Synthesis and Biological Activity Evaluation of Benzothiazole-Isoquinoline Derivatives DOI
Weihua Liu, Liping Guan,

Donghai Zhao

и другие.

SSRN Electronic Journal, Год журнала: 2022, Номер unknown

Опубликована: Янв. 1, 2022

There are currently no suitable clinical drugs available for patients with neurodegenerative diseases complicated by depression, based on a fusion technique to create effective multi-target ligands (MTDLs), we synthesized series of ( R )- N -(benzo[d]thiazol-2-yl)-2-(1-phenyl-3,4-dihydroisoquinolin-2(1 H )-yl) acetamide, and all compounds were subsequently tested their inhibitory potency against MAO cholinesterase in vitro enzyme activity assays, further specific MAO-B BuChE, among them, six 4b-4c , 4f 4g 4i ) have excellent activity. Subsequently, the classical antidepressant forced swim test (FST) was used verify results, results showed that indeed can significantly reduce immobility time, especially compound . In addition, cytotoxicity assessed MTT method AO staining, cell viabilities above 90% at concentrations, they not toxic L929 cells. Reversibility, kinetics, molecular docking studies also performed highest BuChE activities, which us bind main interaction sites both enzymes good blood-brain barrier (BBB) penetration. Provide new strategies future research combined depression.

Язык: Английский

Effect of magnetization on antibacterial, lipid-lowering and antioxidant activities of isoquinoline alkaloids DOI Creative Commons

Caihong Feng,

Weijie Li, Xiaoling Wang

и другие.

Scientific Reports, Год журнала: 2025, Номер 15(1)

Опубликована: Янв. 27, 2025

Язык: Английский

Процитировано

0
Benzophenanthridine and Related Alkaloids DOI
J. Armando Muñoz-Sánchez,

Lloyd Loza-Müller,

Felipe Vázquez‐Flota

и другие.

Springer eBooks, Год журнала: 2025, Номер unknown, С. 1 - 17

Опубликована: Янв. 1, 2025

Язык: Английский

Процитировано

0
Berberrubine as a novel TrxR inhibitor enhances cisplatin sensitivity in the treatment of non-small cell lung cancer DOI

Yajun Chu,

Qiuying Nie,

Xiedong Zhou

и другие.

Bioorganic Chemistry, Год журнала: 2025, Номер 158, С. 108329 - 108329

Опубликована: Март 4, 2025

Язык: Английский

Процитировано

0
Рециклізація 3-арил-1Н-ізохромен-4-карбальдегідів як ефективний підхід до синтезу функціоналізованих ізокумаринів та ізохінолінонів DOI Creative Commons
К.В. Кукушкіна, Виктория С. Москвина

Reports of the National Academy of Sciences of Ukraine, Год журнала: 2025, Номер 1, С. 49 - 57

Опубликована: Фев. 27, 2025

Досліджено перетворення 3-арил-1Н-ізохромен-4-карбальдегідів у 4-ароїл-1H-ізохромен-1-они та 4-ароїл- ізохінолін-1(2H)-они. Встановлено, що кип’ятіння ізокумарин-4-карбальдегідів метанолі з додаванням хлороводневої кислоти дає можливість отримати нові похідні 4-ароїлізокумаринів високими вихода- ми (75—84 %). Також показано, взаємодія як 3-арил-1Н-ізохромен-4-карбальдегідів, так і отриманих 4-ароїл-1H-ізохромен-1-онів аміаком N-нуклеофілом або етанолі приводить до утворення виключно 4-ароїлізохінолін-1(2H)-онів виходами 89 %. Синтезовані сполуки є перспективними для за- стосування в синтетичній органічній медичній хімії.

Процитировано

0
Spasmolytic Activity of 1,3-Disubstituted 3,4-Dihydroisoquinolines DOI Creative Commons
Miglena Milusheva, Mihaela Stoyanova, Vera Gledacheva

и другие.

Biomedicines, Год журнала: 2024, Номер 12(7), С. 1556 - 1556

Опубликована: Июль 13, 2024

This article concerns the spasmolytic activities of some novel 1,3-disubstituted 3,4-dihydroisoquinolines. These compounds can be evaluated as potential therapeutic candidates according to Lipinski's rule five, showing high gastrointestinal absorption and ability cross blood-brain barrier, which is a very important parameter in drug discovery processes. In silico simulation predicted smooth muscle relaxant activity for all compounds. Since contractile failure characteristic feature many disorders, current paper, we concentrate on parameters spontaneous responses (SM) cells compared well-known mebeverine. Two newly synthesized substances identified essential modulating regulators potentially used molecules. One these molecules also showed significant DPPH antioxidant rutin.

Язык: Английский

Процитировано

0
Diastereoselective dearomative bifunctionalization of isoquinolinium salts to access bridged tetrahydroisoquinolines DOI

Jiaqi Pei,

Tiantian Tang,

Jianing Zhang

и другие.

New Journal of Chemistry, Год журнала: 2024, Номер 48(37), С. 16151 - 16154

Опубликована: Янв. 1, 2024

We report a diastereoselective dearomative bifunctionalization strategy of using isoquinolinium salts to access bridged tetrahydroisoquinolines through one-pot three-component cascade process.

Язык: Английский

Процитировано

0
Synthesis of 4‐Cyclobutene‐Isoquinolines From Aryl Imidates by Ru(II)‐Catalyzed Domino C–H Activation/Cyclization DOI

Min Wang,

Lei Gao, Maozhong Miao

и другие.

Applied Organometallic Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Ноя. 13, 2024

ABSTRACT A highly regioselective approach for constructing 4‐cyclobutene‐isoquinoline derivatives through ruthenium‐catalyzed domino C–H activation/cyclization of aryl imidates has been demonstrated. This new transformation tolerates various substituted functional groups on and propargylic monofluoroalkynes, resulting in the corresponding products being delivered moderate yields.

Язык: Английский

Процитировано

0
Hendersines J–M: Isoquinoline alkaloids from Corydalis hendersonii Hemsl. with cardiomyocyte protective and NO production inhibitory effects DOI
Xiaochun Zhou, Zefeng Zhang, Changxin Liu

и другие.

Phytochemistry, Год журнала: 2024, Номер unknown, С. 114365 - 114365

Опубликована: Дек. 1, 2024

Язык: Английский

Процитировано

0
Exploring the microbial composition and metabolites in dark tea Kombucha: a comparative analysis with green tea Kombucha DOI Creative Commons
Qing Nie,

Shuqia Ding,

Mingwei Xie

и другие.

Beverage Plant Research, Год журнала: 2020, Номер 0(0), С. 1 - 12

Опубликована: Янв. 1, 2020

Язык: Английский

Процитировано

0
Synthesis and Biological Activity Evaluation of Benzothiazole-Isoquinoline Derivatives DOI
Weihua Liu, Liping Guan,

Donghai Zhao

и другие.

SSRN Electronic Journal, Год журнала: 2022, Номер unknown

Опубликована: Янв. 1, 2022

There are currently no suitable clinical drugs available for patients with neurodegenerative diseases complicated by depression, based on a fusion technique to create effective multi-target ligands (MTDLs), we synthesized series of ( R )- N -(benzo[d]thiazol-2-yl)-2-(1-phenyl-3,4-dihydroisoquinolin-2(1 H )-yl) acetamide, and all compounds were subsequently tested their inhibitory potency against MAO cholinesterase in vitro enzyme activity assays, further specific MAO-B BuChE, among them, six 4b-4c , 4f 4g 4i ) have excellent activity. Subsequently, the classical antidepressant forced swim test (FST) was used verify results, results showed that indeed can significantly reduce immobility time, especially compound . In addition, cytotoxicity assessed MTT method AO staining, cell viabilities above 90% at concentrations, they not toxic L929 cells. Reversibility, kinetics, molecular docking studies also performed highest BuChE activities, which us bind main interaction sites both enzymes good blood-brain barrier (BBB) penetration. Provide new strategies future research combined depression.

Язык: Английский

Процитировано

0