Synthesis and herbicidal activities of fluorine-containing 3-pyridylmethyl-2-phenyliminothiazolidine derivatives
摘要:
A series of fluorine-containing 2-phenyliminothiazolidine derivatives were synthesized by a facile and mild method in high yields. The structures of all the title compounds were characterized by H-1 NMR, IR and HRMS. The results of bioassay showed that most of target compounds exhibited efficient herbicidal activities against Echinochloa crusgalli, Sorghum vulgare, Digitaria sanguinalis, Eclipta prostrasta, Cucumis sativus and Brassica campestris at 50 mg L-1. (c) 2005 Elsevier B.V. All rights reserved.
Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
Synthesis and biological evaluation of thiazolidine-2-one 1,1-dioxide as inhibitors of Escherichia coli β-ketoacyl-ACP-synthase III (FabH)
作者:Mamoun M. Alhamadsheh、Norman C. Waters、Donald P. Huddler、Mara Kreishman-Deitrick、Galina Florova、Kevin A. Reynolds
DOI:10.1016/j.bmcl.2006.11.067
日期:2007.2
coli FabH (ecFabH), but not Mycobacteriumtuberculosis FabH (mtFabH) or Plasmodiumfalciparum KASIII (PfKASIII). The activity against ecFabH ranges from 0.9 to >100microM and follows a consistent general SAR trend. Many of the compounds were shown to have antimalarial activity against chloroquine (CQ)-sensitive (D6) P. falciparum (IC(50)=5.3microM for the most potent inhibitor) and some were active against
functionalizations of C60 with amino alcohols with aerobic oxygen as the sole oxidant have been explored. For 2-/3-amino alcohols, an aminooxygenation reactionoccurs to generate fulleromorpholine and fullerooxazepane derivatives. When a tethered furan ring exists, a further intramolecular [4 + 2] reaction with the neighboring double bond occurs to furnish the cis-1 products. In the case of 4-/5-amino
A pyridothienopyrimidine derivative of formula (I),
or the pharmaceutically acceptable salts or N-oxides thereof are disclosed, as well as pharmaceutical compositions comprising said compounds and methods of treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4 using said compounds are disclosed.