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Ghandi M.,University of Tehran | Kia M.A.,University of Tehran | Sadeghzadeh M.,Radioisotope Research Group | Bozcheloei A.H.,Radioisotope Research Group | Kubicki M.,Adam Mickiewicz University
Journal of Heterocyclic Chemistry | Year: 2014

The synthesis of novel pyrrolidine or pyrrolizine-fused benzosultams is described. A number of (E)-N-(2-formylphenyl)-N-alkyl-2-phenylethenesulfonamides derivatives were synthesized and subjected to intramolecular [3+2] cycloaddition with azomethine ylides derived in situ from the reaction with sarcosine, phenylglycine, and L-proline. copy; 2014 HeteroCorporation. Source

Ghandi M.,University of Tehran | Sheibani S.,Radioisotope Research Group | Sadeghzadeh M.,University of Tehran | Sadeghzadeh M.,Radioisotope Research Group | And 2 more authors.
Journal of the Iranian Chemical Society | Year: 2013

An efficient catalyst-free and diastereoselective synthesis of novel dihydropyrano[2,3-d]pyrimidine and dihydropyrano[3,2-c]chromen-annulated benzosultams is described. A number of (E)-N-(2-formylphenyl)-N-methyl-2- phenylethenesulfonamides were synthesized and underwent a one-pot domino Knoevenagel hetero-Diels-Alder reaction, respectively, with N,N- dimethylbarbituric acid and 4-hydroxycoumarin in water, giving the desired products, in moderate to excellent yields. © 2013 Iranian Chemical Society. Source

Sadeghzadeh M.,Radioisotope Research Group | Sadeghzadeh M.,University of Tehran | Sheibani S.,Radioisotope Research Group | Ghandi M.,University of Tehran | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2013

This study presents the synthesis and biological evaluation of a new series of arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as sigma receptor ligands. It was found that a number of halogen substituted sulfonamides display relatively high and low affinities to σ1 and σ2 receptors, respectively. The σ1 affinities and subtype selectivities of four piperidine derivatives were also found to be generally comparable to those of piperazine analogues. Compared to σ1-Rs compounds with n = 0 and 2, those with n = 1 proved to have optimal length of carbon chain by exhibiting higher affinities. Within this series, the 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine sigma ligand was identified with 96-fold σ1/σ2 selectivity ratio (Kiσ1 = 0.96 ± 0.05 nM and K iσ2 = 91.8 ± 8.1 nM). © 2013 Elsevier Inc. All rights reserved. Source

Sadeghzadeh M.,Radioisotope Research Group | Sadeghzadeh M.,Islamic Azad University at Karaj | Charkhlooiea G.,Radioisotope Research Group | Charkhlooiea G.,Islamic Azad University at Karaj | Johari Daha F.,Radioisotope Research Group
Iranian Journal of Pharmaceutical Research | Year: 2013

Two deoxyglucose (DG) derivatives, (a,/?)-2-deoxy-2-amino(ethylcarbamate)-D-glucose (ECB-DG) and (a,/)-2-deoxy-2-amino(1,2-dihydroxypropyl)-D-glucose (DHP-DG), were synthesized and radiolabeled successfully with [99mTc(H2O)3(CO)3]+ complex. [99mTc]-ECB-DG and [99mTc]-DHP-DG complexes were prepared (96% and 93% radiochemical purities respectively) by using 46 mCi of Na99mTcO4 in 1 mL saline. Radio-HPLC analysis of [99mTc]-ECB-DG at pH = 7.4, revealed that labeling with 99mTc leads to formation of one radiochemical species with tR = 381 second. Three radiochemical species, Na99mTcO4, [99mTc]-DHP-DG and [99mTc(H2O)3(CO)3]+ complexes with tR = 342 sec, tR = 567 sec and tR = 1586 sec respectively, were obtained when [99mTc]-DHP-DG complex evaluated by HPLC. Biodistribution of two complexes were studied on normal mice at 10, 30 and 60 min post-injections. Compared to the 18F-FDG, [99mTc]-ECB-DG displayed a 2.8-fold reduction in brain uptake (1.7 ± 0.2 versus 0.61% ± 0.09),whereas [99mTc]-DHP-DG just showed 1.9-fold reduction in heart uptake (2.2 ± 0.05 towards 1.16±0.10) at 1 h post-injection. On the basis of our results, it seems that ECB-DG and DHP-DG analogues could be used as brain and heart imaging agent respectively. © 2013 by School of Pharmacy. Source

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