Selective α(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

Philippe G. Nantermet; James C. Barrow; Harold G. Selnick; Carl F. Homnick; Roger M. Freidinger; Raymond S.L. Chang; Stacey S. O'Malley; Duane R. Reiss; Theodore P. Broten; Richard W. Ransom; Douglas J. Pettibone; Timothy Olah; Carlos Forray

doi:10.1016/S0960-894X(99)00696-4

Selective α(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

Philippe G. Nantermet, James C. Barrow, Harold G. Selnick, Carl F. Homnick, Roger M. Freidinger, Raymond S.L. Chang, Stacey S. O'Malley, Duane R. Reiss, Theodore P. Broten, Richard W. Ransom, Douglas J. Pettibone, Timothy Olah, Carlos Forray

Research output: Contribution to journal › Article › peer-review

39 Scopus citations

Abstract

A series of α(1a) receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original language	English (US)
Pages (from-to)	1625-1628
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	15
DOIs	https://doi.org/10.1016/S0960-894X(99)00696-4
State	Published - Aug 7 2000
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(99)00696-4

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Nantermet, P. G., Barrow, J. C., Selnick, H. G., Homnick, C. F., Freidinger, R. M., Chang, R. S. L., O'Malley, S. S., Reiss, D. R., Broten, T. P., Ransom, R. W., Pettibone, D. J., Olah, T., & Forray, C. (2000). Selective α(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones. Bioorganic and Medicinal Chemistry Letters, 10(15), 1625-1628. https://doi.org/10.1016/S0960-894X(99)00696-4

Nantermet, PG, Barrow, JC, Selnick, HG, Homnick, CF, Freidinger, RM, Chang, RSL, O'Malley, SS, Reiss, DR, Broten, TP, Ransom, RW, Pettibone, DJ, Olah, T & Forray, C 2000, 'Selective α(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones', Bioorganic and Medicinal Chemistry Letters, vol. 10, no. 15, pp. 1625-1628. https://doi.org/10.1016/S0960-894X(99)00696-4

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abstract = "A series of α(1a) receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.",

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doi = "10.1016/S0960-894X(99)00696-4",

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AU - Nantermet, Philippe G.

AU - Barrow, James C.

AU - Selnick, Harold G.

AU - Homnick, Carl F.

AU - Freidinger, Roger M.

AU - Chang, Raymond S.L.

AU - O'Malley, Stacey S.

AU - Reiss, Duane R.

AU - Broten, Theodore P.

AU - Ransom, Richard W.

AU - Pettibone, Douglas J.

AU - Olah, Timothy

AU - Forray, Carlos

PY - 2000/8/7

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AB - A series of α(1a) receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.

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Selective α(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

Abstract

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