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Start Over Author "Woolven JM" Journal bioorganic medicinal chemistry letters
2 results on '"Woolven JM"'

1. Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.

Author

Young RJ, Alderton W, Angell AD, Beswick PJ, Brown D, Chambers CL, Crowe MC, Dawson J, Hamlett CC, Hodgson ST, Kleanthous S, Knowles RG, Russell LJ, Stocker R, and Woolven JM

Subjects
Amidines chemistry, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors chemistry, Heterocyclic Compounds chemistry, Heterocyclic Compounds pharmacology, Humans, Inhibitory Concentration 50, Models, Molecular, Molecular Structure, Proline chemical synthesis, Proline chemistry, Proline pharmacology, Amidines chemical synthesis, Amidines pharmacology, Enzyme Activation drug effects, Enzyme Inhibitors pharmacology, Heme antagonists & inhibitors, Heterocyclic Compounds chemical synthesis, Nitric Oxide Synthase Type II antagonists & inhibitors, Proline analogs & derivatives
Abstract

Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC(50)=0.12 μM) and selective iNOS inhibitor (>100-fold vs both eNOS and nNOS), with probable binding to the key anchoring glutamate residue and co-ordination to the haem iron., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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2. Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.

Author

Barnett HA, Coe DM, Cooper TW, Jack TI, Jones HT, Macdonald SJ, McLay IM, Rayner N, Sasse RZ, Shipley TJ, Skone PA, Somers GI, Taylor S, Uings IJ, Woolven JM, and Weingarten GG

Subjects
Administration, Oral, Animals, Benzamides pharmacology, Humans, Hydrophobic and Hydrophilic Interactions, Prednisolone, Pyrazoles pharmacology, Rats, Structure-Activity Relationship, Benzamides chemical synthesis, Pyrazoles chemical synthesis, Receptors, Glucocorticoid agonists
Abstract

Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compounds with lower lipophilicity, for example N-hydroxyethyl benzamides (e.g., 16e).

Published
2009
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