Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase

K. Shankaran; Karla L. Donnelly; Shrenik K. Shah; Ravindra N. Guthikonda; Malcolm MacCoss; John L. Humes; Stephen G. Pacholok; Stephan K. Grant; T. M. Kelly; K. K. Wong

doi:10.1016/j.bmcl.2004.06.033

Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase

K. Shankaran
, Karla L. Donnelly
, Shrenik K. Shah
, Ravindra N. Guthikonda
, Malcolm MacCoss
, John L. Humes
, Stephen G. Pacholok
, Stephan K. Grant
, T. M. Kelly
, K. K. Wong

Department of Chemistry and Chemical Biology

Merck

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

40 Scopus citations

Abstract

Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.

Original language	English
Pages (from-to)	4539-4544
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2004.06.033
State	Published - 6 Sep 2004

Keywords

1,3-Thiazolidin-2-imine
NOS
Pyrrolidin-2-imine

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10.1016/j.bmcl.2004.06.033

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title = "Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase",

abstract = "Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.",

keywords = "1,3-Thiazolidin-2-imine, NOS, Pyrrolidin-2-imine",

author = "K. Shankaran and Donnelly, \{Karla L.\} and Shah, \{Shrenik K.\} and Guthikonda, \{Ravindra N.\} and Malcolm MacCoss and Humes, \{John L.\} and Pacholok, \{Stephen G.\} and Grant, \{Stephan K.\} and Kelly, \{T. M.\} and Wong, \{K. K.\}",

year = "2004",

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doi = "10.1016/j.bmcl.2004.06.033",

language = "English",

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TY - JOUR

T1 - Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase

AU - Shankaran, K.

AU - Donnelly, Karla L.

AU - Shah, Shrenik K.

AU - Guthikonda, Ravindra N.

AU - MacCoss, Malcolm

AU - Humes, John L.

AU - Pacholok, Stephen G.

AU - Grant, Stephan K.

AU - Kelly, T. M.

AU - Wong, K. K.

PY - 2004/9/6

Y1 - 2004/9/6

N2 - Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.

AB - Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.

KW - 1,3-Thiazolidin-2-imine

KW - NOS

KW - Pyrrolidin-2-imine

UR - https://www.scopus.com/pages/publications/3843124407

UR - https://www.scopus.com/pages/publications/3843124407#tab=citedBy

U2 - 10.1016/j.bmcl.2004.06.033

DO - 10.1016/j.bmcl.2004.06.033

M3 - Article

C2 - 15357988

AN - SCOPUS:3843124407

SN - 0960-894X

VL - 14

SP - 4539

EP - 4544

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 17

ER -

Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase

Abstract

Keywords

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