Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Martyn Clive Pritchard"'
Autor:
Pamela Kent, Alexander T. McKnight, Tania Bédard, Zul Merali, Hymie Anisman, Nick Andrews, M Isabel Gonzalez, Ben Davis, Martyn Clive Pritchard
Publikováno v:
The Journal of Neuroscience. 26:10387-10396
The effects of PD 176252 [3-(1H-indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(nitro-phenyl)ureido]propionamide], a nonpeptide bombesin (BB) BB1/BB2receptor antagonist, were assessed in rats using several ethologically rel
Autor:
B. G. M. Burgaud, Jean Martinez, N. Bernad, David Christopher Horwell, R. A. Lewthwaite, Martyn Clive Pritchard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:1245-1248
The design, synthesis and biological actions of a novel, non-peptide CCK1 receptor agonist (PD 170292) which exhibits a similar pharmacological profile to the CCK analogue JMV180 is reported. PD 170292 was designed based on a consideration of the str
Autor:
J. Ronald Rubin, Russell A. Lewthwaite, David C. Horwell, Martyn Clive Pritchard, Ratcliffe Giles S
Publikováno v:
Tetrahedron. 54:4591-4606
A series of piperazinone ring systems have been synthesised as a means of evaluating the effect of conformational restriction on high affinity non-peptide NK1, NK3 and CCK-B receptor ligands. The synthesis of the targeted heterocycles is described al
Autor:
Martyn Clive Pritchard, Bruce D. Roth, N. Suman-Chauhan, Daniel F. Ortwine, C.E. Augelli-Szafran, David R. Hill, David Christopher Horwell, Clare O. Kneen, Bharat K. Trivedi, Louise Webdale, Terri S. Purchase
Publikováno v:
Bioorganic & Medicinal Chemistry. 4:1733-1745
A study of structure-activity relationships of a series of ‘dipeptoid’ CCK-B receptor antagonists was performed in which variations of the phenyl ring were examined while the [(2-adamantyloxy)carbonyl]-α-methyl-R)-tryptophan moiety of the potent
Autor:
Martyn Clive Pritchard, Jennifer Raphy, J.M. Eden, J. Hodgson, P. Boden, David Christopher Horwell, N. Suman-Chauhan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1773-1778
In this paper we describe the transformation of a series of modified dipeptide NK3 receptor selective ligands, previously developed from a hit identified from the screening of a dipeptide chemical library, into non-peptide, nanomolar affinity NK3 rec
Publikováno v:
Tetrahedron: Asymmetry. 6:1081-1084
The asymmetric synthesis, CCK receptor binding affinities and CCK-A agonist properties of a novel series of non-peptide CCK-A receptor selective ligands is reported.
Publikováno v:
Tetrahedron: Asymmetry. 6:93-96
α-Bromoamides derived from bornane-10,2-sultam can be prepared diastereoselectively starting from racemic α-bromo acids, and undergo epimerisation under appropriate conditions leading to an enhanced d.e.. By reacting the individual isomers, or in s
Autor:
J.M. Eden, J. Hodgson, P. Boden, Ratcliffe Giles S, Alexander T. McKnight, David Christopher Horwell, Martyn Clive Pritchard, Jenny Raphy, N. Suman-Chauhan, John Hughes, Kenneth G. Meecham, Geoffrey N. Woodruff, William Howson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1679-1684
Boc(S)Phe(S)PheNH2 (1c) was identified from the biological screening of an in-house dipeptide chemical library as a micromolar NK3 receptor selective ligand (IC50=1150nM). This lead structure has subsequently been developed into a series of potent an
Autor:
Geoffery N. Woodruff, John O'Toole, John Hughes, David C. Rees, Michael Higginbottom, Steven Boyle, William Howson, David Christopher Horwell, Kevan Martin, Martyn Clive Pritchard, Steven Guard, Alexander T. McKnight, K.J. Watling, Edward Roberts, Jenny Raphy
Publikováno v:
Bioorganic & Medicinal Chemistry. 2:357-370
The rational design of a non-peptide tachykinin NK 1 receptor antagonist, [(2-benzofuran)-CH 2 OCO]-( R )-α-MeTrp-( S )-NHCH(CH 3 )Ph ( 28 , PD 154075) is described. Compound 28 has a K i = 9 and 0.35 nM for the NK 1 receptor binding site in guinea-
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:989-992
The design and synthesis of high affinity α,β-didehydrotryptophan substituted CCK ligands is described. Ligands selective for both the CCK-A and CCK-B receptor subtypes have been prepared.