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Volumn 20, Issue 17, 2010, Pages 5147-5152

Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists

Author keywords

Calcium channel antagonists; Epilepsy; Quinazolin 2 ones; T Type calcium channel

Indexed keywords

1,2,3,5 TETRAHYDROIMIDAZO[2,1 B]QUINAZOLIN 2 ONE DERIVATIVE; CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL T TYPE; PREGNANE X RECEPTOR; QUINAZOLINONE DERIVATIVE;

EID: 77955654799     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.07.010     Document Type: Article
Times cited : (24)

References (29)
  • 21
    • 77955661166 scopus 로고    scopus 로고
    • The synthesis of 4,4-disubstituted quinazolinones has been reported in the following patent literature: WO2009009015 and WO2006098969
    • The synthesis of 4,4-disubstituted quinazolinones has been reported in the following patent literature: WO2009009015 and WO2006098969.
  • 23
    • 77955654116 scopus 로고    scopus 로고
    • note
    • Based on Ref. 22 and in house data, the following guidelines are used to determine the potential for clinical drug-drug interactions. Using % activation (compared to the positive control Rifampin), the criteria for having a high potential for clinical drug-drug interaction is defined as a value of >40%, between 15% and 40% for moderate potential, and <15% as having a low potential.
  • 25
    • 77955660655 scopus 로고    scopus 로고
    • For metabolic stability assay, compounds (1 μM) were incubated with human liver microsomes (0.2 mg protein/mL) in the presence of NADPH cofactor for 30 or 60 min at 37 °C
    • For metabolic stability assay, compounds (1 μM) were incubated with human liver microsomes (0.2 mg protein/mL) in the presence of NADPH cofactor for 30 or 60 min at 37 °C.
  • 26
    • 77955661769 scopus 로고    scopus 로고
    • Compound 45 is a single, active enantiomer. All in vitro and in vivo data included for 45 was collected on the active enantiomer
    • Compound 45 is a single, active enantiomer. All in vitro and in vivo data included for 45 was collected on the active enantiomer.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.