User profiles for Howard Broughton

Howard Broughton

Lilly, SA
Verified email at lilly.com
Cited by 4110

Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved …

…, I Collins, MS Beer, HB Broughton… - Journal of medicinal …, 1999 - ACS Publications
It has previously been reported that a 3-(3-(piperazin-1-yl)propyl)indole series of 5-HT 1D
receptor ligands have pharmacokinetic advantages over the corresponding 3-(3-(piperidin-1-yl…

Identification of a Novel, Selective GABAA α5 Receptor Inverse Agonist Which Enhances Cognition

MS Chambers, JR Atack, HB Broughton… - Journal of medicinal …, 2003 - ACS Publications
In pursuit of a GABA A α5-subtype-selective inverse agonist to enhance cognition, a series
of 6,7-dihydro-2-benzothiophen-4(5H)-ones has been identified as a novel class of GABA A …

The chemical basis of serine palmitoyltransferase inhibition by myriocin

…, PRR Langridge-Smith, HB Broughton… - Journal of the …, 2013 - ACS Publications
Sphingolipids (SLs) are essential components of cellular membranes formed from the
condensation of l-serine and a long-chain acyl thioester. This first step is catalyzed by the pyridoxal…

Selection of heterocycles for drug design

HB Broughton, IA Watson - Journal of Molecular Graphics and Modelling, 2004 - Elsevier
A method has been devised to obtain heterocyclic ring systems suitable for use in drug design
and library design, with an emphasis on the selection of systems with good absorption, …

5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl) piperidin-4-yl) isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors

M Rowley, HB Broughton, I Collins… - Journal of medicinal …, 1996 - ACS Publications
Schizophrenia is a mental illness for which there is still a great need for novel drug therapy.
Classical neuroleptics, which are presumed to act by antagonism of dopamine D2 receptors, …

An X-ray crystallographic, mass spectroscopic, and NMR study of the limonoid insect antifeedant azadirachtin and related derivatives

JN Bilton, HB Broughton, PS Jones, SV Ley, HS Rzepa… - Tetrahedron, 1987 - Elsevier
The limonoid insect antifeedant azadirachtin (1) may be partially hydrogenated at the C22-C23
position and subsequently treated with an excess of sodium periodate and potassium …

Inositol monophosphatase—a putative target for Li+ in the treatment of bipolar disorder

JR Atack, HB Broughton, SJ Pollack - Trends in neurosciences, 1995 - cell.com
Despite ITS SIDE-EFFECT profile and narrow thera-peutic window, Li’remains the treatment
of choice for bipolar disorder’,‘. However, the mechanism by which it attenuates the dramatic …

Mechanism of inositol monophosphatase, the putative target of lithium therapy.

…, LL Iversen, HB Broughton - Proceedings of the …, 1994 - National Acad Sciences
myo-Inositol monophosphatase (myo-inositol-1-phosphate phosphohydrolase, EC 3.1.3.25)
is an attractive target for mechanistic investigation due to its critical role in the …

Controlled Modification of Acidity in Cholecystokinin B Receptor Antagonists:  N-(1,4-Benzodiazepin-3-yl)-N '-[3-(tetrazol-5-ylamino)phenyl]ureas

JL Castro, RG Ball, HB Broughton… - Journal of medicinal …, 1996 - ACS Publications
The design, synthesis, and biological activity of a novel series of CCK-B receptor antagonists
(1) which incorporate a tetrazol-5-ylamino functionality attached to the phenyl ring of the …

N-Arylsulfonylindole Derivatives as Serotonin 5-HT6 Receptor Ligands

…, MS Beer, L Bristow, HB Broughton… - Journal of medicinal …, 2001 - ACS Publications
A series of N 1 -arylsulfonyltryptamines were found to be potent ligands of the human serotonin
5-HT 6 receptor with the 5-methoxy-1-benzenesulfonyl analogue (19) having the highest …