ChemInform Abstract: Synthesis, Anticonvulsant and Toxicity Screening of Newer Pyrimidine Semicarbazone Derivatives.

Alam, Ozair; Mullick, Pooja; Verma, Surajpal; Gilani, Sadaf Jamal; Khan, Samia; Siddiqui, Nadeem; Ahsan, Waquar

doi:10.1002/chin.201040218

Cited by 2 publications

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“…Substituted 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) [24] bearing variable substitution patterns exhibit interesting multifaceted (calcium channel modulators, [25] antihypertensive agents, [26] adrenergic receptor antagonists, [27] mitotic kinesin Eg5 inhibitors, [28] and hepatitis B replication inhibitors [29] ) pharmacological profiles. Furthermore, the batzelladine alkaloids A isolated from marine sources containing a DHPM core inhibit the binding of HIV [30] envelop protein gp-120 to human CD4 cells, making them potential new leads for AIDS therapy.…”

Section: Introductionmentioning

confidence: 99%

Quinoline‐Dihydropyrimidin‐2(1H)‐one Hybrids: Synthesis, Biological Activity, and Mechanistic Studies

et al. 2022

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A novel class of quinoline-dihydropyrimidin-2(1H)-one (DHPM) hybrids was synthesized and in vitro antiplasmodial activity was evaluated against chloroquine sensitive (D10) and chloroquine resistant (Dd2) strains of Plasmodium falciparum, the human malaria parasite. The antiplasmodial activity was compared to previously reported DHPM based molecular hybrids. Dual mode of antiplasmodial action of the most active member has been evaluated through heme binding study and in silico docking in the active site of dihydrofolate enzymes (wild-type as well as mutant). Favourable pharmacokinetic parameters were pre-dicted in the ADMET evaluation. The new hybrids were also tested against a number of DNA and RNA viruses. No antiviral activity was found, except for one hybrid that showed mild inhibitory activity against two strains of cytomegalovirus (AD-169 and Davis), The most active hybrid was found to be a selective inhibitor of the growth of P. falciparum as well as a modest inhibitor of varicella zoster virus in HEL cells. Cytotoxicity of all hybrids was assessed in HEL, HeLa, Vero, MDCK, and CRFK cell cultures.

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Section: Introductionmentioning

confidence: 99%

Quinoline‐Dihydropyrimidin‐2(1H)‐one Hybrids: Synthesis, Biological Activity, and Mechanistic Studies

et al. 2022

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An overview of structurally diversified anticonvulsant agents

Alotaibi

2019

Acta Pharmaceutica

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There are several limited approaches to treat epilepsy in hospitals, for example, using medicines, surgery, electrical stimulation and dietary interventions. Despite the availability of all these new and old approaches, seizure is particularly difficult to manage. The quest for new antiepileptic molecules with more specificity and less CNS toxicity continues for medicinal chemists until a new and ideal drug arrives. This review covers new antiseizure molecules of different chemical classes, the exact mode of action of which is still unidentified. Newer agents include sulfonamides, thiadiazoles, semi- and thiosemicarbazones, pyrrolidine-2,5-diones, imidazoles, benzothiazoles and amino acid deriva tives. These new chemical entities can be useful for the design and development of forthcoming antiseizure agents.

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ChemInform Abstract: Synthesis, Anticonvulsant and Toxicity Screening of Newer Pyrimidine Semicarbazone Derivatives.

Cited by 2 publications

References 1 publication

Quinoline‐Dihydropyrimidin‐2(1H)‐one Hybrids: Synthesis, Biological Activity, and Mechanistic Studies

Quinoline‐Dihydropyrimidin‐2(1H)‐one Hybrids: Synthesis, Biological Activity, and Mechanistic Studies

An overview of structurally diversified anticonvulsant agents

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