Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist

Robert J. DeVita; Darius D. Hollings; Mark T. Goulet; Matthew J. Wyvratt; Michael H. Fisher; Jane L. Lo; Yi Tien Yang; Kang Cheng; Roy G. Smith

doi:10.1016/S0960-894X(99)00446-1

Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist

Robert J. DeVita, Darius D. Hollings, Mark T. Goulet, Matthew J. Wyvratt, Michael H. Fisher, Jane L. Lo, Yi Tien Yang, Kang Cheng, Roy G. Smith

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

64 Scopus citations

Abstract

Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (~300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chlorosubstitution of the 1H-quinolone core.

Original language	English
Pages (from-to)	2615-2620
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	9
Issue number	17
DOIs	https://doi.org/10.1016/S0960-894X(99)00446-1
State	Published - 6 Sep 1999
Externally published	Yes

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title = "Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist",

abstract = "Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (~300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chlorosubstitution of the 1H-quinolone core.",

author = "DeVita, {Robert J.} and Hollings, {Darius D.} and Goulet, {Mark T.} and Wyvratt, {Matthew J.} and Fisher, {Michael H.} and Lo, {Jane L.} and Yang, {Yi Tien} and Kang Cheng and Smith, {Roy G.}",

year = "1999",

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T1 - Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist

AU - DeVita, Robert J.

AU - Hollings, Darius D.

AU - Goulet, Mark T.

AU - Wyvratt, Matthew J.

AU - Fisher, Michael H.

AU - Lo, Jane L.

AU - Yang, Yi Tien

AU - Cheng, Kang

AU - Smith, Roy G.

PY - 1999/9/6

Y1 - 1999/9/6

N2 - Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (~300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chlorosubstitution of the 1H-quinolone core.

AB - Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (~300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chlorosubstitution of the 1H-quinolone core.

UR - http://www.scopus.com/inward/record.url?scp=0033530102&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(99)00446-1

DO - 10.1016/S0960-894X(99)00446-1

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AN - SCOPUS:0033530102

SN - 0960-894X

VL - 9

SP - 2615

EP - 2620

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 17

ER -

Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist

Abstract

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