Fused Imidazo[1,2‐d][1,2,4]Thiadiazolo[1,2,3]Triazoles: One‐Pot Synthesis, Anti‐Bacterial, Anti‐Biofilm and TLR4 Inhibitory Activities DOI Open Access

Karukuri Premalatha,

Mohammad Azam, Ravikumar Kapavarapu

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(32)

Published: Aug. 23, 2024

Abstract We developed and evaluated several new fused imidazo[1,2‐d][1,2,4]thiadiazolo[1,2,3]triazoles to see how they perform against bacteria biofilms. Some compounds showed acceptable activity compared the primary standard, Dicloxacillin. of demonstrated significant antibacterial S. aureus , with MIC values ranging from 1.56–12.5 μg/mL. also found anti‐biofilm properties in potent compounds. The results that derivatives 3‐(4‐fluorophenyl)imidazo[1,2‐d] [1,2,3] triazolo[1,5‐b][1,2,4]thiadiazole 8,8‐dioxide 3‐(3,5‐difluorophenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4] thiadiazole were strong agents effective MSSA MRSA biofilm growth inhibitors. conducted silico studies assess molecular interactions more TLR4 proteins (PDB: 3FXI, 3VQ1, 3RG1). Our findings revealed 3‐(4‐chloro‐3,5‐dimethoxyphenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b] [1,2,4]thiadiazole 8,8‐dioxide, 3‐(3,5‐dichlorophenyl)imidazo[1,2‐d] [1,2,3]triazolo[1,5‐b][1,2,4] 3‐(4‐(trifluoromethyl)phenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4] exhibited binding than dicloxacillin. ADME examined this study could potentially inhibit cytochrome P450 CYP2C19 isoform.

Language: Английский

Design, synthesis, and molecular modeling studies of novel 2-quinolone-1,2,3-triazole-α-aminophosphonates hybrids as dual antiviral and antibacterial agents DOI

Khadija El Gadali,

Meriem Rafya, Az‐Eddine El Mansouri

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 268, P. 116235 - 116235

Published: Feb. 16, 2024

Language: Английский

Citations

14
Synthesis of 1,2,3-triazole-piperazin-benzo[b][1,4]thiazine 1,1-dioxides: antibacterial, hemolytic and in silico TLR4 protein inhibitory activities DOI Creative Commons

N. Ramu,

Thupurani Murali Krishna, Ravikumar Kapavarapu

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(13), P. 8921 - 8931

Published: Jan. 1, 2024

Novel 1,2,3-triazoles (6a–6j & 8a–8g) were synthesized and evaluated for their antibacterial activity against S. aureus . The more potent compounds further in silico TLR4 inhibitory activity.

Language: Английский

Citations

7
An updated review on 1,2,3-/1,2,4-triazoles: synthesis and diverse range of biological potential DOI

Anirudh Pratap Singh Raman,

M. Aslam, Amardeep Awasthi

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: July 27, 2024

Language: Английский

Citations

7
Review of synthesis process of benzimidazole-heterocycle hybrid compounds DOI

Abouelhaoul El Alami,

Hamid Sdassi, Said Bouzikri

et al.

Synthetic Communications, Journal Year: 2024, Volume and Issue: 54(8), P. 613 - 635

Published: Feb. 16, 2024

Over the last few years, benzimidazole-heterocycle hybrid compounds have received considerable attention due to wide spectrum of their biological property and many important chemical pharmacological applications. These revealed antibacterial, antimicrobial, anticoagulant, antidiabetic other activities, they been used as drugs in market treat several diseases. Furthermore, heterocyclic possessing a benzimidazole skeleton exhibit significant complexing anticorrosive properties. All these applications favored development large number synthetic strategies prepare systems different reaction conditions. Many research articles on synthesis reported literature. In this review, we present discuss routes compounds.

Language: Английский

Citations

5
In Vitro and In Silico Studies on Benzimidazole‐Based Compounds DOI
Saad Bouchekioua, Senem Akkoç, Rafik Menacer

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(1)

Published: Jan. 4, 2024

Abstract Colon cancer remains a significant health concern, necessitating the synthesis of novel therapeutic agents. Benzimidazole derivatives have shown promising anticancer potential. In this study, two benzimidazole were synthesized, and their antiproliferative activities investigated in vitro against human colon colorectal cell line normal lung fibroblast line. The viability revealed that molecule 3 had high activity inhibited growth DLD‐1 cells for 48 h. Furthermore, was found to more selectivity Computational calculations performed predict molecular properties molecules using B3LYP/6‐311++(2d,2p) density functional theory level. quantum atoms (QTAIM) energy decomposition analysis (EDA) utilized investigate nature interatomic bonding existing among studied molecules. ultraviolet‐visible (UV–vis) results calculated time‐dependent density‐functional (TD‐DFT). chemical reactivity stability also by DFT computational analysis. docking dynamics simulations conducted, reveal concordance with experimental results. Molecule has better anti‐cancer targets (PDB ID: 2HQ6) compared 2 .

Language: Английский

Citations

4
Synthesis of novel quinoline-thiazolobenzimidazolone hybrids as anticancer agents through caspase-dependent apoptosis DOI

Houria Bouria,

Hayette Alliouche, Mohamed Imed Chouiter

et al.

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 13

Published: Feb. 26, 2025

Aim This work explores the synthesis of new bi-heterocyclic hybrid compounds based on quinoline ring and investigates their potential as anticancer agents.

Language: Английский

Citations

0
Quinoline-1,2,3-triazole hybrids: Design, synthesis, antimalarial and antimicrobial evaluation DOI
Jyoti Yadav, C. P. Kaushik

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1316, P. 138882 - 138882

Published: June 20, 2024

Language: Английский

Citations

3
Microwave-assisted Click Synthesis, Characterisation, and In silico Studies of novel 2H-chromene-1,2,3-triazolyl glycoconjugates as Potent Anticancer and Antibacterial agents DOI
Bhabani Shankar Panda, Mohammed Ansar Ahemad,

Suhasini Mohapatra

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1318, P. 139323 - 139323

Published: July 17, 2024

Language: Английский

Citations

3
Benzimidazole–Oxadiazole Hybrids—Development in Medicinal Chemistry: An Overview DOI

Raveendra Bhat,

Venkatraman Hegde, Srinivasa Budagumpi

et al.

Chemical Biology & Drug Design, Journal Year: 2024, Volume and Issue: 104(2)

Published: Aug. 1, 2024

To increase the success rate of drug discovery, one practical strategy is to begin molecular hybridisation. The presence two or more pharmacophores in a single unit leads pharmacological potency greater than sum each individual moiety's potency. Heterocyclic compounds are very widely distributed nature and essential for life activities. Benzimidazole oxadiazole privileged structures medicinal chemistry used discovery development due their vast biological properties. drug-like properties (like pharmacokinetics pharmacodynamics) scaffolds can be improved by benzimidazole-oxadiazole chimeric molecules via hybridisation approach. cores either fused incorporated using functional groups/bonds. Over last few decades, scientists have predicted that these moieties could interconnected yield novel modified hybrid compound. hybrids were identified as most potent anticancer, antimicrobial, anti-inflammatory, antioxidant, anticonvulsant, antidepressant, antihypertensive antitubercular agents. In this context, present review describes (1,3,4 1,2,4) hybrids, possible structure-activity relationship mechanism action studies presented. This article intended stimulate fresh ideas search rational designs active less toxic prospective therapeutic candidates, well effective diagnostic agents pathologic probes.

Language: Английский

Citations

1
Fused Imidazo[1,2‐d][1,2,4]Thiadiazolo[1,2,3]Triazoles: One‐Pot Synthesis, Anti‐Bacterial, Anti‐Biofilm and TLR4 Inhibitory Activities DOI Open Access

Karukuri Premalatha,

Mohammad Azam, Ravikumar Kapavarapu

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(32)

Published: Aug. 23, 2024

Abstract We developed and evaluated several new fused imidazo[1,2‐d][1,2,4]thiadiazolo[1,2,3]triazoles to see how they perform against bacteria biofilms. Some compounds showed acceptable activity compared the primary standard, Dicloxacillin. of demonstrated significant antibacterial S. aureus , with MIC values ranging from 1.56–12.5 μg/mL. also found anti‐biofilm properties in potent compounds. The results that derivatives 3‐(4‐fluorophenyl)imidazo[1,2‐d] [1,2,3] triazolo[1,5‐b][1,2,4]thiadiazole 8,8‐dioxide 3‐(3,5‐difluorophenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4] thiadiazole were strong agents effective MSSA MRSA biofilm growth inhibitors. conducted silico studies assess molecular interactions more TLR4 proteins (PDB: 3FXI, 3VQ1, 3RG1). Our findings revealed 3‐(4‐chloro‐3,5‐dimethoxyphenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b] [1,2,4]thiadiazole 8,8‐dioxide, 3‐(3,5‐dichlorophenyl)imidazo[1,2‐d] [1,2,3]triazolo[1,5‐b][1,2,4] 3‐(4‐(trifluoromethyl)phenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4] exhibited binding than dicloxacillin. ADME examined this study could potentially inhibit cytochrome P450 CYP2C19 isoform.

Language: Английский

Citations

1