Synthesis and in vitro Antidiabetic Screening of Novel Dihydropyrimidine Derivatives

Lalpara, Jaydeep N.; Vachhani, M. D.; Hadiyal, Sanjay D.; Goswami, Swati; Dubal, G. G.

doi:10.1134/s1070428021020159

Cited by 19 publications

(5 citation statements)

References 12 publications

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“…33 Another study by Karrouchi et al 36 synthesized a new chiral pyrazole derivative having α-glucosidase and α-amylase enzyme inhibitory actions. For the synthesis (Figure 7), ethyl-2,4-dioxopentanoate 28 was refluxed with isoniazid 37 to produce ethyl-5-hydroxy-1-isonicotinoyl-3-methyl-4,5-dihydro-1H-pyrazole-5-carboxylate. 38 This compound showed in-vitro antidiabetic activity and the molecular studies revealed its interaction with Gln298, Lys254, Leu639, Lys643, Leu638, and Ile300 at the active site of α-glucosidase (PDB ID:4XP0), and with Val382, Gly383, and Ala400 at the active site of α-amylase (PDB ID:2QPU).…”

Section: Pyrazolementioning

confidence: 99%

“…Another study by Karrouchi et al 36 synthesized a new chiral pyrazole derivative having α‐glucosidase and α‐amylase enzyme inhibitory actions. For the synthesis (Figure 7), ethyl‐2,4‐dioxopentanoate 28 was refluxed with isoniazid 37 to produce ethyl‐5‐hydroxy‐1‐isonicotinoyl‐3‐methyl‐4,5‐dihydro‐1 H ‐pyrazole‐5‐carboxylate 38 …”

Section: Five‐membered Ring Natural Heterocyclicsmentioning

confidence: 99%

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Advancement in chiral heterocycles for the antidiabetic activity

Gupta,

Rani,

Nainwal

et al. 2024

Chirality

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For the synthesis and development of pharmaceuticals, chirality is an important structural component. Chiral heterocyclic compounds have annoyed the interest of synthetic chemists who are working to create useful and efficient techniques for these molecules. As indicated by the expanding number of chiral drugs created in the last two decades, the link between chirality and pharmacological activity has become more important in the pharmaceutical and biopharmaceutical industries. Approximately 65% of currently used drugs are chiral, and many of them are promoted as racemates in many circumstances. There are a growing number of new chiral heterocyclic compounds with important biological properties and intriguing uses in medical chemistry and drug discovery. In this study, we review current breakthroughs in chiral heterocycles and their different physiological activities that have been published in the last year (from 2010 to early 2023). This study focuses on the current trends in the use of chiral heterocycles in drug design and the creation of several powerful and competent candidates for diabetic illnesses.

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Section: Pyrazolementioning

confidence: 99%

Section: Five‐membered Ring Natural Heterocyclicsmentioning

confidence: 99%

Advancement in chiral heterocycles for the antidiabetic activity

Gupta,

Rani,

Nainwal

et al. 2024

Chirality

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“…Among the derivatives, compound 10 exhibited good inhibition compared to that of the standard drug acarbose. [ 92 ] In an endeavor to find an antidiabetic drug, Bairagi et al synthesized, purified, and characterized a series of ethyl or methyl 4‐(hydroxyphenyl)‐6‐methyl‐2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidine‐5‐carboxylate derivatives using NMR ( 1 H and 13 C) and FTIR spectroscopy. The compounds were tested for antihyperglycemic action in a diabetic rat model induced by streptozotocin (STZ).…”

Section: Biological Applicationsmentioning

confidence: 99%

Catalytic role in Biginelli reaction: Synthesis and biological property studies of 2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidines

Kamat

Reddy

Kumar

2023

Archiv der Pharmazie

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The Biginelli reaction has received significant consideration in recent years due to its easily accessible aldehyde, urea/thiourea, and active methylene compounds. When it comes to pharmacological applications, the Biginelli reaction end‐products, the 2‐oxo‐1,2,3,4‐tetrahydropyrimidines, are vital in pharmacological applications. Due to the ease of carrying out the Biginelli reaction, it offers a number of exciting prospects in various fields. Catalysts, however, play an essential role in Biginelli's reaction. In the absence of a catalyst, it is difficult to form products with a good yield. Many catalysts have been used in search of efficientmethodologies, including biocatalysts, Brønsted/Lewis acids, heterogeneous catalysts, organocatalysts, and so on. Nanocatalysts are currently being applied in the Biginelli reaction to improve the environmental profile as well as speed up the reaction process. This review describes the catalytic role in the Biginelli reaction and pharmacological application of 2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidines. This study provides information that will facilitate the development of newer catalytic methods for the Biginelli reaction, by academics as well as industrialists. It also offers a broad scope for drug design strategies, which may enable the development of novel and highly effective bioactive molecules.

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“…An increase in the lipophilic chain is a key factor to improve the bioavailability of molecules in the body protein. Mainly our focus and contribution to medicinal chemistry are to design and develop antidiabetic, anticancer, antioxidant, and antimicrobial agents [14][15][16][17][18][19][20][21].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, SAR, Pharmacokinetic Prediction of New 4-Quinolones as Anti-Microbial Agents

Dubal

Vachchharajani²,

Solanki³

et al. 2022

Russ J Gen Chem

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A series of new 4-quinolone derivatives was synthesized by conventional heating method. For the synthesized compounds, we performed pharmacokinetic prediction, SAR and antimicrobial assay. The presence of halogen elements plays a key role in the biological activity that is clear by in vitro analysis. Target compounds exhibit moderate to significant activity near to standard marketed drugs like amoxycillin, chloramphenicol, ciprofloxacin, norfloxacin, griseofulvin, and nystatin.

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Synthesis and in vitro Antidiabetic Screening of Novel Dihydropyrimidine Derivatives

Cited by 19 publications

References 12 publications

Advancement in chiral heterocycles for the antidiabetic activity

Advancement in chiral heterocycles for the antidiabetic activity

Catalytic role in Biginelli reaction: Synthesis and biological property studies of 2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidines

Design, Synthesis, SAR, Pharmacokinetic Prediction of New 4-Quinolones as Anti-Microbial Agents

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