- Cardiosulfa, a small molecule that induces abnormal heart development in zebrafish, and its biological implications
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A change of heart: Cardiosulfa, a small molecule that induces heart deformation during zebrafish development, has been identified by using a forward chemicalgenetic approach. Zebrafish embryos exposed to cardiosulfa have a narrow and elongated heart within an enlarged pericardial sac (see picture; heart marked with green fluorescent protein).
- Ko, Sung-Kyun,Jin, Hui Juan,Jung, Da-Woon,Tian, Xizhe,Shin, Injae
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supporting information; experimental part
p. 7809 - 7812
(2010/04/05)
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- Synthesis and anticandidal activity of azole-containing sulfonamides
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Twenty five benzenesulfonamides containing one imidazole or triazole ring, or two imidazole or triazole rings have been synthesized and evaluated as anticandidal agents. The most active compounds were 5c, 6b, 6c, 6e, and 17b, which exhibited MIC values of 4.55-24.39 mM depending on the clinical isolate. Comparing imidazole to triazole derivatives did not show a clear effect on activity. Compounds containing a N-benzyl group also showed no clear evidence on activity given the fact that they have an extra aromatic ring. Secondary sulfonamides, 5l, 5m, and 5n showed activities that were proportional to their lipophilicity. The activities of N-aryl-substituted derivatives 5j, 5k, 5l, 5m, 5n, and 6j were also proportional to their lipophilicity. Halogenation enhanced the activity as a result of improvement of lipophilicity. The presence of two imidazole or triazole rings in the same compound did not show a clear enhancement of activity.
- Qandil, Amjad M.,Hassan, Mohammad A.,Al-Shar'i, Nizar A.
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experimental part
p. 99 - 112
(2009/04/03)
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- 2-Anilino-4-(Heterocyclic) Amino-Pyrimidines
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The present invention relates to 2-arylamino-4-(heterocyclic)aminopyrimidines inhibitors which are inhibitors and therefore inhibit Protein Kinase C-alpha (PKC-α). The PKC-α inhibitors of the present invention are important for improving myocardial intracellular calcium cycling, resulting in improved myocardial contraction and relaxation performance and thereby slowing the progression of heart failure. The present invention further relates to compositions comprising said 2-arylamino-4-(heterocyclic)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure.
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Page/Page column 23; 24
(2008/06/13)
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- Synthesis of polymer-bound 4-acetoxy-3-phenylbenzaldehyde derivatives: Applications in solid-phase organic synthesis
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(Chemical Equation Presented) Aminomethyl polystyrene resin was reacted with 4-(5′-formyl-2′-hydroxyphenyl)benzoic acid and 4-(5′-formyl-2′-hydroxyphenyl)phenyl propionic acid, respectively, in the presence of 1-hydroxybenzotriazole and 1,3-diisopropylcarbodiimide to yield polymer-bound benzaldehydes. The phenolic group in resins was acetylated with acetic anhydride to afford two polymer-bound 4-acetoxybenzaldehydes. The reductive amination of polymer-bound linkers by amines and sodium triacetoxyborohydride, followed by sulfonylation with arylsulfonyl chloride derivatives in the presence of pyridine and the cleavage with TFA/DCM/H 2O, produced pure sulfonamides.
- Kumar, Anil,Ye, Guofeng,Ahmadibeni, Yousef,Parang, Keykavous
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p. 7915 - 7918
(2007/10/03)
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- Antifungal activities of N-arylbenzenesulfonamides against phytopathogens and control efficacy on wheat leaf rust and cabbage club root diseases.
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A set of N-arylbenzenesulfonamides with various substituents at the arylamine and benzenesulfonyl positions were prepared, and their antifungal properties were measured in vitro against such plant pathogenic fungi as Pythium ultimum, Phytophthora capsici, Rhizoctonia solani, and Botrytis cinerea. Compounds 3, 4, 8, 9, 10, 14, 16, 18, 20, 21, 24 and 27 had antifungal activity over a broad spectrum of the phytopathogenic fungi tested, where 50% of inhibition (ED50) was in the range of 3-15 microg/ml. Based on the in vitro activity, six derivatives (3, 4, 10, 18, 21 and 27) were selected and tested further for their fungicidal efficacy in vivo. The fungicidal efficacy of 10, 21 and 27 had a disease control value of over 85% at 50 microg/ml against wheat leaf rust, while that of 4 was selective against cabbage club root disease.
- Kang, Jae Gon,Hur, Jong Hyun,Choi, Sung Jun,Choi, Gyung Ja,Cho, Kwang Yun,Ten, Leonid N,Park, Ki Hun,Kang, Kyu Young
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p. 2677 - 2682
(2007/10/03)
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- Catalytic effect of dimethyl sulfoxide and hexamethylphosphoramide on the kinetics of aniline acylation with 3-nitrobenzenesulfonyl chloride
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The kinetics of acylation of aniline with 3-nitrobenzenesulfonyl chloride in methyl ethyl ketone in the presence of dimethyl sulfoxide and hexamethylphosphoramide were studied. The latter two compounds efficiently catalyze acylation of aniline with aromatic sulfonyl chlorides. The effect of the catalysts was explained in terms of the base and nucleophilic catalysis concepts.
- Kustova,Kuritsyn
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p. 283 - 284
(2007/10/03)
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- Synthesis of 3-Methyl-1-Phenyl-5-Pyrazolones Containing Arylaminosulfonyl Groups
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N-Aryl-substituted 3(4)-aminobenzenesulfonamides were synthesized.They are the starting compounds for the production of the corresponding substituted 3(4)-(3-methyl-5-oxo-2-pyrazolin-1-yl)-N-phenylbenzenesulfonamides.Data from the IR, PMR, and mass spectra are presented, and the fragmentation of the molecules is discussed.
- Lisitsyn, V. N.,Sazonchik, O. B.
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p. 780 - 784
(2007/10/02)
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