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Tarek, Aboul-Fadl,Mohammed, Faragany Abdel-Hamid,Hassan, Ehsan Abdel-Saboor The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.10
N'-(1-alkyl-2,3-dihydro-2-oxo-1H-3-indolyliden)-4-pyridinecarboxylic acid hydrazide derivatives, 3(a-g), were synthesized in a trial to overcome the resistance developed with the therapeutic uses of isoniazid (INH). The lipophilicity of the synthesized derivatives supersedes that of the INH as expressed by Clog p values. The synthesized compounds and INH were tested against bovin, human sensitive and human resist strains of Mycobacterium tuberculosis. Compounds 3a, 3d, 3f and 3g with 1-unsubstituted, 1-propyl, 1-propynyl and 1-benzyl groups respectively exhibited equipotent growth inhibitory activity (MIC 10 $\mu$mol) against the tested strains as compared with INH however the later has no activity against human resist strain. Pharmacokinetic study revealed that the rate and extent of absorption of the tested derivatives (3d and 3f) significantly higher than that of INH (p<0.05). The relative bioavailabilities ($F_R%$) were 183.15 and 443.25 for 3f and 3d respectively as compared to INH. These results preliminary indicate the possible use of the prepared derivatives for treatment of tuberculosis infections in order to overcome the resistance developed with INH.
Hatem A. Abdel-Aziz,Tarek Aboul-Fadl,Abdul-Rahman M. Al-Obaid,Mohamed Ghazzali,Abdullah Al-Dhfyan,Alessandro Contini 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.9
Novel 6-aryl-2-methylnicotinic acid hydrazides 4a-c and their corresponding hydrazones 5a-c and 6a-i were synthesized. X-ray single crystal diffraction of 6h confirmed the chemical structure of hydrazones 6a-i. Antiproliferative activity of the synthetic compounds was investigated against K562 leukemia cell lines. Variable cell growth inhibitory activities were obtained with IC50 range from 24.99 to 66.78 μM where the compound 6c exhibited the maximum activity. Structure activity relationship analysis has been performed and a common pharmacophore model for the synthesized derivatives has been obtained by using the pharmacophore elucidation module of the software MOE. The best model obtained is characterized by two projected locations of potential H-bond donors (F3 and F4) and two Aromatic annotations (F1 and F2).
3,5-Disubstituted Thiadiazine-2-thiones: New Cell-Cycle Inhibitors
Awwad A. Radwan,Tarek Aboul-Fadl,Abdullah Al-Dhfyan,Mohammed K. Abdel-Hamid,Abdullah A. Al-Badr 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.1
Two series, a and b, of 3-cyclopentyl or (3-cyclohexyl)-5-substituted-3,4,5,6-tetrahydro-2H-1,3,5-thiadiazine-2-thiones (THTT) 2a-9a and 3b, 4b, 6b-9b, were synthesized to develop new cell cycle inhibitors. Variable and promising in vitro antiproliferative activities were shown with the synthesized THTT derivatives. Compound 5a with a 5-cyclopentyl group on position-3 and a glutamine residue on position-5 of the THTT moiety showed maximum activity (IC50 = 8.98 μM). Compound 5a possessed notable cell cycle disrupting and apoptotic activities with enhanced selectivity against cancer cells, suggesting the potential for the development of new selective cell cycle inhibitors. There is no evident relationship between the cytotoxic activity of the tested compounds and their lipophilicity. In addition, a pharmacophore based study was performed to explain the biological activity on structural bases. A successful model was generated with a good correlation with the observed activity.
Hajjaj H. M. Abdu-Allah,Bahaa G. M. Youssif,Mostafa H. Abdelrahman,Mohammed K. Abdel-Hamid,Rudraraju Srilakshmi Reshma,Perumal Yogeeswari,Tarek Aboul-Fadl,Dharmarajan Sriram 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.2
The antitubercular drug; para-aminosalicylicacid (PAS) was used as the core scaffold for the design of aseries of 1H-1,2,3-triazolylsalicylhydrazones upon couplingwith triazole and arylhydrazone moietis to furnish asingle molecular architecture. The obtained derivativeswere screened against Mycobacterium tuberculosis H37Rvrevealing good to high activity for the active compounds(MIC values of 0.39–1.5 lg/mL) compared to the marketeddrugs isoniazid, rifampicin and ethambutol. Moreover, themost active analogue N-(1-(4-chlorobenzyl)-2-oxoindolin-3-ylidene)-2-hydroxy-4-(4-phenyl-1H-1,2,3-triazol-1-yl)-benzohydrazide (20) was found to be ten-fold more potentthan PAS and equipotent to rifampicin (MIC 0.39 lg/mL),while exhibiting low cytotoxicity with a selectivity indexof[128. In addition, this compound was shown to beactive against persistent forms of mycobacteria comparableto standard drugs in nutrient starvation model. Accordingly,we introduce compound 20 as a valuable lead forfurther development. A 3D-QSAR study was also conductedto help in explaining the observed activity and toserve as a tool for further development.