5-Chloro-3-(phenylsulfonyl) indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase
TM Williams, TM Ciccarone… - Journal of medicinal …, 1993 - ACS Publications
Development of effective pharmaceutical interventions in acquired immunodeficiency syndrome
(AIDS) is a high priority goal. About 10 million individuals worldwide are estimated to be …
(AIDS) is a high priority goal. About 10 million individuals worldwide are estimated to be …
Evaluation of farnesyl: protein transferase and geranylgeranyl: protein transferase inhibitor combinations in preclinical models
…, WC Lumma, SV Machotka, E Rands, TM Williams… - Cancer research, 2001 - AACR
Farnesyl:protein transferase (FPTase) inhibitors (FTIs) were originally developed as potential
anticancer agents targeting the ras oncogene and are currently in clinical trials. Whereas …
anticancer agents targeting the ras oncogene and are currently in clinical trials. Whereas …
Discovery of 3-{5-[(6-Amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): A Potent, Orally Bioavailable HIV-1 Non …
…, JT Sisko, RM Tynebor, TM Williams… - Journal of medicinal …, 2008 - ACS Publications
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have been shown to be a key
component of highly active antiretroviral therapy (HAART). The use of NNRTIs has become part …
component of highly active antiretroviral therapy (HAART). The use of NNRTIs has become part …
Pharmacological characterization of MK-0974 [N-[(3R, 6S)-6-(2, 3-difluorophenyl)-2-oxo-1-(2, 2, 2-trifluoroethyl) azepan-3-yl]-4-(2-oxo-2, 3-dihydro-1H-imidazo [4, 5-b] …
…, AW Shaw, SL Graham, JP Vacca, TM Williams… - Journal of pharmacology …, 2008 - ASPET
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide that plays a key role in the
pathophysiology of migraine headache. CGRP levels in the cranial circulation are …
pathophysiology of migraine headache. CGRP levels in the cranial circulation are …
Potent, Orally Bioavailable Calcitonin Gene-Related Peptide Receptor Antagonists for the Treatment of Migraine: Discovery of N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1- (2,2,2 …
…, SL Graham, JP Vacca, TM Williams - Journal of medicinal …, 2007 - ACS Publications
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine.
Herein we describe optimization of CGRP receptor antagonists based on an earlier lead …
Herein we describe optimization of CGRP receptor antagonists based on an earlier lead …
Psychomotor slowing is associated with distal symmetrical polyneuropathy in adults with diabetes mellitus
CM Ryan, TM Williams, TJ Orchard, DN Finegold - Diabetes, 1992 - Am Diabetes Assoc
To test the hypothesis that diabetes mellitus is associated with cognitive dysfunction, a battery
of neuropsychological tests was administered to 75 diabetic adults and an equal number …
of neuropsychological tests was administered to 75 diabetic adults and an equal number …
Effects of insulin-dependent diabetes on learning and memory efficiency in adults
CM Ryan, TM Williams - Journal of clinical and experimental …, 1993 - Taylor & Francis
Previous work with elderly adults with maturity-onset non-insulin-dependent diabetes has
demonstrated the presence of significant learning and memory deficits which are correlated …
demonstrated the presence of significant learning and memory deficits which are correlated …
Mechanism based neurotoxicity of mGlu5 positive allosteric modulators–development challenges for a promising novel antipsychotic target
…, TW Rosahl, JP Rocher, R Hargreaves, TM Williams - …, 2014 - Elsevier
Previous work has suggested that activation of mGlu5 receptor augments NMDA receptor
function and thereby may constitute a rational approach addressing glutamate hypofunction in …
function and thereby may constitute a rational approach addressing glutamate hypofunction in …
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)
…, GD Hartman, JP Vacca, TM Williams - Bioorganic & medicinal …, 2008 - Elsevier
… Williams a … In 1993, Williams and co-workers reported that 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide
(1, Fig. 1) was a potent NNRTI against wild-type enzyme. Compound 1 also displays sub-micromolar …
(1, Fig. 1) was a potent NNRTI against wild-type enzyme. Compound 1 also displays sub-micromolar …
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency
…, JS Taylor, ES Walsh, TM Williams… - Journal of medicinal …, 2002 - ACS Publications
A series of macrocyclic 3-aminopyrrolidinone farnesyltransferase inhibitors (FTIs) has been
synthesized. Compared with previously described linear 3-aminopyrrolidinone FTIs such as …
synthesized. Compared with previously described linear 3-aminopyrrolidinone FTIs such as …