Synthesis and Molecular Docking of novel 1,3-Thiazole Derived 1,2,3-Triazoles and In vivo Biological Evaluation for their Anti anxiety and Anti inflammatory Activity

Ankali, Kariyappa N; Rangaswamy, Javarappa; Shalavadi, Mallappa; Naik, Nagaraja; Krishnamurthy, G.

doi:10.1016/j.molstruc.2021.130357

Cited by 25 publications

(7 citation statements)

References 30 publications

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“…The 1,2,3‐triazole is one of the prominent scaffolds used for the development of the active compounds [24–27] . 1,2,3‐Triazole‐containing compounds received more attention due to their varied biological activities such as antifungal, [28–34] antimicrobial, [35,36] antivirals, [37,38] antimalarial, [39,40] anticancer [41–43] and anti‐inflammatory activities [44,45] . The isoxazole containing natural and synthetic compounds reported for a wide range of biological activities such as antimicrobial, [46,47] antibacterial, [48–50] antifungal, [51,52] antitubercular, [16,53–55] antiviral, [56,57] anticancer, [58–60] and anti‐inflammatory [61–63] …”

Section: Introductionmentioning

confidence: 99%

An Efficient Synthesis, Antimicrobial Evaluation and In Silico Studies of 1,2,3‐Triazolyl‐isoxazolyl‐ethanol Derivatives

Bhoye,

Latif Shaikh,

Walunj

et al. 2024

ChemistrySelect

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A series of 2‐(1‐substituted benzyl‐1H‐1,2,3‐triazol‐4‐yl)‐1‐(5‐arylisoxazol‐3‐yl)ethanol (8 a–p) have been designed and efficiently synthesized. The structure of the compounds 8 a–p was characterized by spectral methods. The newly synthesized 1,2,3‐triazolyl‐isoxazolyl‐ethanol (8 a–p) derivatives were evaluated for in vitro antimicrobial activity against P. mirabilis, E. coli, S. albus, B. subtilis, C. albicans and A. niger. Eleven derivatives showed good activity against the Gram‐negative strains. Compounds 8 b, 8 c, 8 d, 8 g, 8 h, 8 i, 8 j, 8 k, 8 n, 8 o, and 8 p showed good antibacterial against E. coli activity. Against P. mirabilis, compounds 8 a, 8 b, 8 d, 8 g, 8 h, 8 k, 8 l, 8 m, 8 n, 8 o, and 8 p showed good activity, compounds 8 o, and 8 p showed two‐fold less activity than the reference drug streptomycin. Against the Gram‐positive strain, B. subtilis, compounds 8 c, 8 d and 8 f showed good activity, from which the compounds 8 d and 8 f were found only two‐fold less potent than the reference drug streptomycin. Against fungal strains, C. albicans, compound 8 g and against A. niger, compounds 8 f, 8 h and 8 j showed good antifungal activity. Against A. niger strain, the compounds 8 f and 8 h reported only two‐fold less activity than the reference drug fluconazole. The active compounds were studied for molecular docking and molecular dynamics simulations.

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Section: Introductionmentioning

confidence: 99%

An Efficient Synthesis, Antimicrobial Evaluation and In Silico Studies of 1,2,3‐Triazolyl‐isoxazolyl‐ethanol Derivatives

Bhoye,

Latif Shaikh,

Walunj

et al. 2024

ChemistrySelect

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“…38 In this review, we elucidate contemporary strides in the synthetic methodology for the synthesis of thiazolyl-pyrazoline and thiazolyl-pyrazole hybrids employing phenacyl bromides as an emerging precursor. The resulting hybrids exhibit diverse pharmaceutical applications such as anticancer, 39 antibacterial, 40 antiinflammatory, 41 antifungal, 42 antitubercular, 43 anticonvulsant, 44 antioxidant, 45 antiviral, 46 etc. (Figure 3).…”

Section: Introductionmentioning

confidence: 99%

Development in the Synthesis of Bioactive Thiazole-Based Heterocyclic Hybrids Utilizing Phenacyl Bromide

Kumari,

Dhillon,

Rani

et al. 2024

ACS Omega

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Heterocyclic hybrid frameworks represent a burgeoning domain within the realms of drug discovery and medicinal chemistry, attracting considerable attention in recent years. Thiazole pharmacophore fragments, inherent in natural products such as peptide alkaloids, metabolites, and cyclopeptides, have demonstrated a broad spectrum of pharmacological potentials. Given their profound biological significance, a plethora of thiazole-based hybrids have been synthesized through the conjugation of thiazole moieties with bioactive pyrazole and pyrazoline fragments. This review systematically presents a compendium of robust methodologies for the synthesis of thiazole-linked hybrids, employing the (3 + 2) heterocyclization reaction, specifically the Hantzsch-thiazole synthesis, utilizing phenacyl bromide as the substrate. The strategic approach of molecular hybridization has markedly enhanced drug efficacy, mitigated resistance to multiple drugs, and minimized toxicity concerns. The resultant thiazole-linked hybrids exhibit a myriad of medicinal properties viz. anticancer, antibacterial, anticonvulsant, antifungal, antiviral, and antioxidant activities. This compilation of methodologies and insights serves as a valuable resource for medicinal chemists and researchers engaged in the design of novel thiazole-linked hybrids endowed with therapeutic attribute.

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“…35 Some of the natural products such as spirotryprostatin A, spirotryprostatin B and horsifiline are based on the spiropyrrolidine-oxindole framework. The fascinating array of pharmacological properties such as antimicrobial, 36 anticancer, 37 antitubercular, 38,39 anti-HIV, 40 b-lactamase inhibition, 41 antidiabetic activity, 42,43 anti-proliferative 44 and anti-inflammatory 45 associated with 1,2,3-triazoles has attracted medicinal chemists to explore this structural framework in the development of novel pharmacophores.…”

Section: Introductionmentioning

confidence: 99%

Thiazolidine-2,4-dione framework containing spiropyrrolidine-oxindole and 1,2,3-triazole scaffold: synthesis, in vitro α-amylase inhibition and in silico studies

et al. 2023

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Synthesis and Molecular Docking of novel 1,3-Thiazole Derived 1,2,3-Triazoles and In vivo Biological Evaluation for their Anti anxiety and Anti inflammatory Activity

Cited by 25 publications

References 30 publications

An Efficient Synthesis, Antimicrobial Evaluation and In Silico Studies of 1,2,3‐Triazolyl‐isoxazolyl‐ethanol Derivatives

An Efficient Synthesis, Antimicrobial Evaluation and In Silico Studies of 1,2,3‐Triazolyl‐isoxazolyl‐ethanol Derivatives

Development in the Synthesis of Bioactive Thiazole-Based Heterocyclic Hybrids Utilizing Phenacyl Bromide

Thiazolidine-2,4-dione framework containing spiropyrrolidine-oxindole and 1,2,3-triazole scaffold: synthesis, in vitro α-amylase inhibition and in silico studies

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