Synthesis of metabolically stable arylpiperazine 5-HT1A receptor agonists

Arthur G. Romero; William H. Darlington; Monford F. Piercey; Robert A. Lahti

doi:10.1016/S0960-894X(00)80460-6

Synthesis of metabolically stable arylpiperazine 5-HT_1A receptor agonists

Arthur G. Romero, William H. Darlington, Monford F. Piercey, Robert A. Lahti

Division of Pulmonary & Critical Care Medicine

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

26 Scopus citations

Abstract

Although N-alkylarylpiperazines as a class are finding use as anxiolytics and antidepressants, many of these arylpiperazines are highly metabolically labile at the n-alkyl-piperazine bond. We have found that cyclopropanating the n-butyl chain contained in the 5-HT_1A receptor agonist ipsapirone (2) instills a resistance to this metabolism as well as providing information about the geometrical requirements of the 5-HT_1A receptor.

Original language	English
Pages (from-to)	1703-1706
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	2
Issue number	12
DOIs	https://doi.org/10.1016/S0960-894X(00)80460-6
State	Published - Dec 1992

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abstract = "Although N-alkylarylpiperazines as a class are finding use as anxiolytics and antidepressants, many of these arylpiperazines are highly metabolically labile at the n-alkyl-piperazine bond. We have found that cyclopropanating the n-butyl chain contained in the 5-HT1A receptor agonist ipsapirone (2) instills a resistance to this metabolism as well as providing information about the geometrical requirements of the 5-HT1A receptor.",

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AU - Darlington, William H.

AU - Piercey, Monford F.

AU - Lahti, Robert A.

PY - 1992/12

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AB - Although N-alkylarylpiperazines as a class are finding use as anxiolytics and antidepressants, many of these arylpiperazines are highly metabolically labile at the n-alkyl-piperazine bond. We have found that cyclopropanating the n-butyl chain contained in the 5-HT1A receptor agonist ipsapirone (2) instills a resistance to this metabolism as well as providing information about the geometrical requirements of the 5-HT1A receptor.

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ER -

Synthesis of metabolically stable arylpiperazine 5-HT_1A receptor agonists

Abstract

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