54551-50-7Relevant academic research and scientific papers
Synthesis and antioxidant activities of berberine 9-: O -benzoic acid derivatives
Liu, Yanfei,Long, Shuo,Zhang, Shanshan,Tan, Yifu,Wang, Ting,Wu, Yuwei,Jiang, Ting,Liu, Xiaoqin,Peng, Dongming,Liu, Zhenbao
, p. 17611 - 17621 (2021/05/29)
Although berberine (BBR) shows antioxidant activity, its activity is limited. We synthesized 9-O-benzoic acid berberine derivatives, and their antioxidant activities were screened via ABTS, DPPH, HOSC and FRAP assays. The para-position was modified with halogen elements on the benzoic acid ring, which led to an enhanced antioxidant activity and the substituent on the ortho-position was found to be better than the meta-position. Compounds 8p, 8c, 8d, 8i, 8j, 8l, and especially 8p showed significantly higher antioxidant activities, which could be attributed to the electronic donating groups. All the berberine derivatives possessed proper lipophilicities. In conclusion, compound 8p is a promising antioxidant candidate with remarkable elevated antioxidant activity and moderate lipophilicity.
Development of 5-nitrothiazole derivatives: Identification of leads against both replicative and latent Mycobacterium tuberculosis
Jeankumar, Variam Ullas,Chandran, Manoj,Samala, Ganesh,Alvala, Mallika,Koushik, Pulla Venkat,Yogeeswari, Perumal,Salina, Elena G.,Sriram, Dharmarajan
, p. 7414 - 7417 (2013/02/22)
Twenty eight 5-nitrothiazole derivatives were synthesized and evaluated for in vitro activities against Mycobacterium tuberculosis (MTB), cytotoxicity against HEK 293T. Among the compounds, 5-nitro-N-(5-nitrothiazol-2-yl)furan-2- carboxamide (20) was found to be the most active compound in vitro with MICs of 5.48 μM against log-phase culture of MTB and also non-toxic up to 100 μM.
Synthesis of flavones and γ-benzopyranones using mild sonogashira coupling and 18-crown-6 ether mediated 6-endo cyclization
Chuang, Da-Wei,El-Shazly, Mohamed,Balaji D., Barve,Chung, Yu-Ming,Chang, Fang-Rong,Wu, Yang-Chang
, p. 4533 - 4540,8 (2020/08/31)
An efficient method for the synthesis of flavones and γ- benzopyranones has been developed utilizing a mild Sonogashira coupling and 18-crown-6 ether mediated 6-endo cyclization of o-alkynoylphenyl acetates. By using this strategy, flavones and γ-benzopyranones bearing electron-donating groups, halogens, and simple alkyl substituents were synthesized in satisfactory yields. A facile, mild, and selective method for the synthesis of flavones and γ-benzopyranones is reported. o-Alkynoylphenyl acetates were obtained from either acyl chloride derivatives or substituted salicylates. Upon removing the acetate group, flavones and γ- benzopyranones were synthesized within 15 min with the aid of 18-crown-6 ether. A library of flavones and γ-benzopyranones was established. Copyright
N-ACYL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF
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Page/Page column 57, (2011/11/13)
An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.)
N-ACYL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF
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Page/Page column 76, (2011/11/13)
An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or th
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
Spencer, Jeffrey R,McGee, Danny,Allen, Darin,Katz, Bradley A,Luong, Christine,Sendzik, Martin,Squires, Neil,Mackman, Richard L
, p. 2023 - 2026 (2007/10/03)
The structure-based design of potent and selective urokinase-type plasminogen activator (uPA) inhibitors with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described.
