Biological Activity of Quinazolinones

Radwan, A E; Alanazi, Fars K.

doi:10.5772/intechopen.90621

Cited by 17 publications

(13 citation statements)

References 104 publications

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“…To date, several investigations have been reported on the biological activities of quinazoline analogues such as fungicidal, antileishmanial, antitrauma activities, antiviral, antitumour, and antibacterial 69–73 . Quinazolines are also used in agrochemical and pharmaceutical industries 67,74 …”

Section: Medicinal Chemistry Approach For Drug Discovery Against Acanthamoebamentioning

confidence: 99%

“…In medicinal chemistry, the quinazoline class of heterocyclic compounds represents a potential platform against several diseases 67,68 . To date, several investigations have been reported on the biological activities of quinazoline analogues such as fungicidal, antileishmanial, antitrauma activities, antiviral, antitumour, and antibacterial 69–73 .…”

Section: Medicinal Chemistry Approach For Drug Discovery Against Acan...mentioning

confidence: 99%

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Applications of medicinal chemistry for drug discovery against Acanthamoeba infections

Ahmed

Anwar

Ong

et al. 2021

Medicinal Research Reviews

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Acanthamoeba is a genus of free‐living amoebae, pervasively found in the environment. Most of its pathogenic species are the causative agent of sight‐threatening Acanthamoeba keratitis and fatal granulomatous amoebic encephalitis. Despite the advancements in the field of chemotherapy, treating Acanthamoeba infections is still challenging due to incomplete knowledge of the complicated pathophysiology. In case of infection, the treatment regimen for the patients is often ineffective due to delayed diagnosis, poor specificity, and side‐effects. Besides the resistance of Acanthamoeba cysts to most of the drugs, the recurrence of infection further complicates the recovery. Thus, it is necessary to develop an effective treatment which can eradicate these rare, but serious infections. Based on various computational and in vitro studies, it has been established that the synthetic scaffolds such as heterocyclic compounds may act as potential drug leads for the development of antiamoebic drugs. In this review, we report different classes of synthetic compounds especially heterocyclic compounds which have shown promising results against Acanthamoeba. Moreover, the antiamoebic activities of synthetic compounds with their possible mode of actions against Acanthamoeba, have been summarized and discussed in this review.

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Section: Medicinal Chemistry Approach For Drug Discovery Against Acanthamoebamentioning

confidence: 99%

Section: Medicinal Chemistry Approach For Drug Discovery Against Acan...mentioning

confidence: 99%

Applications of medicinal chemistry for drug discovery against Acanthamoeba infections

Ahmed

Anwar

Ong

et al. 2021

Medicinal Research Reviews

View full text Add to dashboard Cite

show abstract

“…Among them, 2-[(3-iodobenzyl)thio]quinazolin-4-one found to be most effective (26). [38] Studies were also done on various heterocyclic ring on sulfur like piperazine to determine the MAO inhibitory activity (27). [39]…”

Section: Antidiabetic Activity -α-Glucosidase Inhibitormentioning

confidence: 99%

Untitled

2021

IJMS

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Heterocyclic chemistry being an important branch of chemistry includes many ring structures with heteroatoms such as nitrogen, oxygen, and sulfur. Quinazoline is an important nitrogen containing benzofused heterocycle and has several therapeutic actions such as antimalarial, antimicrobial, anticancer, and anticonvulsant. Quinazoline was first isolated from alkaloid vasicine. Vasicine, deoxyvasicine, tryptanthrin, and rutecarpine are some of the potent naturally occurring quinazolines. Substitutions on different positions of quinazoline ring lead to different activities. Detailed survey of activities of quinazoline such as anticancer, anticonvulsant, antifungal, antibacterial, and antidiabetic according to structure-activity relationship and marketed preparations containing quinazoline as an active moiety is described in this review.

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“…Quinazolin-4(3H)-ones are an important class of biologically active molecules [1] which show anticancer, antimalarial, antiviral, anticonvulsant, analgesic, anti-inflammatory and antimicrobial activity. [2] Different synthetic routes were used for their preparation and the reaction sequences employed in synthesis of 2-amino-quinazolin-4(3H)-ones starting from readily available aromatic amines which include Me 3 SiCl [3] and CDI [4] catalyzed reactions are depicted in Scheme 1. All these routes employ thermal conversion of guanidine to heterocycle as the key reaction step [5] and the authors realized the advantageous use of microwave (MW) heating as the method of thermal activation.…”

Section: Introductionmentioning

confidence: 99%

Consecutive Utilization of Mechanochemical and Microwave Methods for the Synthesis of Boc‐2‐amino‐quinazolin‐4(3H)‐ones and DFT Study of Mechanism 6π‐Diazaelectrocyclization Process

et al. 2022

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Two eco‐friendly synthetic methods were used consecutively in the preparation of quinazolin‐4(3H)‐one heterocycles. The first reaction step, synthesis of a series of aryl guanidines was carried out by solvent‐free mechanochemical milling of aryl amines with 1H‐pyrazole‐N,N‐di‐(tert‐butyloxycarbonyl)‐1‐carboxamidine. In the following synthetic step, aryl guanidines were converted into Boc‐2‐amino‐quinazolin‐4(3H)‐ones by microwave heating. The experimental studies were supplemented by detailed quantum chemical studies (DFT) of the reaction mechanism of 6π‐diazaelectrocyclization process, and the predicted reactivities and regioselectivities are consistent with the experimental observations.

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Biological Activity of Quinazolinones

Cited by 17 publications

References 104 publications

Applications of medicinal chemistry for drug discovery against Acanthamoeba infections

Applications of medicinal chemistry for drug discovery against Acanthamoeba infections

Untitled

Consecutive Utilization of Mechanochemical and Microwave Methods for the Synthesis of Boc‐2‐amino‐quinazolin‐4(3H)‐ones and DFT Study of Mechanism 6π‐Diazaelectrocyclization Process

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