An Overview on Biological Evaluation of Tetrazole Derivatives

Kabi, Arup K.; Sravani, Sattu; Gujjarappa, Raghuram; Garg, Aakriti; Vodnala, Nagaraju; Tyagi, Ujjawal; Kaldhi, Dhananjaya; Ravichandiran, V.; Singh, Virender; Gupta, Shikhar; Malakar, Chandi C.

doi:10.1007/978-981-16-8399-2_8

Cited by 12 publications

(6 citation statements)

References 82 publications

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“…Thiazole and related substituted derivatives have been widely employed as physiologically active chemicals in sulphur medicines. [262][263][264][265] For the synthesis of 2-aminothiazoles, a few organocatalysts have been employed, [266] including NEt 3 (Scheme 26 (a)), and asparagine (Scheme 26 (b)). [267,268] In a recent study, the aluminium oxide nanoparticles were prepared using a two-step process involving the grafting of 3chloropropyltrimethoxysilane onto Al 2 O 3 and subsequent functionalization with asparagine (Scheme 26 (c)).…”

Section: Csp 2 à S Bond Formationmentioning

confidence: 99%

Iodine and DMSO as Surrogate of Hazardous Metal and Non‐Metal Reagents in Organic Synthesis

Reetu,

Kalita,

Dash

et al. 2024

ChemistrySelect

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Organic synthesis involves the production of important chemical structures using scalable and cost‐effective methods that are also environmentally friendly. In this review, a detailed analysis of the use of iodine and DMSO in various synthetic routes for the preparation of valuable targets are presented. These methods reduce the acceptance on expensive additives and reagents, and offer a more sustainable solution for the synthesis of these important chemical scaffolds.

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Section: Csp 2 à S Bond Formationmentioning

confidence: 99%

Iodine and DMSO as Surrogate of Hazardous Metal and Non‐Metal Reagents in Organic Synthesis

Reetu,

Kalita,

Dash

et al. 2024

ChemistrySelect

Self Cite

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“…Studies demonstrated that VT-1161 has greater specificity against fungal cytochrome over the human one. 35,36 VT-1129 and VT-1598 are two more tetrazole-based molecules in the preclinical phase. 37,38 Apart from azoles, polyenes have also been used extensively as primary fungicidal agents against species of Aspergillus, Candida, and Cryptococcus since their discovery in the 1950s (Fig.…”

Section: Clinically Used Antifungal Agentsmentioning

confidence: 99%

Section: Clinically Used Antifungal Agentsmentioning

confidence: 99%

Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance

Mehta¹,

Saini²,

Bajaj³

2023

RSC Med. Chem.

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“…The immense importance of heterocycles in medicinal chemistry and drug‐discovery research has been broadly witnessed during the past decades [1a–e] . The heterocycles are present in a wide range of naturally occurring products and other biologically active substances.…”

Section: Introductionmentioning

confidence: 99%

Cu‐Catalyzed Synthesis of 4H‐benzo[4,5]thiazolo[3,2‐a]pyrimidin‐4‐ones: Molecular Docking Studies and Anti‐Proliferative Activities Against HepG2 Hepatocellular Carcinoma Cells

Aljaar,

Aboalrub,

Shtaiwi

et al. 2024

Asian J Org Chem

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The copper‐catalyzed regioselective domino synthesis of 4H‐benzo[4,5]thiazolo[3,2‐a]pyrimidin‐4‐ones 3 through N,S‐arylation strategies has been accomplished. This transformation was operated by the reaction of 1‐bromo‐2‐iodobenzenes 1 with 2‐thioxo‐2,3‐dihydropyrimidin‐4(1H)‐ones 2 in the presence of trans‐4‐hydroxy‐L‐proline as a ligand in DMSO as a solvent. Using this method, a library of diversely functionalized 4H‐benzo[4,5]thiazolo[3,2‐a]pyrimidin‐4‐one derivatives 3 were obtained in yields ranging 66‐85%. The described process revealed a very good tolerance to substituents on both 1‐bromo‐2‐iodobenzenes 1 and 2‐thioxo‐2,3‐dihydropyrimidin‐4(1H)‐ones 2. In addition, the reaction with 1,2‐diodobenzene yielded the corresponding 2‐methyl‐4H‐benzo[4,5]thiazolo[3,2‐a]pyrimidin‐4‐one (3a) in 70% yield. Docking studies explained that the derivatives 3h, 3e, and 3p bind to the lipophilic pocket of the phosphoinositide 3‐kinase beta (PI3Kβ) and epidermal growth factor receptor (EGFR) with high affinities. In addition, the complex 3h‐4bfr formed a very stable complex with PI3Kβ with the lowest binding free energy of ‐7.89 kcal/mol. The anti‐proliferative activity against HepG2 hepatocellular carcinoma cells was evaluated using MTT assay. The compound 3h exhibited cytotoxic activity against HepG2 cells comparable to that of Erlotinib, a standard EGFR inhibitor (IC50 values of 19.1 and 14.7 µM). Four of the tested compounds (3e, 3f, 3o, and 3p) showed moderate anti‐proliferative activities (IC50 values of 53.9 to 92.2 µM).

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An Overview on Biological Evaluation of Tetrazole Derivatives

Cited by 12 publications

References 82 publications

Iodine and DMSO as Surrogate of Hazardous Metal and Non‐Metal Reagents in Organic Synthesis

Iodine and DMSO as Surrogate of Hazardous Metal and Non‐Metal Reagents in Organic Synthesis

Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance

Cu‐Catalyzed Synthesis of 4H‐benzo[4,5]thiazolo[3,2‐a]pyrimidin‐4‐ones: Molecular Docking Studies and Anti‐Proliferative Activities Against HepG2 Hepatocellular Carcinoma Cells

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