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Volumn 21, Issue 6, 2011, Pages 1692-1696

Pyridyl amides as potent inhibitors of T-type calcium channels

Author keywords

Electrocorticogram; Epilepsy; Pregnane X receptor; Structure activity relationships; T type calcium channel

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL T TYPE; PIPERIDINE; PYRIDYLAMIDE DERIVATIVE; QUINAZOLINONE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79952362824     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.089     Document Type: Article
Times cited : (26)

References (54)
  • 35
    • 79952360510 scopus 로고    scopus 로고
    • The TTA-Ax nomenclature is provided for consistency across publications, such as Refs. 18 and 19
    • The TTA-Ax nomenclature is provided for consistency across publications, such as Refs. 18 and 19.
  • 36
    • 79952364658 scopus 로고    scopus 로고
    • Due to its potency, favorable physical properties, and ease of preparation compound 15 was labeled with tritium and demonstrated to be an effective radioligand for binding assays. See Ref. 19 for more details
    • Due to its potency, favorable physical properties, and ease of preparation compound 15 was labeled with tritium and demonstrated to be an effective radioligand for binding assays. See Ref. 19 for more details.
  • 43
    • 79952360016 scopus 로고    scopus 로고
    • 50 values of >30 μM at -80 mV. See Ref. 26 for details
    • 50 values of >30 μM at -80 mV. See Ref. 26 for details.
  • 48
    • 79952359493 scopus 로고    scopus 로고
    • We have previously reported that the effects of 37 on active wake in rat are dose-dependent when the compound is dosed during the active phase. See Ref. 28 for details
    • We have previously reported that the effects of 37 on active wake in rat are dose-dependent when the compound is dosed during the active phase. See Ref. 28 for details.
  • 49
    • 79952364471 scopus 로고    scopus 로고
    • Compound 37 (TTA-A2) and quinazolinone 2 (TTA-Q6) are both state-dependent T-type channel blockers while piperidine 1 (TTA-P2) is a state-independent blocker. The consistent effect of all three compounds on sleep and wake in rodents suggests that binding to the inactivated state of the channel is sufficient for pharmacological effects
    • Compound 37 (TTA-A2) and quinazolinone 2 (TTA-Q6) are both state-dependent T-type channel blockers while piperidine 1 (TTA-P2) is a state-independent blocker. The consistent effect of all three compounds on sleep and wake in rodents suggests that binding to the inactivated state of the channel is sufficient for pharmacological effects.
  • 50
    • 4143071432 scopus 로고    scopus 로고
    • For a discussion on the diastereoselectivity of Grignard additions to chiral 2-pyridyl tert-butyl (Ellman) sulfinimines, see
    • For a discussion on the diastereoselectivity of Grignard additions to chiral 2-pyridyl tert-butyl (Ellman) sulfinimines, see: Kuduk, S. D.; DiPardo, R. M.; Chang, R. K.; Ng, C.; Bock, M. G. Tetrahedron Lett. 2004, 45, 6641-6643.
    • (2004) Tetrahedron Lett. , vol.45 , pp. 6641-6643
    • Kuduk, S.D.1    Dipardo, R.M.2    Chang, R.K.3    Ng, C.4    Bock, M.G.5
  • 51
    • 79952362069 scopus 로고    scopus 로고
    • The absolute stereochemistry of a closely related analog of 43 was firmly established by X-ray crystallographic analysis. See Supplementary data for details
    • The absolute stereochemistry of a closely related analog of 43 was firmly established by X-ray crystallographic analysis. See Supplementary data for details.
  • 52
    • 0037163328 scopus 로고    scopus 로고
    • The synthesis of 4-cyclopropylphenylacetic acid is described in the Supplementary data. For a leading reference on the use of cyclopropylboronic acid in Suzuki cross-coupling reactions, see: Wallace, D. J.; Chen, C. Y. Tetrahedron Lett. 2002, 43, 6987-6990.
    • (2002) Tetrahedron Lett. , vol.43 , pp. 6987-6990
    • Wallace, D.J.1    Chen, C.Y.2
  • 53
    • 79952360606 scopus 로고    scopus 로고
    • We have recently reported that 37 inhibits high-fat diet-induced weight gain in mice. See Ref. 28 for details
    • We have recently reported that 37 inhibits high-fat diet-induced weight gain in mice. See Ref. 28 for details.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.