Search Results - "Jaynes, Burton H"
-
1
5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure–activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog
Published in Bioorganic & medicinal chemistry letters (15-01-2006)“…Structure–activity relationship studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-lyl]-5-methanesulfonyl (SO 2Me)/5-sulfamoyl (SO 2NH…”
Get full text
Journal Article -
2
Quantitative Structure−Activity Relationships among Macrolide Antibacterial Agents: In Vitro and in Vivo Potency against Pasteurella multocida
Published in Journal of medicinal chemistry (25-04-1997)“…Quantitative structure−activity relationships have been found among macrolide antibacterial agents in their potencies against the bacterial pathogen…”
Get full text
Journal Article -
3
5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: Molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile
Published in Bioorganic & medicinal chemistry letters (15-02-2007)“…The SAR of the 5-heteroatom and aryl substituted pyrazoles with 4-nitrile substitution shows substantial improvement in activity against the COX enzymes…”
Get full text
Journal Article -
4
Comparative structure–activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition
Published in Bioorganic & medicinal chemistry (01-02-2008)“…Structure–activity relationship (SAR) studies of novel 5-alkyl and 5-aryl/heteroaryl substituted 1,2,4-triazoles are described. The in vitro activity is…”
Get full text
Journal Article -
5
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-04-2006)“…The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure–activity relationship (SAR)…”
Get full text
Journal Article -
6
5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure–activity relationship studies of 5-alkylethers and 5-thioethers
Published in Bioorganic & medicinal chemistry letters (01-03-2006)“…Structure–activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine…”
Get full text
Journal Article -
7
In vitro and in vivo profile of 5-[(4' -trifluoromethyl -biphenyl -2-carbonyl ) -amino]-1H -indole -2 -carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity
Published in Bioorganic & medicinal chemistry letters (01-04-2007)“…The synthesis of a novel gut selective MTP inhibitor, 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl…”
Get full text
Journal Article -
8
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine
Published in Bioorganic & medicinal chemistry letters (05-01-2004)“…Structure–activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes…”
Get full text
Journal Article -
9
Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents
Published in Bioorganic & medicinal chemistry letters (01-06-2006)“…Structure activity relationship (SAR) studies of a novel class of MTP inhibitors are described. A number of novel MTP inhibitors have been identified with…”
Get full text
Journal Article -
10
Efficient Preparation of Hygromycin A Aglycon and Its Antibacterial 4'-Allyl Ether, CP-111905
Published in Journal of organic chemistry (01-03-1994)Get full text
Journal Article -
11
In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor
Published in Bioorganic & medicinal chemistry (01-03-2005)“…The synthesis of a novel canine COX-2 selective inhibitor, 2-(3-difluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, and its in vitro and in vivo…”
Get full text
Journal Article -
12
A synthetic route to forskolin
Published in Journal of the American Chemical Society (01-12-1987)Get full text
Journal Article -
13
Repromicin Derivatives with Potent Antibacterial Activity against Pasteurella multocida
Published in Journal of medicinal chemistry (14-03-1997)“…Reductive amination of repromicin with polyfunctional amines has led to new macrolide antibacterial agents, some of which are highly potent against the…”
Get full text
Journal Article -
14
Efficient fluoride-mediated synthesis of 5-alkyl amino- and ether-substituted pyrazoles
Published in Tetrahedron letters (03-10-2005)“…Fluoride-mediated nucleophilic substitution reactions of 1-(4-methylsulfonyl (or sulfonamido)-2-pyridyl)-5-chloro-4-cyano pyrazoles with various amines and…”
Get full text
Journal Article -
15
In vitro and in vivo profile of 5-[(4′-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1 H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity
Published in Bioorganic & medicinal chemistry letters (2007)“…The synthesis of a novel gut selective MTP inhibitor, 5-[(4′-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1 H-indole-2-carboxylic acid benzylmethyl…”
Get full text
Journal Article -
16
Semisynthetic hygromycin A analogs: synthesis and anti-bacterial activity of derivatives lacking the furanose moiety
Published in Journal of antibiotics (01-10-1992)Get more information
Journal Article