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New asymmetric ligands have been synthesized by condensing o-phenylene diamine with CS2 and PhCHO/MeCHO, and their complexes with MnII, CoII, NiII, CuII and ZnII were prepared and characterized by elemental analyses, conductivity measurements, i.r., u.v.–vis., e.p.r. and n.m.r. spectra. The transition metals in the complexes show square planar geometry and are ionic. Photokinetic studies of the DNA-metal complexes [C10H10S4N2Cu](NO3)2 and [C10H10S4N2Ni](NO3)2 were carried out and the rate constants k(DNA-complex) were calculated. The results indicate that DNA reacts with the metal complex in two steps. DNA first undergoes structural degradation and is then completely hydrolysed as indicated by spectral changes consistent with earlier results. The asymmetric N2S2 macrocyclic metal complexes show a strong propensity for DNA inhibition and can be used as an intercalating binding model. 相似文献
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A new template-directed chiral porphyrin [(TPP)Co(Trp)], where TPP = tetraphenylporphyrin and Trp = 1-tryptophan, was prepared and characterized by various physico-chemical methods. Interaction of [(TPP)Co(Trp)] with calf thymus DNA was studied by u.v.–vis. spectroscopy and cyclic voltammetry. The complex [(TPP)Co(Trp)], after interaction with calf thymus DNA, shows a shift in the absorption spectrum and a large hypochromicity, indicating an intercalating binding mode. This observation was further confirmed by the electrochemical behavior of [(TPP)Co(Trp)] before and after interaction with calf thymus DNA. The complex experiences a negative shift in E
1/2 and a decrease in E
p. The ratio of cathodic to anodic peak currents i
pc/i
pa was 1 for [(TPP)Co(Trp)] while for DNA bound complex i
pc/i
pa 1, suggesting that the calf thymus DNA moiety is bound strongly to the complex [(TPP)Co(Trp)]. Kinetic studies of the DNA-porphyrin complex reveal a psuedo-first order rate law as the plot of k
obs
versus calf thymus DNA is linear passing through the origin. 相似文献
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A new series of 1, 2, 4-triazine derivatives possessing indole nucleus were synthesized with an aim to explore their effect on in vitro growth of microorganisms causing microbial infection. In vitro antimicrobial activity was performed against S. aureus, S. epidermidis, P. mirabilis and E. coli using disk diffusion method. The MIC was detected using the double dilution method. The results were compared by calculating percent inhibition area/μg of the compounds with the standard drug "Ciprofloxacin". Selected compounds were evaluated for toxic effects using human hepatocellular carcinoma (HepG2) cell line by MTT-assay. Results revealed that some compounds of the series were found to exhibit better activity with less toxicity than Ciprofloxacin. 相似文献
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Md Amjad Beg Shivangi Obaid Afzal Md Sayeed Akhtar Abdulmalik S. A. Altamimi Afzal Hussain Md Ali Imam Mohammad Naiyaz Ahmad Sidharth Chopra Fareeda Athar 《Molecules (Basel, Switzerland)》2022,27(14)
The emergence of drug resistance and the limited number of approved antitubercular drugs prompted identification and development of new antitubercular compounds to cure Tuberculosis (TB). In this work, an attempt was made to identify potential natural compounds that target mycobacterial proteins. Three plant extracts (A. aspera, C. gigantea and C. procera) were investigated. The ethyl acetate fraction of the aerial part of A. aspera and the flower ash of C. gigantea were found to be effective against M. tuberculosis H37Rv. Furthermore, the GC-MS analysis of the plant fractions confirmed the presence of active compounds in the extracts. The Mycobacterium target proteins, i.e., available PDB dataset proteins and proteins classified in virulence, detoxification, and adaptation, were investigated. A total of ten target proteins were shortlisted for further study, identified as follows: BpoC, RipA, MazF4, RipD, TB15.3, VapC15, VapC20, VapC21, TB31.7, and MazF9. Molecular docking studies showed that β-amyrin interacted with most of these proteins and its highest binding affinity was observed with Mycobacterium Rv1636 (TB15.3) protein. The stability of the protein-ligand complex was assessed by molecular dynamic simulation, which confirmed that β-amyrin most firmly interacted with Rv1636 protein. Rv1636 is a universal stress protein, which regulates Mycobacterium growth in different stress conditions and, thus, targeting Rv1636 makes M. tuberculosis vulnerable to host-derived stress conditions. 相似文献
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Saraswati S. Velu Irmaizatussyehdany Buniyamin Lee Kiew Ching Dr. Fareeda Feroz Dr. Ibrahim Noorbatcha Dr. Lim Chuan Gee Khalijah Awang Prof. Ibtisam Abd. Wahab Dr. Jean‐Frédéric Faizal Weber Prof. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2008,14(36):11376-11384
Oligostilbenoids are polyphenols that are widely distributed in nature with multifaceted biological activities. To achieve biomimetic synthesis of unnatural derivatives, we subjected three resveratrol analogues to oligomerization by means of one‐electron oxidants. Upon varying the metal oxidant (AgOAc, CuBr2, FeCl3 ? 6 H2O, FeCl3 ? 6 H2O/NaI, PbO2, VOF3), the solvent (over the whole range of polarities), and the oxygenated substitution pattern of the starting material, stilbenoid oligomers with totally different carbon skeletons were obtained. Here we propose to explain the determinism of the type of skeleton produced with the aid of hard and soft acid/base concepts in conjunction with the solvating properties of the solvents and the preferred alignment by the effect of π stacking. 相似文献
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Atta-ur-Rahman Feroz F Zaheer-ul-Haq Nawaz SA Khan MR Choudhary MI 《Natural product research》2003,17(4):235-241
Two new steroidal alkaloids, salonine-A [(20S)-20-(N,N-dimethylamino)-3beta-(tigloylamino)-5alpha-pregn-14-en-2beta,4beta-diol] (1), and salonine-B [(20S)-20-(N,N-dimethylamino)-3beta-methoxy-pregn-5,16-diene] (2), were isolated from the MeOH extract of Sarcococca saligna, along with a known base, alkaloid-C (3). Their structures were elucidated on the basis of spectroscopic methods. All three compounds were found to be cholinesterase inhibitors. 相似文献
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Atta‐ur‐Rahman Zaheer‐ul‐Haq Fareeda Feroz Asaad Khalid SarfrazAhmad Nawaz M.Riaz Khan M.Iqbal Choudhary 《Helvetica chimica acta》2004,87(2):439-448
Seven new steroidal alkaloids, 2‐hydroxysalignarine‐E (=(2′E,20S)‐20‐(dimethylamino)‐2β‐hydroxy‐3β‐(tigloylamino)pregn‐4‐ene; 1 ), 5,6‐dihydrosarconidine (=(20S)‐20‐(dimethylamino)‐3β‐(methylamino)‐5α‐pregn‐16‐ene; 2 ), salignamine (=(20S)‐20‐(methylamino)‐3β‐methoxypregna‐5,16‐diene; 3 ), 2‐hydroxysalignamine (=(20S)‐20‐(dimethylamino)‐2β‐hydroxy‐3β‐methoxypregna‐5,16‐diene; 4 ), salignarine‐F (=(2′E, 20S)‐20‐(dimethylamino)‐4β‐hydroxy‐3β‐(tigloylamino)pregn‐5‐ene; 5 ), salonine‐C (=(2′E,20S)‐20‐(dimethylamino)‐3β‐(tigloylamino)pregna‐4,14‐diene; 6 ), and N‐[formyl(methyl)amino]salonine‐B (=(20S)‐20‐[formyl(methyl)amino]‐3β‐methoxypregna‐5,16‐diene; 7 ) have been isolated from the MeOH extract of Sarcococca saligna, along with the six known alkaloids dictyophlebine ( 8 ), epipachysamine‐D ( 9 ), saracosine ( 10 ), iso‐N‐formylchonemorphine ( 11 ), sarcodinine ( 12 ), and alkaloid‐C ( 13 ). The structures of 1 – 7 were deduced from spectral data. Compounds 1 – 13 demonstrated significant activity against acetyl‐ and butyrylcholinesterase. 相似文献
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A series of asymmetric heterobimetallic complexes of the type [LMLSn]Cl and [LMLSn]Cl2, where L = ethylene diamine, M = MnII, CoII, NiII and CuII, M = CrIII and FeIII and L = 1-tryptophan and 1-valine, have been synthesized and characterized by elemental analyses, u.v.–vis., i.r., e.p.r., n.m.r., cyclic voltammetry and conductivity measurements. The CoIII analogue of these complexes was characterized by two dimensional n.m.r. COSY data. The kinetics of oxygen binding with the complex [C15H23N4O2SnCo]Cl has also been studied. The kinetic data proves that CoII of a coordinated molecule participates in the rate-determining step of the dioxygen binding process. The plots of the pseudo-first-order rate k
obs
versus [O2] are linear passing through an intercept. The electrochemical behaviour of [C15H23N4O2SnCo]2+ and [C15H23N4O2SnCu]+ was monitored by cyclic voltammetry. Comparison of the electrochemical properties of [CoIIISnIV]2+ and [CuIISnIV]+ reveal that, in both the species, one electron transfer reaction takes place. For the [CoIIISnIV]2+ species E
0 = 0.272 and –1.1 V and for the [CuIISnIV]+ species E
0 = 0.078 and –0.300 V values were obtained, respectively. 相似文献
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