- Synthesis of 5-Substituted 1H-Tetrazoles Catalyzed by M-SAPO-34 (M = Co, Cu, Mn, Fe, and V) Nanostructures
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Abstract: The synthesis of 5-substituted 1H-tetrazoles by use of a series of M-SAPO-34 (M = Co, Cu, Mn, Fe, and V) nanocatalysts are presented. Following the optimized conditions, Co-SAPO-34 nanocatalyst has been found to effectively catalyze the 5-substi
- Baghershiroudi, Mahrokh,Bafandeh, Fereshteh Taghipour,Safa, Kazem D.,Panahi, Parvane Nakhostin
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p. 230 - 236
(2021/04/09)
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- Triple reuptake inhibitors: Design, synthesis and structure–activity relationship of benzylpiperidine–tetrazoles
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Monoamine transporters are important targets in the treatment of various central nervous disorders. Several limitations of traditional reuptake inhibitors, like delayed onset of action, insomnia, and sexual dysfunction, have compelled the search for safer, more effective compounds. In this study, we have sought to identify novel monoamine reuptake inhibitors. Based upon the docking study of compounds that we had reported previously, aromatic rings (A1) were modified to generate a novel series of benzylpiperidine–tetrazoles. Thirty-one compounds were synthesized and evaluated for their triple reuptake inhibition of serotonin, norepinephrine and dopamine. Triple reuptake inhibitor, compound 2q, in particular, showed potent serotonin reuptake inhibition, validating our design approach.
- Paudel, Suresh,Min, Xiao,Acharya, Srijan,Khadka, Daulat Bikram,Yoon, Goo,Kim, Kyeong-Man,Cheon, Seung Hoon
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p. 5278 - 5289
(2017/10/06)
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- Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: Structure-activity relationship and mechanism of action
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CRM1-mediated nucleocytoplasmic transport plays an important role in many cellular processes and diseases. To investigate the structural basis required for the inhibition of the CRM1-mediated nuclear export we have synthesized analogs of a previously identified small molecule lead compound and monitored their activity against the Rev function of the human immunodeficiency virus. Microscopy studies show that the active congeners of this series inhibit the nucleocytoplasmic transport of Rev and the co-localization between Rev and CRM1 in living cells. Mechanism of action studies show their interaction with the Cys528 residue of CRM1 involving a Michael-addition type of reaction. However, structure-activity relationship demonstrates strict constraints to the structure of the inhibitors, and shows that activity is not solely correlated to Michael-addition suggesting a more complex mechanism of action. Our results are suggestive for the existence of a well-defined interaction at the CRM1-NES binding site. In addition, the most selective congener inhibited the HIV-1 production in latently infected cells. These specific CRM1 inhibitors are of interest as tool for analyzing the mechanisms of post-transcriptional control of gene expression and provide insight in the design of new agents.
- Van Neck, Tine,Pannecouque, Christophe,Vanstreels, Els,Stevens, Miguel,Dehaen, Wim,Daelemans, Dirk
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experimental part
p. 9487 - 9497
(2009/04/11)
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- A Practical Synthesis of 5-Substituted Tetrazoles.
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Nitrosation of N-formyl amidrazones 8a-g with sodium nitrite - aqueous hydrochloric acid gives tetrazoles 10a-g in good yields.
- Boivin, Jean,Husinec, Suren,Zard, Samir Z.
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p. 11737 - 11742
(2007/10/02)
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