Synthesis, in vitro biological analysis and molecular docking studies of new thiadiazole-based thiourea derivatives as dual inhibitors of a-amylase and a-glucosidase DOI Creative Commons

Imran Khan,

Wajid Rehman, Fazal Rahim

et al.

Arabian Journal of Chemistry, Journal Year: 2023, Volume and Issue: 16(9), P. 105078 - 105078

Published: June 17, 2023

Diabetes mellitus is a syndrome that caused due to the imbalance of insulin production in body. In present study we have synthesized class fifteen compounds (1–15) based on thiadiazole-bearing thiourea were assessed for vitro alpha-amylase and alpha-glucosidase inhibitory potentials against standard drug acarbose. this series, all scaffolds recognized as inhibitors both targeted enzymes, α-amylase having varied range from IC50 values = 35.70 ± 0.70 µM 1.30 0.05 acarbose (10.30 0.20 µM) while α-glucosidase 37.60 0.80 2.20 0.10 (9.80 µM). Among nine such 4, 6, 7, 9, 8, 11, 12, 14 15 showed excellent activity a-amylase a-glucosidase found many folds more potent than drugs change nature number/s substituent along entire skeleton. A molecular docking was conducted active understand binding modes synthetic analogs how they show interaction with part enzymes. To confirm structure different spectroscopic techniques will be used like NMR HREI-MS.

Language: Английский

Transition-Metal-Catalyzed C–S, C–Se, and C–Te Bond Formations via Cross-Coupling and Atom-Economic Addition Reactions. Achievements and Challenges DOI
I. P. Beletskaya, Valentine P. Ananikov

Chemical Reviews, Journal Year: 2022, Volume and Issue: 122(21), P. 16110 - 16293

Published: Sept. 16, 2022

In the present review, we discuss recent progress in field of C–Z bond formation reactions (Z = S, Se, Te) catalyzed by transition metals. Two complementary methodologies are considered─catalytic cross-coupling and catalytic addition reactions. The development advanced systems is aimed at improved catalyst efficiency, reduced loading, better cost environmental concerns, higher selectivity yields. important rise research efforts sustainability green chemistry areas critically assessed. paramount role mechanistic studies a new generation addressed, key achievements, problems, challenges summarized for this field.

Language: Английский

Citations

201

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase DOI Creative Commons

Rami J. Obaid,

Nafeesa Naeem, Ehsan Ullah Mughal

et al.

RSC Advances, Journal Year: 2022, Volume and Issue: 12(31), P. 19764 - 19855

Published: Jan. 1, 2022

The present review focuses on various heterocyclic scaffolds and their role in designing developing new potential AChE BChE inhibitors to treat AD.

Language: Английский

Citations

85

The chemistry of heterocycles in the 21st century DOI
Valery N. Charushin, Egor V. Verbitskiy, О. Н. Чупахин

et al.

Russian Chemical Reviews, Journal Year: 2024, Volume and Issue: 93(7), P. RCR5125 - RCR5125

Published: July 1, 2024

The chemistry of heterocyclic compounds has traditionally been and remains a bright area chemical science in Russia. This is due to the fact that many heterocycles find widest application. These are key structural fragments most drugs, plant protection agents. Many natural also derivatives heterocycles. At present, more than half hundreds millions known collective review devoted achievements Russian chemists this field over last 15–20 years. presents leading heterocyclists representing both RAS institutes university science. It worth noting wide scope review, terms geography author teams, covering whole our large country, diversity research areas. Practically all major types represented review. special attention focused on practical applications design new drugs biologically active compounds, high-energy molecules, materials for organic electronics photovoltaics, ligands coordination chemistry, other rapidly developing advances would not be possible without development fundamental transformations chemistry.<br> Bibliography — 2237 references.

Language: Английский

Citations

37

Computational study of 3-thiophene acetic acid: Molecular docking, electronic and intermolecular interactions investigations DOI

Takoua Ben Issa,

Abir Sagaama,

Noureddine Issaoui

et al.

Computational Biology and Chemistry, Journal Year: 2020, Volume and Issue: 86, P. 107268 - 107268

Published: April 22, 2020

Language: Английский

Citations

74

A review of recent synthetic strategies and biological activities of isoxazole DOI
Chandrashekhar P. Pandhurnekar,

Himani C. Pandhurnekar,

Arvind J. Mungole

et al.

Journal of Heterocyclic Chemistry, Journal Year: 2022, Volume and Issue: 60(4), P. 537 - 565

Published: Oct. 13, 2022

Abstract Among different heterocyclic compounds, isoxazole and their analogues are very important classes of compounds as they display an extensive range biological actions. This makes such scaffolds structures in the field medicinal chemistry. From literature assessment, is clinically proven to be effective anti‐bacterial, anti‐fungal, anti‐inflammatory, anti‐cancer, anti‐tubercular, anti‐neoplastic agent. The derivatives which exhibits adjustment structure have shown a high degree variety properties evident them beneficial progress novel bioactive drugs show enhanced effectiveness along with minor harmfulness. Structural aspects having aromaticity weaker nitrogen‐oxygen bonding provide potential site for ring cleavage. Thus, this system allows easier modifications substituents consequently make useful intermediates various synthetic routes compounds. Hence, synthesis evaluation isoxazole‐containing molecules wider therapeutic consequences always topic interest chemists. light comprehensive research on isoxazole, it thought worthwhile review pathways broad spectrum

Language: Английский

Citations

60

A general electron donor–acceptor complex enabled cascade cyclization of alkynes to access sulfur-containing heterocycles DOI
Wenchao Yang, Yu Sun, Xiaobo Bao

et al.

Green Chemistry, Journal Year: 2023, Volume and Issue: 25(8), P. 3111 - 3116

Published: Jan. 1, 2023

A general visible light-promoted and electron–donor–acceptor complex-enabled cascade reaction of alkynes to produce functionalized sulfur-containing heterocycles under photocatalyst-, base-, oxidant- metal-free conditions was developed.

Language: Английский

Citations

28

Synthesis of new pyridine-thiazolidin-4-one and pyridine-pyrazole-thiazolidin-4-one conjugates: Molecular modelling and docking as antimicrobial agents DOI
Hana M. Abumelha,

Omar M. Alatawi,

Ali Hamzah Alessa

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1309, P. 138233 - 138233

Published: April 3, 2024

Language: Английский

Citations

12

Biological activity and laser efficacy of new Co (II), Ni (II), Cu (II), Mn (II) and Zn (II) complexes with phthalic anhydride DOI

Ban D. Salih,

Adil Hussein Dalaf, Mustafa A. Alheety

et al.

Materials Today Proceedings, Journal Year: 2020, Volume and Issue: 43, P. 869 - 874

Published: Aug. 9, 2020

Language: Английский

Citations

62

A Review: Medicinally Important Nitrogen Sulphur Containing Heterocycles DOI Open Access
Praveen Kumar Sharma,

Andleeb Amin,

Manjeet Kumar

et al.

The Open Medicinal Chemistry Journal, Journal Year: 2020, Volume and Issue: 14(1), P. 49 - 64

Published: Sept. 14, 2020

Nitrogen sulphur containing heterocycles have specific properties due to which they can be used as a potential material in different type of industries such medicinal/pharmaceutical, paint, packing and textile, required for various chemical, physical operations their use products. Especially dyes, agrochemicals, medicine, etc . make them more significant. In present days, Nitrogen-Sulfur are repeatedly attracting the interest chemists exceptional bioactive behavior. The study is review work carried out by chemist discovery new, effective, medicinally important heterocyclic compounds. basically focused on nitrogen-sulfur therapeutic interest, especially with thiazole, thiazine, pyrimidine, morpholine piperazine heterosystems, benzothiazines, pyrazole-benzothiazines, morpholine-benzothiazines, piperazine-benzothiazines pyrimidine-benzothiazoles, mainly unique structural features, enable exhibit number biological pharmacological activities. Due novel mode action, broad spectrum activity, lesser toxicity towards mammalian cells, suitable profiles humans triggered Sulphur designing synthesizing derivatives better properties. overall objective discuss importance biodynamic structurally diverse interest: morpholine, piperazine, pyrozole, benothiazoles, pyrimidobenzothiazoles, 4H-1,4-benzothiazines, pyrazolyl-benzothiazines, morpholinyl-benzothiazines piperazinylbenzothiazines order access commercial molecules search future.

Language: Английский

Citations

59

Furazans in Medicinal Chemistry DOI

Ross S. Mancini,

Christopher Barden, Donald F. Weaver

et al.

Journal of Medicinal Chemistry, Journal Year: 2021, Volume and Issue: 64(4), P. 1786 - 1815

Published: Feb. 11, 2021

Incorporation of heterocycles into drug molecules can enhance physical properties and biological activity. A variety heterocyclic groups is available to medicinal chemists, many which have been reviewed in detail elsewhere. Oxadiazoles are a class heterocycle containing one oxygen two nitrogen atoms, three isomeric forms. While the 1,2,4- 1,3,4-oxadiazoles seen widespread application chemistry, 1,2,5-oxadiazoles (furazans) less common. This Review provides summary furazan-containing chemistry development programs from analysis both patent academic literature. Emphasis placed on that reached clinical or preclinical stages development. The examples provided herein describe pharmacology activity furazan derivatives with comparative data where possible for other pharmacophores commonly used chemistry.

Language: Английский

Citations

44