Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea

Kashaw, Sushil K.; Kashaw, Varsha; Mishra, Pradeep; Jain, Neha; Stables, James P.

doi:10.1016/j.ejmech.2009.05.008

Cited by 129 publications

(62 citation statements)

References 10 publications

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“…It has been observed that they possess anticancer [1–5], antibacterial [6, 7], antifungal [7, 8], antitubercular [9, 10], antiviral [11, 12], anticoccidial [13, 14], anti-inflammatory and analgesics [15–21], antidepressant [22–24], anticonvulsant [23, 24], antimalarial [25, 26], antioxidant [27], antileishmanial [28], neuroprotective [29], antiobesity [30], antihypertensive [31], anti-H 1 -antihistaminic [32], and antiprotozoal activities [33]. The quinazoline moiety is a core unit in a variety of drugs such as Alfuzosin, Nolatrexed, CS 1101 (CAL 101), Balaglitazone, Milciclib, and Letermovir (Fig.…”

Section: Introductionmentioning

confidence: 99%

Molecular docking and biological evaluation of some thioxoquinazolin-4(3H)-one derivatives as anticancer, antioxidant and anticonvulsant agents

Al-Shamary

Al-Alshaikh

Kheder

et al. 2017

Chemistry Central Journal

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BackgroundThe quinazoline are an important class of medicinal compounds that possess a number of biological activities like anticancer, anticonvulsant and antioxidant etc.ResultsWe evaluated the previously synthesized quinazoline derivatives 1–3 for their anticancer activities against three cancer cell lines (HepG2, MCF-7, and HCT-116). Among the tested compounds, quinazolines 1 and 3 were found to be more potent than the standard drug Vinblastine against HepG2 and MCF-7 cell lines. All the tested compounds had less antioxidant activity and did not exhibit any anticonvulsant activity. Also, molecular docking studies were performed to get an insight into the binding modes of the compounds with human cyclin-dependent kinase 2, butyrylcholinesterase enzyme, human gamma-aminobutyric acid receptor. These compounds showed better docking properties with the CDK2 as compared to the other two enzymes.ConclusionsThe overall study showed that thioxoquinazolines are suitable antitumor agents and they should be explored for other biological activities. Modification in the available lot of quinazoline and synthesis of its novel derivatives is essential to explore the potential of this class of compounds. The increase in the threat and with the emergence of drug resistance, it is important to explore and develop more efficacious drugs.

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Section: Introductionmentioning

confidence: 99%

Molecular docking and biological evaluation of some thioxoquinazolin-4(3H)-one derivatives as anticancer, antioxidant and anticonvulsant agents

Al-Shamary

Al-Alshaikh

Kheder

et al. 2017

Chemistry Central Journal

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“…Most importantly, isatoic anhydrides serves the role of intermediate in the synthesis of a variety of heterocyclic compounds, such as quinazolinones, quinazolones, benzimidazolones, phthalimides, pyrroloquinazolones, quinazolinediones, in addition to its use in the fluorescent labeling of mRNA and tRNA [6–9]. Among the various heterocycles derived from ISA, quinazolones are the most prominent due to their various biological effects including antihypertensive [10], antimicrobial [11–13], antihyperlipidemic [14,15], antioxidant [16], anti-inflammatory [17–19], anticonvulsant [20,21], and anticancer activities [22–25]. …”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of 2-Aminobenzamide Derivatives as Antimicrobial Agents: Opening/Closing Pharmacophore Site

Mabkhot

Al‐Majid

Barakat

et al. 2014

IJMS

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A series of new 2-aminobenzamide derivatives (1–10) has been synthesized in good to excellent yields by adopting both conventional and/or a time-efficient microwave assisted methodologies starting from isatoic anhydride (ISA) and characterized on the basis of their physical, spectral and microanalytical data. Selected compounds of this series were then tested against various bacterial (Bacillus subtilis (RCMB 000107) and Staphylococcus aureus (RCMB 000106). Pseudomonas aeruginosa (RCMB 000102) and Escherichia coli (RCMB 000103) and fungal strains (Saccharomyces cerevisiae (RCMB 006002), Aspergillus fumigatus (RCMB 002003) and Candida albicans (RCMB 005002) to explore their potential as antimicrobial agents. Compound 5 was found to be the most active compound among those tested, which showed excellent antifungal activity against Aspergillus fumigatus (RCMB 002003) more potent than standard Clotrimazole, and moderate to good antibacterial and antifungal activity against most of the other strains of bacteria and fungi. Furthermore, potential pharmacophore sites were identified and their activity was related with the structures in the solution.

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“…In the family of heterocyclic compounds, nitrogen-containing heterocycles are considered to be an important class of compounds because of their interesting diversified biological properties. One of the most frequently encountered heterocycles in medicinal chemistry is quinazolin-4(3H)-one with widespread applications as antibacterial (Gupta et al, 2008), antifungal (Bartroli et al, 1998), analgesic, anti-inflammatory (Alafeefy et al, 2008), antitubercular, anticancer (Raghavendra et al, 2007), antiviral (Selvam et al,2008), anticonvulsant (Micale et al, 2006), CNS depressant (Kashaw et al, 2009), and antihyperglycemic (Ram et al, 2003) therapeutic agent. Among different heterocyclic systems five-member heterocycles represent a class of compounds of biological significance.…”

Section: Introductionmentioning

confidence: 99%

In vitro evaluation of the antibacterial and antifungal activity of some new pyrazolyl-quinazolin-4(3H)-one derivatives

Patel

Barat

2010

Med Chem Res

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Several pyrazolyl-quinazolin-4(3H)-ones 6a-m were synthesized by the cyclization of acrylamides 5a-m with hydrazine hydrate. The overall reaction was carried out by multi step process. The base-catalyzed cyclization of acid chloride 1 with 5-iodo anthranilic acid yielded benzoxazinone 2, which on reaction with hydrazine hydrate afforded amino quinazolin-4(3H)-one 3. The acrylamides 5a-m were easily synthesized by acetylation and then condensation with aromatic aldehyde of quinazolin-4(3H)-one 3. The structural confirmation of the synthesized compounds was carried out on the basis of elemental analyses as well as IR and NMR spectral results. The title compound 6a-m was evaluated for antibacterial and antifungal activity in vitro.

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Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea

Cited by 129 publications

References 10 publications

Molecular docking and biological evaluation of some thioxoquinazolin-4(3H)-one derivatives as anticancer, antioxidant and anticonvulsant agents

Molecular docking and biological evaluation of some thioxoquinazolin-4(3H)-one derivatives as anticancer, antioxidant and anticonvulsant agents

Synthesis and Biological Evaluation of 2-Aminobenzamide Derivatives as Antimicrobial Agents: Opening/Closing Pharmacophore Site

In vitro evaluation of the antibacterial and antifungal activity of some new pyrazolyl-quinazolin-4(3H)-one derivatives

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