- Synthesis, characterization and crystal structures of two novel sulfa drug Schiff base ligands derived sulfonamide and molecular docking study
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The present paper reports the synthesis of two new sulfa drugs: based Schiff base N-(salicylidene) sulfadiazine = sal-sdzH (1) and N-(salicylidene) sulfathiazole = sal-stzH (2) derived from sulfonamide and substituted salicylaldehyde. These compounds were
- Salehi, Mehdi,Kubicki, Maciej,Galini, Masumeh,Jafari, Mahbobeh,Malekshah, Rahime Eshaghi
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- Nano-synthesis and spectral, thermal, modeling, quantitative structure–activity relationship and docking studies of novel bioactive homo-binuclear metal complexes derived from thiazole drug for therapeutic applications
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Seven novel homo-binuclear Cr(III), Fe(III), Cu(II), ZrO(II), Sn(II), Pb(II) and Ce(III) nanosized complexes of a thiazole drug (H2L) were synthesized for chemotherapeutic applications. H2L was prepared via a condensation reaction be
- Saad, Fawaz A.
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- Synthesis of Schiff base ligand from N-substituted benzenesulfonamide and its complexes: Spectral, thermal, electrochemical behavior, fluorescence quenching, in vitro-biological and in-vitro cytotoxic studies
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Convenient synthesis of new octahedral complexes from 4-amino-N-(1,3-thiazol-2-yl) benzenesulfonamide and 2-hydroxybenzaldehyde with the molecular formula [M(L)2Cl2] (where M = Mn(II), Co(II) and Cu(II) ions) have been described. The
- Valarmathy, Govindaraj,Subbalakshmi, Ramanathan,Sumathi, Rajendran,Renganathan, Rajalingam
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- Bioactive co(Ii), ni(ii), and cu(ii) complexes containing a tridentate sulfathiazole‐based (onn) schiff base
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New Co(II), Ni(II), and Cu(II) complexes were synthesized with the Schiff base ligand obtained by the condensation of sulfathiazole with salicylaldehyde. Their characterization was performed by elemental analysis, molar conductance, spectroscopic techniqu
- Carabet, Alice Carla,Cioater?, Nicoleta,D?buleanu, Irina,Dobri?escu, Aurelian,G?nescu, Anca,Parisi, Filippo,Reiss, Aurora,Rotaru, Mihaela,Rotaru, Petre,Sp?nu, Cezar Ionu?
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- Synthesis, characterization, biological evaluation, and molecular docking approach of nickel (II) complexes containing O, N-donor chelation pattern of sulfonamide-based Schiff bases
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A series of Schiff bases (L1–L4) that possess in their structure bioactive sulfonamide group and their nickel (II) complexes have been synthesized. Microanalytical analyses, various spectroscopic methods such as Fourier transform infrared spectroscopy (FT-IR), 1H nuclear magnetic resonance (NMR), 13C NMR, UV–Vis, and MS, are used to explore the nature of bonding and to elucidate the chemical structures. The analytical and magnetic values suggest a range of stoichiometries 1:1, 1:2, and 2:1 (M:L) for the synthesized complexes of almost square planar geometry. The spectral comparative interpretation reveals that L1 and L2 coordinate to the central Ni (II) in tetradentate ONON donor sequence, whereas L3 and L4 in bidentate ON pattern through deprotonated phenolic-O and the azomethine-N. Density functional theory (DFT) and MOE-docking approaches are used to evaluate the molecular parameters and the binding propensity of the synthesized ligands and their complexes with 3s7s protein and to signify their inhibition strength. Besides, the anticancer, antimicrobial and antifungal activities have been screened against number of tumor cells and human pathogen strains. These in vitro studies reveal that Schiff base L4 and its complex, [Ni(L4-H)(OAc)(H2O)], have superior activities reflecting the importance of inserting bioactive pendant substituents such as thiazole ring and 3-fluorophenylazo to the pharmacophoric sulfonamide moiety. Moreover, some of the synthesized Ni (II) complexes display promising therapeutic effects as novel non-platinum antitumor agents after further preclinical investigations.
- Ramadan, Ahmed M.,Bayoumi, Hoda A.,Elsamra, Rehab M. I.
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- Synthesis of new ?-lactam- N-(thiazol-2-yl)benzene sulfonamide hybrids: Their in vitro antimicrobial and in silico molecular docking studies
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New ?-lactam- N-(thiazol-2-yl) benzene sulfonamide hybrids were synthesized via [2+2] keteneimine cycloaddition (Staudinger reaction) reaction starting from sulfathiazole, a versatilesynthetic precursor. The structures of the newly synthesized compounds w
- Azeez, Hashim Jalal,Aziz, Dara Muhammed
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- Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase
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Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Our group has taken a particular interest in platelet-type 12-(S)-LOX (12-LOX) because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Herein, we report the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino) benzenesulfonamide-based scaffold. Top compounds, exemplified by 35 and 36, display nM potency against 12-LOX, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties. In addition, both compounds inhibit PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells.
- Luci, Diane K.,Jameson, J. Brian,Yasgar, Adam,Diaz, Giovanni,Joshi, Netra,Kantz, Auric,Markham, Kate,Perry, Steve,Kuhn, Norine,Yeung, Jennifer,Kerns, Edward H.,Schultz, Lena,Holinstat, Michael,Nadler, Jerry L.,Taylor-Fishwick, David A.,Jadhav, Ajit,Simeonov, Anton,Holman, Theodore R.,Maloney, David J.
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p. 495 - 506
(2014/02/14)
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