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Alireza Foroumadi,Fatemeh Soltani,Raheleh Jabini,Mohammad Hasan Moshafi,Fatemeh Mohammadian Rasnani 대한약학회 2004 Archives of Pharmacal Research Vol.27 No.5
Two series of 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-propyl, allyl and propargyl)thio-1,3,4-thiadiazoles (6a-f) and 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1H-imidazol- 2-yl)-5-(nitrobenzyl)thio-1,3,4-thiadiazole derivatives (8a-f) have been synthesized and evaluated against Mycobacterium tuberculosis, as part of the TAACF TB screening program under direction of the US National Institute of Health, the NIAID division. Primary screening was conducted at a single concentration, 6.25 mgmL-1, against M. tuberculosis H37Rv in BACTEC 12B medium, using the Microplate Alamar Blue Assay (MABA). The minimum inhibitory concentration (MIC) was determined for the compounds that demonstrated ³90% growth inhibition in the primary screening. A varying degree of antituberculosis activity (from 0-97% of growth inhibition) was observed with the alkylthio series (6a-f), and the nitroimidazole derivative with a propylthio group (6b) and the nitrofuran derivative with a propargylthio group (6e), were the most active compounds (MIC=3.13 and 1.56 mgmL-1, respectively). Among the nitrobenzylthio derivatives (8a-f), all the ortho, meta and para nitrobenzyl isomers in the nitrofuran series exhibited good antituberculosis activity (MIC=3.13 mgmL-1), while the corresponding nitroimidazole analogues were completely inactive (Inhibition=0%).
Alireza Foroumadi,Loghman Firoozpour,Saeed Emami,Shahla Mansouri,Abdolrasoul H. Ebrahimabadi,Ali Asadipour,Mohsen Amini,Nosratollah Saeid-Adeli,Abbas Shafiee 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
A series of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives (4a-l) have been synthesized by reaction of piperazinyl quinolones with 5-chloro-2-(chlorobenzylthio)- 1,3,4-thiadiazoles. Their structures were confirmed by elemental analysis, IR and NMR spectra. The antibacterial activities of 4a-l against a variety of Gram-positive and Gram-negative bacteria were determined. Several compounds showed a good antibacterial activity against Gram-positive bacteria among which, compound 4e with a 2-chlorobenzylthio moiety in ciprofloxacin derivative, exhibited high activities against Staphylococcus aureus and Staphylococcus epidermidis (MIC=0.06 µg/mL). The structure-activity relationship (SAR) study revealed that the position of chlorine atom on benzyl moiety would dramatically affect the antibacterial activities of the synthesized compounds.
Cytotoxic Activity Evaluation and QSAR Study of Chromene-based Chalcones
Loghman Firoozpour,Alireza Foroumadi,Najmeh Edraki,Maryam Nakhjiri,Saeed Emami,Maliheh Safavi,Sussan Kabudanian Ardestani,Mehdi Khoshneviszadeh,Abbas Shafiee 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.12
Chalcone and chromene motifs are synthetic or naturally occurring scaffolds with significant cytotoxic profile. Two types of novel regioisomeric chromene-chalcone hybrids, namely 1-(6-chloro or 6-methoxy-2H-chromen-3-yl)-3-phenylprop-2-en-1-one (Type A) and 3-(6-chloro or 6-methoxy-2H-chromen-3-yl)-1-phenylprop-2-en-1-one (Type B), both with different substituents on the phenyl ring attached to propenone linkage, have been evaluated for their cytotoxic activity against breast cancer cell lines (MCF-7 and MDA-MB-231). The results indicate that type A of chromene-chalcones demonstrated better cytotoxic profile than type B especially in MDA-MB-231 cell line. In addition, the growth inhibitory activity of most of the target compounds is higher than Etoposide as a reference drug. QSAR analysis of these novel compounds demonstrated that topological and geometrical parameters are among the important descriptors that influence the cytotoxic activity profile of compounds.
Khoobi, Mehdi,Ramazani, Ali,Foroumadi, Alireza,Souldozi, Ali,Ś,lepokura, Katarzyna,Lis, Tadeusz,Mahyari, Amir,Shafiee, Abbas,Joo, Sang Woo WILEY‐VCH Verlag 2013 Helvetica chimica acta Vol.96 No.5
<P><B>Abstract</B></P><P>Dialkylammonium dicyano(7‐methyl‐6‐oxo‐6<I>H</I>‐dibenzo[<I>b</I>,<I>d</I>]pyran‐9‐yl)methanides <B>4a</B>–<B>4j</B> are obtained in good yields <I>via</I> a simple reaction between 3‐acetylcoumarins (=3‐acetyl‐2<I>H</I>‐1‐benzopyran‐2‐ones) <B>1</B> and malononitrile (<B>2</B>) in EtOH (<I>Table 1</I>). In this reaction, a charge‐separated zwitterionic salt is formed.</P>
Hassan Aryapour,Majid Mahdavi,Seyed Reza Mohebbi,Mohammad Reza Zali,Alireza Foroumadi 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.9
Previous studies suggest that 4-aryl-4H-chromenes are potent apoptosis-inducing agents in various cancer cell lines. In this study, anti-proliferative and apoptotic effects of the derivatives from 4-aryl-4H-chromene family were investigated in the human leukemia K562 cells using [3-(4,5)-dimethyl-2-thiazolyl]-2,5-diphenyl-2H-tetrazolium bromide (MTT) growth inhibition assay. 3-NC was more active among these compounds with IC50 of 65 nM and was selected for further studies. Apoptosis, as the mechanism of cell death, was investigated morphologically by Hoechst 33258 staining, cell surface expression assay of phosphatidylserine by Annexin V/PI technique,caspase-3 activation assay, as well as the formation of DNA ladder. The K562 cells underwent apoptosis upon a single dose (at IC50 value) of the compound, and also increased caspase-3 activity by more than 2.3-fold, following a 72 h treatment. Caspase-9 was also activated which could be detected 48 hours post-treatment. Furthermore, Western blot analysis revealed that the treatment with the compound down-regulated the expression of certain IAP protein, including survivin. These data further suggest that these derivatives from 4-aryl-4H-chromene may provide a novel therapeutic approach for the treatment of leukemia.
Firoozpour, Loghman,Emami, Saeed,Mansouri, Shahla,Ebrahimabadi, Abdolrasoul H.,Asadipour, Ali,Amini, Mohsen,Saeid-Adeli, Nosratollah,Shafiee, Abbas,Foroumadi, Alireza 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
A series of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolones derivatives (4a-I) have been synthesized by reaction of piperazinyl quinolones with 5-chloro-2-(chlorobenzylthio)-1,3,4-thiadiazoles. Their structures were confirmed by elemental analysis, IR and NMR spectra. The antibacterial activities of 4a-I against a variety of Gram-positive and Gram-negative bacteria were determined. Several compounds showed a good antibacterial activity against Gram-positive bacteria among which, compound 4e with a 2-chlorobenzylthio moiety in ciprofloxacin derivative, exhibited high activities against Staphylococcus aureus and Staphylococcus epidermidis (MIC=0.06 ${\mu}$g/mL). The structure-activity relationship (SAR) study revealed that the position of chlorine atom on benzyl moiety would dramatically affect the antibacterial activities of the synthesized compounds.