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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.
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.
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.
Salman Hassanzadeh,Sepideh Khoee,Loghman Firoozpour 한국고분자학회 2013 Macromolecular Research Vol.21 No.1
The objective of this study was to get an insight into the influence of the newly provided functional groups from the copolymerization as a strategy on the total interactions of the hydrophobic drug and the polyesteric core of the prepared core-shell nanoparticles. Three amphiphile triblock models of monomethoxy poly(ethylene gycol)(mPEG)-b-polyester-b-mPEG with the same PEG hydrophile part but different hydrophobe polyesteric segments were synthesized and used for preparation of the core-shell nanoparticles that were loaded by quercetin as a model hydrophobe drug in the core. The total amount of the interaction between polyesters in the core and loaded quercetin were monitored by parameters such as drug loadings, in vitro release rates and other newly defined parameters such as micelle encapsulation efficiency. The results highlighted that changing the structure of the saturated aliphatic polyesteric core in the poly(butylene adipate) with diol monomers that are capable of forming additional π stacking and π -OH interactions with quercetin weakens the optimal conditions for the main drug-esteric hydrogen bonding. Therefore, the decreased total affinity of the quercetin and polyesteric core finally resulted in the lower amount of encapsulated drug and the increased release rate.