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Monoamine Inhibitors: Shaomeng Wang
Fri Aug 26, 2005 1:43 am |
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Istvan J. Enyedy, Wahiduz A. Zaman, Sukumar Sakamuri, Alan P. Kozikowski, Kenneth M. Johnson, and Shaomeng Wang. "Pharmacophore-Based Discovery of 3,4-Disubstituted Pyrrolidines as A Novel Class of Monoamine Transporter Inhibitors." Bioorg. Med. Chem. Lett. 2001, 11, 1113-1118.
Shaomeng Wang, Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Jacek. Mamczarz, Bidhan C. Bandyopadhyay, Srihari R. Tella, Wahiduz A. Zaman, Kenneth M. Johnson. "Molecular Modeling, Structure-Activity Relationships, Pharmacological and Behavioral Pharmacological Studies of 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-Methylphenyl Ketones as a Novel Class of Dopamine Transporter Inhibitors." Bioorg. Med. Chem. 2001, 9, 1753-1764.
Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Wahiduz A. Zaman, Kenneth M. Johnson and Shaomeng Wang. "Discovery, Synthesis and Biological Evaluation of 4-Phenyl-1-Arylalkyl Piperidines as Dopamine Transporter Inhibitors." Bioorg. Med. Chem. Lett. 2001, 11, 495-500.
Hello, if anybody can access Science Direct i'd like the above 3 articles. There are a couple of other articles I am seeking but i appreciate any feedback
Joseph Ratzinger |
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re: Monoamine Inhibitors: Shaomeng Wang
Sat Sep 03, 2005 3:25 am |
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Seriously now guys, i'd like these articles as well:
Pavel A. Petukhov, Mei Zhang, SAR Studies of Piperidine-Based Analogues of Cocaine. Part 3: Oxadiazoles. Bioorganic and Medicinal Chemistry Letters 2001, Volume 11, Issue 16, pp 2079-2083.
Paval A. Petukhov, Jianrong Zhang, SAR Studies of Piperidine-Based Analogues of Cocaine. 4. Effect of N-Modification and Ester Replacement. Journal of Medicinal Chemistry, 2002, Volume 45, Number 15, pp 3161-3170.
Lomenzo SA, Rhoden JB, Synthesis and Biological Evaluation of Meperidine Analogues at Monoamine Transporters. Journal of Medicinal Chemistry, 2005, Volume 48, Number 5, pp 1336-1343.
The pair of medicinal chemistry documents are particularly valuable to me. I can obtain them but i'd appreciate cooperation on this matter. I'll trade an eye for an eye, a tooth for a tooth. |
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Lego
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| Joined: 15 Apr 2005 |
| Posts: 55 |
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2506.80 Points
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re: Monoamine Inhibitors: Shaomeng Wang
Sun Sep 04, 2005 3:35 am |
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| Give direct links (DOI or similiar) and thou shall receive.... |
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methyl_ethyl
Riedel De Haen
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| Joined: 18 Feb 2005 |
| Posts: 107 |
| Location: Estonia |
7200.76 Points
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re: Monoamine Inhibitors: Shaomeng Wang
Sun Sep 04, 2005 8:01 am |
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Hey Stinging Nettle,
The articles you requested love,
Nettle 1
SAR Studies of Piperidine-Based Analogues of Cocaine. 4. Effect of N-Modification and Ester Replacement
Nettle 2
SAR Studies of Piperidine-Based Analogues of Cocaine.
Part 3: Oxadiazoles
Nettle 3
Synthesis and Biological Evaluation of Meperidine Analogues at Monoamine
Transporters
regards,
m_e |
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re: Monoamine Inhibitors: Shaomeng Wang
Sun Sep 04, 2005 12:19 pm |
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| Thanks for the help. This is appreciated massively. |
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Lego
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| Joined: 15 Apr 2005 |
| Posts: 55 |
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2506.80 Points
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Re: Monoamine Inhibitors: Shaomeng Wang
Sun Sep 04, 2005 2:26 pm |
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| Stinging_Nettle wrote: |
Istvan J. Enyedy, Wahiduz A. Zaman, Sukumar Sakamuri, Alan P. Kozikowski, Kenneth M. Johnson, and Shaomeng Wang. "Pharmacophore-Based Discovery of 3,4-Disubstituted Pyrrolidines as A Novel Class of Monoamine Transporter Inhibitors." Bioorg. Med. Chem. Lett. 2001, 11, 1113-1118.
Shaomeng Wang, Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Jacek. Mamczarz, Bidhan C. Bandyopadhyay, Srihari R. Tella, Wahiduz A. Zaman, Kenneth M. Johnson. "Molecular Modeling, Structure-Activity Relationships, Pharmacological and Behavioral Pharmacological Studies of 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-Methylphenyl Ketones as a Novel Class of Dopamine Transporter Inhibitors." Bioorg. Med. Chem. 2001, 9, 1753-1764.
Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Wahiduz A. Zaman, Kenneth M. Johnson and Shaomeng Wang. "Discovery, Synthesis and Biological Evaluation of 4-Phenyl-1-Arylalkyl Piperidines as Dopamine Transporter Inhibitors." Bioorg. Med. Chem. Lett. 2001, 11, 495-500.
Hello, if anybody can access Science Direct i'd like the above 3 articles. There are a couple of other articles I am seeking but i appreciate any feedback
Joseph Ratzinger
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Anyway, here they are:
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors
Istvan J. Enyedya, Wahiduz A. Zaman, Sukumar Sakamuri, Alan P. Kozikowskid, Kenneth M. Johnson and Shaomeng Wang
Bioorg. Med. Chem. Lett., 2001, 11(9), 1113-1118
http://dx.doi.org/10.1016/S0960-894X(01)00132-9
http://rapidshare.de/files/4706669/Bioorg._Med._Chem._Lett.__2001__11_9___1113-1118.pdf.html
Abstract: 3,4-Disubstituted pyrrolidines were discovered as a novel class of monoamine transporter inhibitors through 3-D database pharmacophore searching using a new pharmacophore model. The most potent analogue 12 has Ki values of 0.084 μM in [3H]mazindol binding, 0.20, 0.23, and 0.031 μM in inhibition of dopamine (DA), serotonin (SER), and norepinephrine (NE) reuptake, respectively. Functional antagonism testing in vitro showed that 11 and 12 are weak cocaine antagonists.
Pharmacophore-Based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors
Sukumar Sakamuri, b, Istvan J. Enyedy, Alan P. Kozikowski, Wahiduz A. Zamane, Kenneth M. Johnson and Shaomeng Wang
Bioorg. Med. Chem. Lett., 2001, 11(4), 495-500
http://dx.doi.org/10.1016/S0960-894X(00)00703-4
http://rapidshare.de/files/4706938/Bioorg._Med._Chem._Lett.__2001__11_4___495-500.pdf.html
Abstract: Pharmacophore-based discovery, synthesis, and structure–activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism.
Molecular Modeling, Structure–Activity Relationships and Functional Antagonism Studies of 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-Methylphenyl Ketones as a Novel Class of Dopamine Transporter Inhibitors
Shaomeng Wang, Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Wahiduz A. Zaman and Kenneth M. Johnson
Bioorg. Med. Chem., 2001, 9(7), 1753-1764
http://dx.doi.org/10.1016/S0968-0896(01)00090-6
http://rapidshare.de/files/4706969/Bioorg._Med._Chem.__2001__9_7___1753-1764.pdf.html
Abstract: We previously disclosed the discovery of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone (3) as a novel class of dopamine transporter (DAT) inhibitors and showed that (±)-3 has a significant functional antagonism against cocaine in vitro. Our previous preliminary structure–activity relationship study led to identification of a more potent DAT inhibitor [(±)-4] but this compound failed to show any significant functional antagonism. To search for more potent analogues than 3 but still displaying significant functional antagonism, further SARs, molecular modeling studies and in vitro pharmacological evaluation of this novel class of DAT inhibitors were performed. Sixteen new analogues were synthesized in racemic form and evaluated as DAT inhibitors. It was found that seven new analogues are reasonably potent DAT inhibitors with Ki values of 0.041–0.30 and 0.052–0.16 μM in [3H]mazindol binding and inhibition of DA reuptake. Chiral isomers of several potent DAT inhibitors were obtained through chiral HPLC separation and evaluated as inhibitors at all the three monoamine transporter sites. In general, the (−)-isomer is more active than the (+)-isomer in inhibition of DA reuptake and all the (−)-isomers are selective inhibitors at the DAT site. Evaluation of cocaine's effect on dopamine uptake in the presence and absence of (+)-3 and (−)-3 showed that (−)-3 is responsible for the functional antagonism obtained with the original lead (±)-3. Out of the new compounds synthesized, analogue (±)-20, which is 8- and 3-fold more potent than (±)-3 in binding and inhibition of DA reuptake, appeared to have improved functional antagonism as compared to (±)-3. |
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re: Monoamine Inhibitors: Shaomeng Wang
Sun Sep 04, 2005 3:05 pm |
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| Thanks again. SWIM will share with you the results of some of his research in the write-up section when he feels that he has got something that is worthy of publishing. |
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re: Monoamine Inhibitors: Shaomeng Wang
Sun Sep 04, 2005 3:39 pm |
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Actually BS to the compounds produced by Wang.
However the Oxadiazole compound looks fairly good |
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