A5103004820- Aquatic Invertebrate Ecology and Behavior
- Fish Ecology and Management Studies
- Algebraic Geometry and Number Theory
- Advanced Combinatorial Mathematics
- Freshwater macroinvertebrate diversity and ecology
- Marine Bivalve and Aquaculture Studies
- Asymmetric Synthesis and Catalysis
- HIV/AIDS drug development and treatment
- Synthesis and Biological Evaluation
- Coordination Chemistry and Organometallics
- Chemical Synthesis and Analysis
- Phosphorus compounds and reactions
- Pesticide Residue Analysis and Safety
- Synthesis and biological activity
- Polynomial and algebraic computation
- Quinazolinone synthesis and applications
- Commutative Algebra and Its Applications
- Carbohydrate Chemistry and Synthesis
- Advanced Algebra and Geometry
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Axial and Atropisomeric Chirality Synthesis
- Algebraic structures and combinatorial models
- Chemical synthesis and alkaloids
- Pesticide and Herbicide Environmental Studies
- Phenothiazines and Benzothiazines Synthesis and Activities
Alabama Department of Conservation and Natural Resources
2013-2024
Health & Safety Laboratory
1996-2024
Zoetis (United States)
2019-2021
University of Sheffield
2010-2021
Cornell University
2019
Colorado State University
2010-2015
University of Edinburgh
2014
AstraZeneca (United Kingdom)
2004-2013
University of York
1997-2012
Columbia University
2012
Medicines play an important role in the treatment and prevention of disease. Whereas side effects on human animal health resulting directly from have been widely documented, only recently occurrence fate medicines environment potential consequences for recognized as issue warranting consideration. shown to be released soils persist environment. This study was performed investigate a range veterinary taken up soil by plants used consumption assess significance this exposure route terms...
ABSTRACT This is the first American Fisheries Society conservation assessment of freshwater gastropods (snails) from Canada and United States by Gastropod Subcommittee (Endangered Species Committee). review covers 703 species representing 16 families 93 genera, which 67 are considered extinct, or possibly 278 endangered, 102 threatened, 73 vulnerable, 157 currently stable, 26 have uncertain taxonomic status. Of entire fauna, 74% imperiled (vulnerable, endangered) exceeds imperilment levels...
A broad screening program previously identified phenprocoumon (1) as a small molecule template for inhibition of HIV protease. Subsequent modification this lead through iterative cycles structure-based design led to the activity enhancements pyrone and dihydropyrone ring systems (II V) amide-based substitution (III). Incorporation sulfonamide within provided series highly potent protease inhibitors, with structure−activity relationships described in paper. Crystallographic studies further...
Wide-ranging exploration of analogues an ATP-competitive pyrrolopyrimidine inhibitor Akt led to the discovery clinical candidate AZD5363, which showed increased potency, reduced hERG affinity, and higher selectivity against closely related AGC kinase ROCK. This compound demonstrated good preclinical drug metabolism pharmacokinetics (DMPK) properties and, after oral dosing, pharmacodynamic knockdown phosphorylation downstream biomarkers in vivo, inhibition tumor growth a breast cancer xenograft model.
An enantiomerically pure (1-trimethylsilyl)ethyl group, constructed by a (−)-sparteine-directed enantioselective quench of laterally lithiated tertiary aromatic amide, exerts powerful thermodynamic control over the conformation adjacent amide substituent. Ortholithiation and functionalization in 6-position allows single conformer to be trapped as an diastereoisomerically atropisomer. Protodesilylation gives functionalized atropisomeric amides with stereogenic axis absolute configuration,...
Cross-relaxation effects are demonstrated between the imino protons and other in yeast tRNAPhe H2O. A detailed examination has been made of observed relaxation rate proton resonance at 11.8 ppm from DSS as a function D2O content solvent. This result, well size number nuclear Overhauser effects, suggests that dipolar magnetization transfer solvent H2O, amino, imino, tRNA may dominate processes low temperature. At higher temperatures is dominated by chemical exchange. The selective shown to be...
Hurwitz numbers count genus g, degree d covers of ℙ1 with fixed branch locus. This equals the a natural map defined on space. In tropical geometry, algebraic curves are replaced by certain piece-wise linear objects called curves. paper develops counterpart and shows that its recovers classical numbers. Further, combinatorial techniques developed applied to recover results Goulden et al. (in Adv. Math. 198:43–92, 2005) Shadrin 217(1):79–96, 2008) piecewise polynomial structure double in 0.
ADVERTISEMENT RETURN TO ISSUELetterNEXTStructure-Based Design of HIV Protease Inhibitors: Sulfonamide-Containing 5,6-Dihydro-4-hydroxy-2-pyrones as Non-Peptidic Inhibitors¶Suvit Thaisrivongs, Harvey I. Skulnick, Steve R. Turner, Joseph W. Strohbach, Ruben A. Tommasi, Paul D. Johnson, Aristoff, Thomas M. Judge, Ronald B. Gammill, Jeanette K. Morris, Karen Romines, Robert Chrusciel, Roger Hinshaw, Kong-Teck Chong, Gary Tarpley, Susan Poppe, David E. Slade, Janet C. Lynn, Miao-Miao Horng,...
A variety of analogues 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3-(ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement the substituted aryl moiety with various indoles provided bis(heteroaryl)piperazines (BHAPs) that 10-100-fold more potent than U-80493E. The pyridyl portion lead molecule was found to be very sensitive modifications. Extensive preclinical...
Recently, cyclooctylpyranone derivatives with m-carboxamide substituents (e.g. 2c) were identified as potent, nonpeptidic HIV protease inhibitors, but these compounds lacked significant antiviral activity in cell culture. Substitution of a sulfonamide group at the meta position, however, produces excellent binding affinity and activity. Guided by an iterative structure-based drug design process, we have prepared evaluated number derivatives, which are readily available via seven-step...
From a broad screening program, the 4-hydroxycoumarin phenprocoumon (I) was previously identified as lead template with HIV protease inhibitory activity. The crystal structure of phenprocoumon/HIV complex initiated structure-based design effort that initially 4-hydroxy-2-pyrone U-96988 (II) first-generation clinical candidate for potential treatment infection. Based upon III/HIV complex, series analogues incorporating 5,6-dihydro-4-hydroxy-2-pyrone were studied. It recognized in addition to...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTotal synthesis of a novel antiulcer agent via modification the intramolecular Wadsworth-Emmons-Wittig reactionPaul A. Aristoff, Paul D. Johnson, and Allen W. HarrisonCite this: J. Am. Chem. Soc. 1985, 107, 26, 7967–7974Publication Date (Print):December 1, 1985Publication History Published online1 May 2002Published inissue 1 December 1985https://pubs.acs.org/doi/10.1021/ja00312a028https://doi.org/10.1021/ja00312a028research-articleACS...
Hodge classes on the moduli space of admissible covers with monodromy group G are associated to irreducible representations G.We evaluate all linear integrals over spaces abelian in terms multiplication an wreath algebra.In case is cyclic and representation faithful, evaluation double Hurwitz numbers.In trivial, formula specializes well-known result Ekedahl-Lando-Shapiro-Vainshtein for curves single numbers.CONTENTS 0. Introduction 11. Stable relative maps 92.
Here we characterize the digestive gland microbiome from wild and cultured (hatchery-reared) Alabama rainbows (Villosa nebulosa) using 16 S rRNA gene pyrosequencing in order to understand effects of propagation on microbial community structure freshwater mussels. Digestive glands nine were analysed, five four a hatchery. Pyrosequencing yielded total 32,962 bacterial sequences 387 operational taxonomic units (OTUs). Tenericutes was dominant phylum all samples (>87%), followed by...
We examined the effects of four levels chronic hypoxic stress at three temperatures on survivorship Dreissena polymorpha and Corbicula fluminea to assess efficacy O 2 deprivation as a macrofouling control treatment examine if critical hypoxia limits support reported distribution patterns. At 25°C, tolerance was Po = 7.9, 11.9, 15.9, 23.8, 31.8 Torr (1 133.322 Pa) or 5, 7.5, 10, 15, 20% full air saturation (Po 159 Torr). 15°C, 15.9 tested 7.9 for 5°C treatments. For both species, temperature...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of CBI-PDE-I-dimer, the benzannelated analog CC-1065Paul A. Aristoff and Paul D. JohnsonCite this: J. Org. Chem. 1992, 57, 23, 6234–6239Publication Date (Print):November 1, 1992Publication History Published online1 May 2002Published inissue 1 November 1992https://doi.org/10.1021/jo00049a035RIGHTS & PERMISSIONSArticle Views303Altmetric-Citations54LEARN ABOUT THESE METRICSArticle Views are COUNTER-compliant sum full text article downloads...
Freshwater mollusks are highly imperiled, with 70% of the North American species extinct, endangered, or at risk extinction. Impoundments and other human impacts on Coosa River Alabama, Georgia Tennessee southeastern USA alone believed to have caused 50 mollusk extinctions, but uncertainty over boundaries among several putatively closely related makes this number preliminary. Our examination freshwater mussels collected during an extensive survey upper-drainage basin, DNA barcoding molecular...
Freshwater mussels, aquatic keystone species, are in global decline. Long life spans, sedentary lifestyles, and unique reproductive strategies involving obligate parasitic stages make unionid freshwater mussels particularly sensitive to environmental perturbations resulting from climate change. A greater understanding of the mechanisms by which closely related species differ their response thermal challenge is critical for successful conservation management practices. As such, both an acute...
Margaritifera hembeli, the Louisiana pearl shell, is a threatened mussel with distribution limited to headwaters of three tributaries Red River in central Louisiana, U.S.A. We assessed role that several habitat characters played determining its abundance and distribution. Pearl shell mussels were more common second-order streams elevated conductivity (approximately 0.04 mS/cm) water hardness (8 mg/L). A discriminant analysis indicated density was related depth, substrate size, compaction,...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStructure-Based Design of Sulfonamide-Substituted Non-Peptidic HIV Protease InhibitorsHarvey I. Skulnick, Paul D. Johnson, W. Jeffrey Howe, K. Tomich, Kong-Teck Chong, Keith Watenpaugh, Musiri N. Janakiraman, Lester A. Dolak, James P. McGrath, and Cite this: J. Med. Chem. 1995, 38, 26, 4968–4971Publication Date (Print):December 1, 1995Publication History Published online1 May 2002Published inissue 1 December...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDNA-directed alkylating agents. 2. Synthesis and biological activity of platinum complexes linked to 9-anilinoacridineBrian D. Palmer, Ho H. Lee, Paul Johnson, Bruce C. Baguley, Geoffrey Wickham, Laurence P. G. Wakelin, W. David McFadyen, William A. DennyCite this: J. Med. Chem. 1990, 33, 11, 3008–3014Publication Date (Print):November 1, 1990Publication History Published online1 May 2002Published inissue 1 November...