Ahmed Mahmoud Alafeefy

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A series of 21 new 2-alkylthio-6-iodo-3-substituted-quinazolin-4-one derivatives was prepared and screened for their in vitro antitubercular activity against Mycobacterium tuberculosis strain H Rv, using the 37 radiometric BACTEC 460-TB methodology. Active compounds were also screened by serial dilution to assess toxicity to a VERO cell line. The results(More)
Medulloblastomas (MBs) constitute an aggressive class of intracranial pediatric tumors. Current multimodality treatments for MBs include surgery, ionizing radiation, and chemotherapy. Toxic side effects of therapies coupled with high incidence of recurrence and the metastatic spread warrant development of more effective, less toxic therapies for this(More)
Tautomerism is an important aspect associated with a variety of pharmacologically and biologically active compounds. It is a challenge to account for tautomerism in computer-aided drug designing (CADD). The estimations and calculations of many physico-chemical properties and theoretical descriptors of the molecules are sensitive to tautomerism. In this(More)
A series of 18 new 3,4-disubstituted-isothiochromeno[3,4-e][1,2]oxazines 28–45 has been obtained from the 3′,4′-di-substituted-4′H-spiro[isothiochromene-3,5′-isoxazol]-4(1H)-ones 10–27 in refluxing HCl acid/ethanol. A series of 15/18 compounds 28–45 was selected by the National Cancer Institute (NCI, Bethesda, USA) and were evaluated against a full panel of(More)
BACKGROUND Colorectal cancer (CRC) is the 3rd most common type of cancer worldwide. New anti-cancer agents are needed for treating late stage colorectal cancer as most of the deaths occur due to cancer metastasis. A recently developed compound, 3c has shown to have potent antitumor effect; however the mechanism underlying the antitumor effect remains(More)
Some novel hydrazone derivatives 6a-o were synthesized from the key intermediate 4-Chloro-N-(2-hydrazinocarbonyl-phenyl)-benzamide 5 and characterized using IR, ¹H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. The inhibitory potential against two secretory phospholipase A₂ (sPLA₂), three protease enzymes and eleven bacterial strains were(More)
An efficient method is described for the synthesis of 2-aminobenzothiazolomethyl naphthol derivatives by one-pot three-component reaction of aldehydes, 2-naphthol, and 2-amino benzothiazole using triton X-100 as a catalyst in water with good yield. The synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, and mass spectra. The synthesized(More)
In the title compound, C(16)H(14)N(2)O(4), the dihedral angle between the aromatic rings is 12.45 (6)°. The central C(=O)-N-N=C bridge is roughly planar (r.m.s. deviation = 0.0346 Å) and makes dihedral angles of 13.01 (7) and 0.56 (7)° with the attached phenyl and benzene rings, respectively. The acetic acid unit (r.m.s. deviation = 0.0066 Å) is twisted(More)
In the title mol-ecular salt, C(16)H(13)N(2)OS(+)·HSO(4) (-), the thia-zolo[3,2-a]benzimidazolium ring system is roughly planar [maximum deviation = 0.046 (3) Å] and makes a dihedral angle of 58.22 (11)° with the benzene ring. The meth-oxy group is almost coplanar with its attached benzene ring [C(meth-yl)-O-C-C = -1.6 (5)°]. In the crystal, the cation is(More)
A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic(More)
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