- METHOD OF IMPROVING STABILITY OF SWEET ENHANCER AND COMPOSITION CONTAINING STABILIZED SWEET ENHANCER
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The present invention includes methods of stabilizing one or more sweet enhancers when they are exposed to a light source as well as liquid compositions containing one or more sweet enhancers and one or more photostabilizers.
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- Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists
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SAR (structure-activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative alloste
- Zheng, Guo Zhu,Bhatia, Pramila,Daanen, Jerome,Kolasa, Teodozyj,Patel, Meena,Latshaw, Steven,El Kouhen, Odile F.,Chang, Renjie,Uchic, Marie E.,Miller, Loan,Nakane, Masaki,Lehto, Sonya G.,Honore, Marie P.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
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p. 7374 - 7388
(2007/10/03)
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- Antifolate and Antibacterial Activities of 5-Substituted 2,4-Diaminoquinazolines
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A series of 5-substituted 2,4-diaminoquinazolines (3) has been synthesized and evaluated as inhibitors of the enzyme dihydrofolate reductase (DHFR) from both bacterial and mammalian sources.The best compounds (e.g. 53) show good activity against Escherichia coli DHFR, but there is no significant selectivity for the bacterial over the mammalian enzyme.The structure-activity relationships for enzyme inhibition appear to be complex and not amenable to simple analysis; a hypotesis to explain the observed qualitative structure-activity relationships is proposed.The inhibitory activities of the compounds against the growth of intact bacterial cells in vitro closely parallel those for the inhibition of the isolated bacterial enzymes, suggesting that their antifolate action is responsible for their antibacterial effects.Five of the compounds were tested for their ability to cure a systemic E. coli infection in the mouse, but they showed no therapeutic effects at their maximum tolerated doses.
- Harris, Neil V.,Smith, Christopher,Bowden, Keith
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p. 434 - 444
(2007/10/02)
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- Trichloromethyl Carbonochloridate: A Dehydrating Reagent for the Preparation of Nitriles from Aldoximes
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Alkyl, aralkyl, and heteroaryl aldoximes bearing various functionalities are readily converted to the corresponding nitriles in good yields using trichloromethyl carbonochloridate as dehydrating agent.
- Mai, Khuong,Path, Ghanshyam
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p. 1037 - 1038
(2007/10/02)
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- Derivatives of 4,6 dioxopyrido[3,2-g]quinoline 2,8 dicarboxylic acid
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Novel chemical compounds of the formula: SPC1 Wherein R is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, phenyl, alkali metal, or an amine cation; X and Y can be the same or different and are selected from the group consisting of hydrogen, alkyl of from one to six carbon atoms, inclusive, cycloalkyl of 5 or 6 carbon atoms, inclusive, phenyl, hydroxyl, alkoxy having from one to three carbon atoms, inclusive, halogen, trifluoromethyl, cyano, carboxyamide and O C-OQ, EQU1 where Q is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, alkali metal, and an amine cation, with the proviso that where R is hydrogen, alkali metal or an amine cation, then Q is the same as R, and where R is phenyl or alkyl from one to three carbon atoms, then Q is phenyl or alkyl from one to three carbon atoms; and Z is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, and phenyl. The compounds are formulated with pharmaceutical carriers for oral or parenteral administration, with insufflation being the preferred method. The compositions are useful in the prophylactic treatment of sensitized humans and mammals for allergy and all anaphylactic reactions of a reagin or non-reagin mediated nature.
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- Oxanilic acids, a new series of orally active antiallergic agents
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A large number of oxanilic acid esters and N heteroaryl oxamic acid esters were prepared and found to have antiallergic activity using the rat passive cutaneous anaphylaxis (PCA) test. Many of the oxanilic acid esters are active orally, with the most active species having an aryl 2' carbamoyl group and a 3' methoxy group. Hydrolysis of the ester from the oxanilic ester moiety causes a loss of oral activity.
- Sellstedt,Guinosso,Begany,Bell,Rosenthale
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p. 926 - 933
(2007/10/05)
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