150-69-6Relevant articles and documents
Design, synthesis, and potential CNS activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-methyl- 4H-quinazolin-3-yl)-urea
Kashaw, Sushil K.,Kashaw, Varsha,Mishra, Pradeep,Jain,Stables
experimental part, p. 738 - 745 (2012/05/20)
Twelve new 1-(4-substituted-phenyl)-3-(4-oxo- 2-methyl-4H-quinazolin-3-yl)- urea were synthesized and screened for anticonvulsant, CNS depressant, and sedativehypnotic activity. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight 2,3-Disubstitutedquinazolin- 4(3H)-one were examined in the maximal electroshock-induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Spectroscopic data and elemental analysis were consistent with the newly synthesized compounds. The neurotoxicity was assessed using the rotorod method. M3, M4 and M10 were found to be active in both MES screen and scPTZ screen at 0.5 h. All except M11 showed more than 44% decrease in locomotor activity after 1 h of compound administration via actophotometer screen. CNS-depressant activity screened with the help of the forced swim method resulted into some potent compounds. Except for M6 and M11 other tested compounds were found to exhibit potent CNS depressants activity as indicated by increased immobility time. It can be concluded that newly synthesized compounds possessed sedative-hypnotic and CNS depressant activities. Springer Science+Business Media, LLC 2010.
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,Stables
experimental part, p. 4335 - 4343 (2009/12/24)
Several new 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea were synthesized and screened for anticonvulsant, CNS depressant and sedative-hypnotic activity in the mice. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight synthesized compounds were examined in the maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Spectroscopic data and elemental analysis were consistent with the newly synthesized compounds. The neurotoxicity was assessed using the rotorod method. Compounds E1, E6, E9, E12, P3, P4 and P6 were found to be active in the MES screen whereas E1, P4, P6 and P11 were found to be active in the scPTZ screen. All except E6, E11 and P6 showed more than 50% decrease in locomotor activity at 1 h of compound administration via actophotometer screen. CNS depressant activity screened with the help of the forced swim method resulted into some potent compounds. All the compounds were found to exhibit potent CNS depressants activity as indicated by increased immobility time. It can be concluded that newly synthesized compounds possessed promising CNS activities.
Synthesis of sulofenur analoges as antitumour agents: Part II
Youssef, Khairia M.,Al-Abdullah, Ebtihal,El-Khamees, Hamad
, p. 481 - 503 (2007/10/03)
A series of N-aryl-N′-heteroaryl or N,N′-diheteroaryl sulfonylurea has been prepared using two different methods. All the intermediates were prepared including heteroarylsulfonyl chlorides and aryl- or hetero-arylurea derivatives. Structural elucidation of the newly synthesized compounds were based on elementary analysis, IR, 1H & 1C NMR and mass spectra. The antitumor screening of the prepared compounds were performed at the National Cancer Institute (NCI) Bethesda, Maryland, USA. Compound N-(3-methylbenzothiazol-2-yl)-N′ -(1-benzodiazolyl-sulfonyl)urea (13) with GI50, TGI, LC50 (MG-MID) values of 25.1, 77.5, 93.3 μM, respectively is the most active compound in this study. It showed a broad spectrum antitumor activity as well as selective activity toward individual cell lines. It showed distinctive activities compared to that of sulofenur against RPMI-8226 leukemia, EKVX Non-small lung cancer, PC-3 prostate cancer, OVCAR-4 Ovarian cancer, CAKI-1Renal cancer, MDA-MB-435 and T-47D Breast cancer with GI50 values of 21.5, 1.7, 28.7, 25.9, 15.9, 27.9, 15.1 μM, respectively.
