Synthesis of local anesthetics derived from cumic and 3-nitrocumic acids

Bryan, J.T.; Foote, P.A.

doi:10.1002/jps.3030391114

Cited by 3 publications

(1 citation statement)

References 1 publication

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“…it became evident that besides the known glycosides of digitalis there are many other glycosidal substances present which have not been isolated and characterized. During the past few years, several new glycosides, gitorin (l), strospeside (2,3), digipurpurin (4), digifolein (4), glucogitofucoside (4), gitaloxin ( 5 ) , verodoxin (F), digiproside (7), and diginatin (S), have been isolated. In this paper we shall describe another glycoside which has not been previously isolated and which we have obtained from extracts of D. Zunatu.…”

Section: Gitoside-a New Digitalis Glycoside *mentioning

confidence: 99%

A Comparative Study of the Local Anesthetic Potencies and Toxicities of Beta-Diethylaminoethyl Cumate and Procaine**College of Pharmacy, University of Florida, Gainesville

Gross

Voss

1957

Journal of the American Pharmaceutical Association (Scientific

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Section: Gitoside-a New Digitalis Glycoside *mentioning

confidence: 99%

A Comparative Study of the Local Anesthetic Potencies and Toxicities of Beta-Diethylaminoethyl Cumate and Procaine**College of Pharmacy, University of Florida, Gainesville

Gross

Voss

1957

Journal of the American Pharmaceutical Association (Scientific

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Preparation and anticancer activity of 2-Diethylaminoethyl-cis- and -trans-methylcyclohexanecarboxylates

Harmon

Meulman

Gupta

1970

Journal of Pharmaceutical Sciences

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Synthesis and Structure−Activity Relationships of Suramin-Derived P2Y₁₁ Receptor Antagonists with Nanomolar Potency

et al. 2005

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Selective and potent P2Y(11) receptor antagonists have yet to be developed, thus impeding an evaluation of this G protein-coupled receptor mainly expressed on immune cells. Taking suramin with moderate inhibitory potency as a template, 18 ureas with variations of the methyl groups of suramin and their precursors were functionally tested at P2Y(11), P2Y(1), and P2Y(2) receptors. Fluorine substitution of the methyl groups of suramin led to the first nanomolar P2Y(11) antagonist (8f, NF157, pK(i): 7.35). For selectivity, 8f was also tested at various P2X receptors. 8f displayed selectivity for P2Y(11) over P2Y(1) (>650-fold), P2Y(2) (>650-fold), P2X(2) (3-fold), P2X(3) (8-fold), P2X(4) (>22-fold), and P2X(7) (>67-fold) but no selectivity over P2X(1). QSAR studies confirm that residues with favored resonance and size parameters in the aromatic linker region can indeed lead to an increased potency as is the case for 8f. A symmetric structure linking two anionic clusters seems to be required for bioactivity. 8f may be helpful for studies evaluating the physiological role of P2Y(11) receptors.

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Synthesis of local anesthetics derived from cumic and 3-nitrocumic acids

Cited by 3 publications

References 1 publication

A Comparative Study of the Local Anesthetic Potencies and Toxicities of Beta-Diethylaminoethyl Cumate and Procaine**College of Pharmacy, University of Florida, Gainesville

A Comparative Study of the Local Anesthetic Potencies and Toxicities of Beta-Diethylaminoethyl Cumate and Procaine**College of Pharmacy, University of Florida, Gainesville

Preparation and anticancer activity of 2-Diethylaminoethyl-cis- and -trans-methylcyclohexanecarboxylates

Synthesis and Structure−Activity Relationships of Suramin-Derived P2Y₁₁ Receptor Antagonists with Nanomolar Potency

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Synthesis of local anesthetics derived from cumic and 3-nitrocumic acids

Cited by 3 publications

References 1 publication

A Comparative Study of the Local Anesthetic Potencies and Toxicities of Beta-Diethylaminoethyl Cumate and Procaine**College of Pharmacy, University of Florida, Gainesville

A Comparative Study of the Local Anesthetic Potencies and Toxicities of Beta-Diethylaminoethyl Cumate and Procaine**College of Pharmacy, University of Florida, Gainesville

Preparation and anticancer activity of 2-Diethylaminoethyl-cis- and -trans-methylcyclohexanecarboxylates

Synthesis and Structure−Activity Relationships of Suramin-Derived P2Y11 Receptor Antagonists with Nanomolar Potency

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Product

Resources

About

Synthesis and Structure−Activity Relationships of Suramin-Derived P2Y₁₁ Receptor Antagonists with Nanomolar Potency