• Bulletin of the Korean Chemical Society
• /
• v.9 no.4
• /
• pp.236-240
• /
• 1988

A thioamide, N-5-trifluoromethyl-6-methoxy-1-thionaphthoyl-N-m ethylglycine, undergoes trans${\rightleftharpoons}$cis photoisomerization around C-N bound in solution. Azulene quenching studies showed the photoisomerization to proceed via both singlet and triplet excited states.The total quantum yield of the trans${\rightarrow}$cis photoisomerization is about 0.26, 0.14 from the singlet excited state and 0.12 from the triplet excited state. Intersystem crossing and internal conversion quantum yields were calculated from sensitized photostationary state and a plausible mechanism is proposed.

• Journal of the Korean Chemical Society
• /
• v.36 no.2
• /
• pp.185-190
• /
• 1992

Near-IR spectra for $ν_{\alpha}$+ Amide Ⅱ combination band of thioamides, and very dilute thioamide-DMSO solution in CCl4 were recorded in the temperature range of $5^{\circ}C$ to $55^{\circ}C$. This combination band was resolved by the computer program into two Lorentzian-Gaussian product function which have been identified with monomeric thioamide and thioamide-DMSO 1 : 1 complex. Equilibrium constants and thermodynamic parameters for the thioamide-DMSO hydrogen bonding were elucidated by the analysis of conce ntration and temperature dependent spectra. The hydrogen bonding strength between thioacetamide (TA) and DMSO in $CCl_4$ is stronger than that between thiopropionamide (TPA) and DMSO in CCl4. The ${\Delta}H^{\circ}$ for the TA-DMSO and TPA-DMSO 1 : 1 complex in CCl4 were -15.3 kJ${\cdot}$$mol^{-1}$ and -14.2 kj${\cdot}$$mol^{-1}$, respectively.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.11
• /
• pp.3318-3326
• /
• 2010

Five new series of 3,4-ethylenedioxythiophene derivatives carrying important pharamacophores, viz., amide, ester, ether and active secondary aryl moieties have been designed and synthesized through multistep reactions starting from thiodiglycolic ester and diethyl oxalate. They have been characterized by elemental and spectral data. All the target compounds have been screened for their anticonvulsant activity at three different models viz. maximal electroshock (MES), subcutaneous metrazole (scMET), and 6 Hz screen and evaluated for their neurotoxicity in rotorod model. Compound 6a emerged as lead with no neurotoxicity. All the five series of compounds are safe in the toxicity studies at the maximum dose of 300 mg/kg of body weight. Amongst the tested compounds, the ester pharmacophore with thioamide fragment has showed better activity than the other analogs.

• Bulletin of the Korean Chemical Society
• /
• v.8 no.1
• /
• pp.56-58
• /
• 1987

• Proceedings of the Korean Society of Life Science Conference
• /
• 2001.09a
• /
• pp.48-48
• /
• 2001

• Journal of Life Science
• /
• v.9 no.2
• /
• pp.49-51
• /
• 1999

Reactions of 2,6-Lutidine with active methyl group anilines in the presence of sulfur gave the desired thioamides 1. Reactions of synthesized thioamides 1 with sulfur and SiO2 or SeO2 gave the corresponding amide 2. We now report conversion of thioamide to amide by using oxidzing inorganic reagant

• Bulletin of the Korean Chemical Society
• /
• v.32 no.4
• /
• pp.1201-1203
• /
• 2011

A one-pot conversion of tertiary thioamides to S-2-oxo thioesters is reported. Hence, tertiary thioamides were reacted with ${\alpha}$-halo ketones or acids under solvent-free conditions to produce the corresponding oxo-thioesters in good to excellent yields.

• Bulletin of the Korean Chemical Society
• /
• v.27 no.9
• /
• pp.1353-1358
• /
• 2006

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

• Journal of Pharmaceutical Investigation
• /
• v.12 no.4
• /
• pp.132-144
• /
• 1982

The inclusion of ${\beta}-cyclodextrin$ $({\beta}-CyD)$ with prothionamide in aqueous phase was investigated by circular dichroism(CD), ultraviolet (UV) absorption, and solubility technique. The results suggested that a region of drug chromophore was located within the asymmetric center of ${\beta}-cyclodextrin$. Solubility and spectral changes were quantitatively treated to obtain stoichiometric ratio, which was found to be 1 : 1, and formation constants which were determined by solubility, CD, and UV method were 257, 367, and 389 $M^{-1}$, respectively. Also, the formation constant of the inclusion complex was determined by CD method at various pH. The result was that $K_c$ depended upon the pH of medium, and this fact also supported that thioamide moiety was accomodated in the cavity of ${\beta}-cyclodextrin$.

• The Korean Journal of Pesticide Science
• /
• v.3 no.3
• /
• pp.6-10
• /
• 1999

New series of pyridylimidazolinorus substituted with N-(2-hydroxyethyl)-${\alpha}$-dicarbonylamide group, N-ethoxycarbonylthioamide and N-benzoylthioamide group in place of carboxyl group at 3-position of pyridine were prepared, and their herbicidal effects were tested(in vivo) in upland conditions. Most of pyridylimidazolinones substituted with hydroxydiketoamide and N-ethoxycarbonylthioamide group at 3-position of pyridine showed good herbicidal effects at a rate of 250 g/ha, while pyridylimidazolinone substituted with N-benzoylthioamide group showed no herbicidal effects.