- Synthesis and root growth-inhibitory activity of 2- and 3-(haloacetylamino)-3-(2-furyl)propanoic acids.
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A convenient synthesis of 2- and 3-(chloroacetylamino)-3-(2-furyl)propanoic acids (6a, 7a) and their fluoro analogs were developed. Both 6a and 7a showed 51-55% root growth-inhibitory activity towards rape seedlings at the concentration of 1.0x10(-4) M.
- Kitagawa, Tokujiro,Nakamura, Mizuki,Masai, Katunori
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- PROCESS FOR THE PREPARATION OF 3,6-DICHLOROCYANO PYRAZINE, 3,6-DIOXOPIPERAZINE DERIVATIVES AND PRODUCTION OF FAVIPIRAVIR THEREOF
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The present invention relates to a method of preparing derivatives of 3,6-dichlorocyano pyrazine, 3,6-dioxopiperizin and the production of favipiravir by cyclization and chlorination mediated by ammonia or amine using POCl3 in the presence of pyridine or PCl5. [Formula] In derivatives of 3,6-dioxopiperazine (III), X represents CN, CONH2 or COOR2', R1, R 2 and R2' are individually selected from H, alkyl C1-C12, COOR3 and SO2R3, R 3 being a linear or branched lower alkyl substituted or unsubstituted.
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Paragraph 0038; 0049-0050
(2021/12/31)
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- PERIPHERALLY RESTRICTED GABA POSITIVE ALLOSTERIC MODULATORS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME AND OTHER AILMENTS OF THE PERIPHERAL NERVOUS SYSTEM
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The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.
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Paragraph 0088-0089
(2016/01/12)
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- Inhibitors of Pyrimidine Biosynthesis. Part 1. Synthesis of Potential Transition-state Analogues of Aspartate Transcarbamylase
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A systematic variation of the structure of a transition-state analogue of aspartate transcarbamylase has been carried out.A new, and general, synthesis of these analogues, starting from the appropriate amino-acid is described.
- Goodson, John J.,Wharton, Clifford J.,Wrigglesworth, Roger
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p. 2721 - 2727
(2007/10/02)
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