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Novel lead generation through hypothetical pharmacophore three-dimensional database searching: discovery of isoflavonoids as nonsteroidal inhibitors of rat 5 alpha-reductase.
- G. S. Chen, C. S. Chang, W. Kan, C. L. Chang, K. Wang, J. Chern
- Chemistry, Medicine
- Journal of medicinal chemistry
- 10 October 2001
This investigation has demonstrated a practical approach toward the development of lead compounds through a hypothetic pharmacophore via three-dimensional database searching. Expand
Site-directed mutagenesis of cysteinyl and serine residues of human thromboxane A2 receptor in insect cells.
Results indicate that various cysteinyl and serine residues of thromboxane A2 receptor may play different roles in ligand binding. Expand
Effect of hydroxyzine on the transport of etoposide in rat small intestine
The results showed that the transport of etoposide was significantly increased from the luminal site to the serosal site in the jejunum by 2- and 4-fold after 90 min in the presence of hydroxyzine and quinidine, respectively. Expand
Selective N-debenzylation of amides with p-TsOH
Abstract N -Benzylamides were debenzylated efficiently with 4 equiv. of p -TsOH in refluxing toluene. Good to quantitative yields of the desired primary amides were obtained within 2–4 h from a wide… Expand
Monoclonal anti-idiotypic antibody to a potent thromboxane A2 receptor antagonist and its interaction with thromboxane A2 receptor.
3D-9E-12 acts as a specific antagonist in the thromboxane A2 receptor, and attenuated U46,619-induced increase in [35S]guanosine 5'-O-(thiotriphosphate) binding and GTPase activity in human platelet membranes. Expand
Design and Synthesis of 3-Aryl-5-Alicylic-(1,2,4)-oxadiazoles as Novel Platelet Aggregation Inhibitors
A series of 4-[2-(alicyclic-[1,2,4]oxadiazol-3-yl)phenoxy]-butyric acids were synthesized from N-hydroxy-2-isopropoxy benzamidine in 4 steps with good yields. These [1,2,4]oxadiazoles are novel… Expand
Improved synthesis of (5Z)-7-(3-endo-[(benzenesulfonamido)-bicyclo[2.2.1]heptyl]hept-5-enoic acid (S-145) derivatives and their iodine-125-labeled radioligands for the study of thromboxane A2…
An improved synthetic scheme for (5Z)-7-(3-endo-[(benzenesulfonamido)-bicyclo[2.2.1]heptyl)hept-5-enoic acid (S145) and its analogs has been designed and both were found to be valuable radioligands for studying thromboxane A2 (TXA2) receptor. Expand
Synthesis of 2‐[4‐(Imidazolin‐2‐Ylideneamino)Benzyl]‐Indan‐1‐Ones as Novel Potent Prostacyclin Antagonists
Prostacyclin is involved in many pathological conditions, such as sensitization of inflammation induced pain and isovolumetic distention. Therefore, antagonism of prostacyclin action may be useful in… Expand
One‐Pot Synthesis of Ene‐Lactams via N‐Debenzylation of Keto‐Containing N‐2,4‐Dimethoxylbenzylamides
Abstract A general method of ene‐lactam preparation is described. Ene‐lactams can be prepared efficiently from keto‐containing N‐2,4‐dimethoxylbenzylamides in good to excellent yields. This method is… Expand