- SUBSTITUTED HETEROCYCLIC INHIBITORS OF LYSINE BIOSYNTHESIS VIA THE DIAMINOPIMELATE PATHWAY
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The present invention relates to certain heterocyclic compounds of Formula (I) that have the ability to inhibit lysine biosynthesis via the diaminopimelate biosynthesis pathway in certain organisms. As a result of this activity these compounds can be used in applications where inhibition of lysine biosynthesis is useful. Applications of this type include the use of the compounds as herbicides. Formula (I)
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- GADOLINIUM BEARING PCTA-BASED CONTRAST AGENTS
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The present invention relates to the RRR/SSS pair of enantiomers of the of Gd(PCTA-tris-glutamic acid), the single enantiomers of the pair, the pharmaceutically acceptable salts thereof, their amide derivatives, and compositions comprising at least 50% of these compounds.
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- COMPOSITION COMPRISING BISTHIOLACTONES AND PROCESS FOR TREATING KERATIN MATERIALS USING SAME
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The present invention relates to i) a process for treating keratin materials, in particular human keratin fibres, comprising the application of a composition comprising at least one bisthiolactone of formula (I), in particular for shaping keratin fibres and/or straightening/relaxing, ii) a composition comprising the bisthiolactone(s) of formula (I), iii) novel bisthiolactones of formula (I), iv) a process for preparing the novel bisthiolactones of formula (I), and v) the use of said bisthiolactones in cosmetics. In which formula (I), R1, R2, R3, R4, X, X', Y, Y', A, A', B, a, b, c, and d are as defined in the description.
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Page/Page column 26; 29
(2018/07/29)
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- Synthesis of 2-(Quinoxalin-2-ylamino-benzotriazolyl) Pentanedioic Derivatives as Potential Anti-Folate Agents
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Anti-folate agents had a significant impact on therapeutic treatment plans for diseases such as cancer, and bacterial and parasitic infections, notably malaria. Quinoxaline derivatives showed in vitro anticancer activity and were able to inhibit both the dihydrofolate reductase and thymidylate synthase. Here, we decided to combine the chemical properties of quinoxalines and quinoxaline 1,4-dioxides with those of benzotriazole nucleus with the aim to evaluate the resulting biological properties. Two main new series, including more than 60 compounds, were prepared. In the first one, the benzotriazole moiety was linked through the nitrogen atoms 1, 2, or 3, to a glutaric acid substituent to simulate a glutamic moiety. In the second series, the glutaric acid was substituted with acetic acid moiety to evaluate the effects of steric hindrance. Here, we describe the multistep chemical processes to obtain all titled quinoxalines starting from commercially available diamines. The classical oxidation of selected quinoxalines was unsuccessful, and we have come to an independent synthetic pathway to obtain new derivatives linked to the benzotriazole moieties starting from synthons bearing N-oxide functionality.
- Briguglio,Piras,Corona,Pirisi,Burrai,Boatto,Gavini,Rassu
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p. 1721 - 1737
(2016/11/23)
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- Preparation of carboxythiolactones and their active derivatives
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The design of peptidyl immunogens requires that a number of elements be covalently linked to enable the appropriate immune response to occur. Two of these elements are: (a) T-cell sequences which after processing, bind to major histocompatibility complex (MHC) molecules and T-cell receptors and (b) B-cell sequences which embody the constellation of atoms which will ultimately be recognized by the desired antibody. Our concept, designed to effectuate this, involved a single molecule which could conjugate three peptides, potentially in discrete steps, in one pot. Activated carboxythiolactones, hitherto unknown entities, provide such a system: two acyl sites susceptible to nucleophilic attack at disparate rates and a liberated thiol susceptible to electrophilic alkylation. Such a set of thiolactones and their derivatives have been synthesized from inexpensive starting materials and their reactivities are under investigation. If successful, the system will not only obviate the difficult syntheses of longer linear peptides, but will also allow a rapid structural permutation of the various elements.
- Garbiras, Bonnie J.,Marburg, Stephen
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p. 270 - 274
(2007/10/03)
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