- Synthesis and Fungicidal Activity of Simple Structural 1,3-Thiazolidine-2-Thione Derivatives
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A series of simple structural 1,3-thiazolidine-2-thione derivatives with various substituents on the S-, N-, 4-, and 5-positions was synthesized with high yields from various vicinal amino alcohols via two steps and screened for their antifungal activity. Bioassay results reveal that some thiazolidine-2-thione derivatives show strong antifungal activities against P. capsici, G. zeae, S. sclerotiorum, A. alternata, B. cinerea, or R. solani. The SAR analysis indicates that N-acyl substituted and 4-alkyl substituents can enhance the antifungal activity. Notably, 4-isopropyl-N-propionylthiazoldine-2-thione shows excellent activity against B. cinerea and G. zeae with IC50 values at 3.7 g/mL and 6.5 g/mL, respectively, and 4-isobutyl-N-propionylthiazoldine-2-thione shows remarkable fungicidal activity against R. solani, S. sclerotiorum, and G. zeae with IC50 values at 1.0 g/mL, 12.1 g/mL, and 11.0 g/mL, respectively. GRAPHICAL ABSTRACT.
- Chen, Ning,Du, Hongguang,Liu, Weidong,Wang, Shanshan,Li, Xinyao,Xu, Jiaxi
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p. 112 - 122
(2015/10/29)
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- A versatile synthesis of various substituted taurines from vicinal amino alcohols and aziridines
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Taurine and structurally diverse substituted taurines have been synthesized by peroxyformic acid, oxidation of the thiazolidine-2-thione intermediates generated from, vicinal amino alcohols or aziridines and carbon disulfide. The stereochemistry and mechanisms of the reactions are disscussed. The method is a salt-free and versatile route, convenient in terms of purification, and can be used to synthesize optically active substituted taurines.
- Chen, Ning,Jia, Weiyi,Xu, Jiaxi
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experimental part
p. 5841 - 5846
(2010/03/03)
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- Gene delivery mediated by liposome-DNA complex with cleavable PEG surface modification
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A liposome composition and method for delivery of a nucleic acid in vivo or ex vivo is described. The liposomes in the composition are comprised of (i) a cationic lipid and (ii) a lipid joined to a hydrophilic polymer by a releasable linkage. The liposomes are associated with a nucleic acid for delivery to a cell.
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- GENE DELIVERY MEDIATED BY LIPOSOME-DNA COMPLEX WITH CLEAVABLE PEG SURFACE MODIFICATION
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A liposome composition and method for delivery of a nucleic acid in vivo or ex vivo is described. The liposomes in the composition are comprised of (i) a cationic lipid and (ii) a lipid joined to a hydrophilic polymer by a releasable linkage. The liposomes are associated with a nucleic acid for delivery to a cell.
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Page/Page column 32
(2008/06/13)
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- Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase
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Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.
- Shankaran,Donnelly, Karla L.,Shah, Shrenik K.,Guthikonda, Ravindra N.,MacCoss, Malcolm,Humes, John L.,Pacholok, Stephen G.,Grant, Stephan K.,Kelly,Wong
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p. 4539 - 4544
(2007/10/03)
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- Liposome composition for delivery of nucleic acid
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A liposome composition for delivery of a nucleic acid in vivo or ex vivo is described. The liposomes in the composition are comprised of (i) a lipid that is neutral in charge at physiologic pH and positively charged at pH values less than physiologic pH and (ii) a lipid joined to a hydrophilic polymer by a dithiobenzyl linkage. The liposomes are associated with a nucleic acid for delievery to a cell.
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- Releasable linkage and compositions containing same
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A compound comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-containing ligand through a dithiobenzyl linkage is described.
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- Synthesis and Insecticidal Activity of Oxazaphospholidines, Oxathiaphospholanes, and Thiazaphospholidines
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Fifty-five new five-membered cyclic organophosphorus compounds including oazaphospholidines, thiazaphospholidines, and oxathiaphospholanes were synthesized, which have substituents at 4- or/and 5-positions besides at the 2-position.The thiazaphospholidines showed the highest insecticidal activity followed by oxathiaphospholanes and oxazaphospholidines.The position preference of substituents in insecticidal activity was most obvious in the oxazaphospholidines.It was preferable for insecticidal activity to have the substituent near the more basic atom: the 4-position for thiazaphospholidine and oxazaphospholidine, the 5-position for oxathiaphospholane, with the exception of 4- or 5-phenyl oxazaphospholidine.
- Wu, Shao-Yong,Hirashima, Akinori,Takeya, Ryuko,Eto, Morifusa
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p. 2911 - 2918
(2007/10/02)
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