Discovery of molluscicidal and cercaricidal activities of 3-substituted quinazolinone derivatives by a scaffold hopping approach using a pseudo-ring based on the intramolecular hydrogen bond formation

Pharmacological characterization of a highly selective Rho kinase (ROCK) inhibitor and its therapeutic effects in experimental pulmonary hypertension

“…2). Such bidentate interaction was further strengthened by the presence of an intramolecular hydrogen bond between the methoxy oxygen and the neighboring amide NH 2 (Guo et al, 2016), yielding to the formation of a pseudo bicyclic system that superimposed well with the isoquinolone ring system of hydroxyfasudil. Besides the hinge interactions, Compound 3 formed extensive hydrophobic contacts with Ile82, Val90, Leu205 and Phe368 through its pyridine ring (not shown in Fig.…”

Evaluation of molluscicidal, miracicidal and cercaricidal activities of crude aqueous extracts of Origanum majorana, Ziziphus spina-christi and Salvia fruticosa on Schistosoma mansoni and Schistosoma haematobium

“…Also in Egypt, most people do agricultural work on irrigation farms, recreational activities, and household chores. For these reasons, they are always exposed to the water that contains the free-swimming larvae infective stage (cercariae), which comes out of the freshwater snail (Guo et al, 2016). In Egypt, Biomphalaria alexandrina freshwater snail is the intermediate host of Schistosoma mansoni (Ibrahim and Abdalla, 2017), also, Bulinus truncatus snail which is widely distributed all over Egypt is the intermediate host of Schistosoma haematobium (Youssef, 2010;Bakry et al, 2004;2015).…”

“…Environmental and economic considerations are increasing for the use of molluscicides that are biodegradable, selectively active, readily available in the affected areas and inexpensive. Niclosamide is a pesticide used as a positive control and consists of 5 chloro-N-(2 chloro-4nitrophenyl)-2-hydroxy-benzamide (Guo et al, 2016). Nevertheless, any chemical compound such as niclosamide does have some drawbacks that involve a risk of toxicity for aquatic plants, fish, birds, domestic animals, and humans, lower solubility, and expensive cost.…”

“…Nevertheless, any chemical compound such as niclosamide does have some drawbacks that involve a risk of toxicity for aquatic plants, fish, birds, domestic animals, and humans, lower solubility, and expensive cost. Also, to achieve snail control niclosamide should be used continuously over a longer time period, and this can lead to drug resistance (Kenawy and Rizk, 2004;Guo et al, 2008;Li et al, 2013;Guo et al, 2016). There are also other compounds that have a fatal effect on adult snails and embryos, such as copper, but they are not used regularly in common practices because they are absorbed by soil and organic materials (Ribeiro et al, 2009;Martins et al, 2014).…”

Comparative study between the Titanium Phosphate TiP2O7 and the Phosphate Fertilizers in the catalysis of the Quinazolin-4(3H)-one derivatives synthesis

“…The quinazolin-4(3H)-one derivatives present an important class of heterocyclic compounds, which attracted considerable attention in these last years, due to their pharmacological and biological activities such as antitumor drugs 1 , antibacterial 2 , antihypertensive 3 , anti-inflammatory 4 , anti-HIV 5 , antifungal 6 , nonpeptide CCK-B antagonists 7 , antiallergic 8 , insecticidal 9 , and inhibition of humane erythrocyte purine nucleoside phosphorylase 10 . In addition, the quinazolin-4(3H)-ones are the basic building blocks in the synthesis of natural products 11 and the constituents of some isolated natural alkaloids 12 .…”