inhibitor ◽  
Biological Evaluation ◽  
Human Breast ◽  
Acid Conjugate ◽  
Synthesis And Biological Evaluation

Compared to 17-AAG, LZY228 exhibited higher Hsp90 inhibitory activity in vitro and better antitumor activity in human breast carcinoma (MDA-MB-231) xenograft nude mice.

scholarly journals Synthesis and Biological Evaluation of Thalidomide Derivatives as Potential Anti-Psoriasis Agents

2018 ◽  
Vol 19 (10) ◽  
pp. 3061 ◽  
Author(s):  
Kai-Wei Tang ◽  
Zih-Chan Lin ◽  
Yeh-Long Chen ◽  
Cherng-Chyi Tzeng ◽  
Jia-You Fang ◽  
...  
Keyword(s):  
Structural Optimization ◽  
Inhibitory Activity ◽  
Methoxy Group ◽  
Biological Evaluation ◽  
Hacat Cells ◽  
Cell Cytotoxicity ◽  
Tnf Α ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Several thalidomide derivatives were synthesized and evaluated for their anti-inflammatory activity. Introduction of the benzyl group to the parent thalidomide is unfavorable in which 2-(1-benzyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione (4a) was inactivated. However, the inhibitory activities on TNF-α and IL-6 expression in HaCaT cells were improved by the substitution of a chloro- or methoxy- group at the phenyl position of 4a. The IL-6 inhibitory activity decreased in an order of 5c (69.44%) > 4c (48.73%) > 6c (3.19%) indicating the 3-substituted derivative is more active than the 4-substituted counterpart, which in turn is more active than the 2-substituted counterpart. Among them, 2-[1-(3-chlorobenzyl)-2,6-dioxopiperidin-3-yl]isoindoline-1,3-dione (5c) was found to inhibit TNF-α and IL-6 expression in HaCaT cells with a higher potency than thalidomide and no significant cell cytotoxicity was detected at 10 μM. In psoriasis, Compound 5c reduced IL-6, IL-8, IL-1β and IL-24 in imiquimod-stimulated models. Our results indicated that compound 5c is a potential lead of novel anti-psoriasis agents. Structural optimization of compound 5c and its in vivo assay are ongoing.

scholarly journals Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation

Biomedicines ◽  
2021 ◽  
Vol 9 (10) ◽  
pp. 1443
Author(s):  
João L. Serrano ◽  
Diana Lopes ◽  
Melani J. A. Reis ◽  
Renato E. F. Boto ◽  
Samuel Silvestre ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Biological Activities ◽  
Chemical Change ◽  
Biological Evaluation ◽  
Reference Drug ◽  
Xanthine Oxidase Inhibitors ◽  
Low Cytotoxicity ◽  
Synthesis And Biological Evaluation ◽  
Better Than

Xanthine oxidase (XO) is the enzyme responsible for the conversion of endogenous purines into uric acid. Therefore, this enzyme has been associated with pathological conditions caused by hyperuricemia, such as the disease commonly known as gout. Barbiturates and their congeners thiobarbiturates represent a class of heterocyclic drugs capable of influencing neurotransmission. However, in recent years a very large group of potential pharmaceutical and medicinal applications have been related to their structure. This great diversity of biological activities is directly linked to the enormous opportunities found for chemical change off the back of these findings. With this in mind, sixteen bis-thiobarbiturates were synthesized in moderate to excellent reactional yields, and their antioxidant, anti-proliferative, and XO inhibitory activity were evaluated. In general, all bis-thiobarbiturates present a good antioxidant performance and an excellent ability to inhibit XO at a concentration of 30 µM, eight of them are superior to those observed with the reference drug allopurinol (Allo), nevertheless they were not as effective as febuxostat. The most powerful bis-thiobarbiturate within this set showed in vitro IC50 of 1.79 μM, which was about ten-fold better than Allo inhibition, together with suitable low cytotoxicity. In silico molecular properties such as drug-likeness, pharmacokinetics, and toxicity of this promising barbiturate were also analyzed and herein discussed.

scholarly journals Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors

2021 ◽  
Vol 22 (11) ◽  
pp. 5680
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Ellagic Acid ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Cognitive Enhancer ◽  
Cell Level ◽  
Design Synthesis ◽  
Comparable Activity ◽  
Inhibitory Potential ◽  
Synthesis And Biological Evaluation

Urolithins (hydroxylated 6H-benzo[c]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6H-benzo[c]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6H-benzo[c]chromen-6-one derivative 1f was found to have the optimal inhibitory potential (IC50: 3.67 ± 0.47 μM). It also exhibited comparable activity in comparison to that of BAY 60-7550 in vitro cell level studies.

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