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Irum Shahzadi Ameer F. Zahoor Azhar Rasul Nasir Rasool Zohaib Raza Shahla Faisal Bushra Parveen Shagufta Kamal Muhammad Zia-ur-Rehman Faisal M. Zahid 《Journal of heterocyclic chemistry》2020,57(7):2782-2794
Theophylline-7-acetic acid (acefylline) ( 3 ) and its derivatives are pharmacologically active compounds and generally recognized as bronchodilators for the treatment of respiratory diseases like acute asthma for over 70 years. In this article, synthesis of 2-((5-((1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-yl)thio)-N-arylacetamides ( 10a-j ) has been reported. All the synthesized derivatives ( 10a-j) were structurally verified by FT-IR, 1H NMR, 13C NMR and evaluated for their anti-cancer (using MTT assay), hemolytic and thrombolytic potential. N-(4-Chlorophenyl)-2-(5-((1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-ylthio)acetamide ( 10g ) was found to be the most active against human liver cancer cell lines (Huh7) having cell viability 53.58 ± 1.28 using 100 μg/mL concentration of compound which was further in-silico modelled to describe the possible mechanistic insights for its anti-proliferative activity. The results of hemolytic and thrombolytic activities indicated that these derivatives were less toxic and hold considerable potential as a drug candidate. 2-(5-((1,3-Dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-ylthio)-N-(2-fluorophenyl)acetamide ( 10c ) of the series was found to be least toxic with 0.1% hemolysis relative to ABTS (95.5%) as positive control. 2-(5-((1,3-Dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-ylthio)-N-(tetrahydro-2H-pyran-4-yl)acetamide ( 10j ) exhibited potent clot lysis activity (90%) as compared to negative control DMSO (0.57%). 相似文献
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Transition Metal Chemistry - A facile synthetic approach has been adopted towards the synthesis of (2R,3R)-N2,N3-bis((S)-1-phenylethyl)butane-2,3-diamine via demetalation of its dichloro Zn(II)... 相似文献
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Mubashir Hassan Balasaheb D. Vanjare Kyou-Yeong Sim Hussain Raza Ki Hwan Lee Saba Shahzadi Andrzej Kloczkowski 《Molecules (Basel, Switzerland)》2022,27(5)
A series of nine novel 1,2,4-triazole based compounds were synthesized through a multistep reaction pathway and their structures were scrutinized by using spectral methods such as FTIR, LC-MS, 1H NMR, and 13C NMR. The synthesized derivatives were screened for inhibitory activity against the mushroom tyrosinase and we found that all the synthesized compounds demonstrated decent inhibitory activity against tyrosinase. However, among the series of compounds, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide exhibited more prominent activity when accompanied with the standard drug kojic acid. Furthermore, the molecular docking studies identified the interaction profile of all synthesized derivatives at the active site of tyrosinase. Based on these results, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide could be used as a novel scaffold to design some new drugs against melanogenesis. 相似文献
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S. Yaqub F. Ahmed Sadiq-ur-Rehman S. Ali S. Shahzadi 《Journal of the Iranian Chemical Society》2009,6(1):88-98
The di- and tri-organotin(IV) complexes of n-butyl hydrogenphthalate and (Z) 3-(4-nitrophenyl)-2-phenyl-2-propenoate were subjected to thermal decomposition by mean of thermogravimetry (TG). The decomposition occurred in steps and the kinetics of every set of reactions was determined using the method described by Coats and Redfern. These results were analyzed to establish the decomposition kinetics and, hence, to calculate the activation energies. The activation energies were also determined by applying the methods described by Horowitz and Metzger, which yielded comparable results. These results confirm that both the ligands act as bidentate in the solid state. 相似文献
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Shabbir Hussain Saira Shahzadi Muhammad Shahid Asif Ali Tahir Syed Mustansar Abbas 《Journal of Coordination Chemistry》2017,70(24):4070-4092
Bimetallic chlorodi-/triorganotin(IV) derivatives of general formulas R2(H2O)SnLCSSSn(Cl)R2 (R=Me: 1; Ph: 2) and R3Sn(Na)LCSSSnR3·H2O (R=Bu: 3; Ph: 4) were prepared by reaction of iminodiacetic acid disodium salt hydrate (Na2LH) with CS2 and R2SnCl2/R3SnCl in methanol. The reaction between Na2LH, CS2, and PdCl2 produced [Na2LCSS]2Pd·2H2O (5) which was treated with R3SnCl to synthesize the heterobimetallic derivatives [R3Sn(Na)LCSS]2Pd·2H2O (R=Me: 6; Ph: 7). The complexes were characterized by microanalysis, spectroscopic, and thermogravimetric analyses. Elemental analysis data, mass fragmentation, and thermal degradation patterns supported the molecular composition of the complexes. FT-IR data indicated monodentate binding of carboxylate while a chelating coordination mode of the dithiocarboxylate was verified in the solid state. A five-coordinate tin(IV) was demonstrated in the solid state. In solution, a tetrahedral/trigonal bipyramidal configuration around Sn(IV) and a square planar geometry of Pd(II) was indicated by multinuclear NMR (1H and 13C) and UV-visible studies. The Pd(II) derivatives showed interaction with salmon sperm-DNA and caused an inhibition of alkaline phosphatase (ALPs). The antibacterial/antifungal potential of the coordination products varied with the nature of incorporated metal and a substitution pattern at tin(IV); the palladium metallation decreased the antimicrobial activities. The triorganotin(IV) products exhibited more powerful action against bacteria/fungi as compared to their diorganotin(IV) counterparts. The complexes displayed sufficiently lower hemolytic effects in vitro as compared to triton X-100 and slightly higher than PBS. 相似文献
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Tanveer Hussain Bokhari Muhammad Bilal Butt Saira Hina Munawar Iqbal Muhammad Daud Muhammad Imran 《Journal of Radioanalytical and Nuclear Chemistry》2017,314(3):1487-1496
The field of therapeutic nuclear medicine is emerging rapidly as choice of treatment in oncology and other cellular malignancies. The growth of this branch of nuclear medicine is greatly facilitated by the introduction of a number of new radiopharmaceuticals and radionuclides. 90Y-radiopharmaceuticals have confirmed their worth in medical and clinical areas in a very short span of time. The 90Y is a radioisotope widely used for therapeutic purposes and considerable perfection has been made to understand the chemistry of 90Y-labeled radiopharmaceuticals. The development of these radiopharmaceuticals can be made favorable by using appropriate buffer, incubation period, optimal pH, specific activity and reaction temperature. In this review, we have discussed the preparation of range of 90Y transporting biological molecules such as antibodies radiolabeled peptides, antigens and microsphere with their clinical applications. 相似文献
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M. Hussain M. Hanif S. Ali S. Shahzadi M. S. Ahmad B. Mirza H. S. Evans 《Journal of the Iranian Chemical Society》2010,7(1):155-163
New organotin(IV) compounds containing the carboxylate ligand 2,3-methylenedioxybenzoic acid (HL) have been synthesized with the general formula R2SnL2 (R = Me, Et, n-Bu, Ph and n-Oct) and R3SnL (R = n-Bu). All compounds have been studied in the solution state by multinuclear NMR (1H, 13C and 119Sn) by using the non-coordinating solvent and also in solid sate by FTIR, mass spectrometry and X-ray crystallography. Spectroscopic data have shown that methylenedioxy moiety does not coordinate with tin atom and the coordination site is actually -COO group, as is proved by X-ray structure determination. The solid state structure of compound (2) has been determined by X-ray crystallography which shows that the complex (2) has distorted octahedral geometry. These complexes have been evaluated in vitro against crown gall tumor and antibacterial activity. Interesting results were noticed during the bio-activity screenings, which proved their in vitro biological potential and possible use as drugs. 相似文献
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Saqib Ali Syed Usman Ahmad Sadiq‐ur‐Rehman Saira Shahzadi Masood Parvez Muhammad Mazhar 《应用有机金属化学》2005,19(1):200-200
A trigonal bipyramidal C2ClS2 coordination geometry for tin is found in Ph2Sn(S2CN(CH2)5)Cl. Copyright © 2005 John Wiley & Sons, Ltd. 相似文献