Synthesis, spectral characterization, docking studies and biological activity of urea, thiourea, sulfonamide and carbamate derivatives of imatinib intermediate

Chandrasekhar, Mandala; Prasad, G.; Venkataramaiah, Chintha; Raju, C. Naga; Seshaiah, K.; Rajendra, Wudayagiri

doi:10.1007/s11030-018-9906-4

Cited by 13 publications

(4 citation statements)

References 46 publications

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“…Sulfonamides have also been used as protective agents in chemotherapy against various diseases, as many drugs that contain sulfa drugs used as antibacterial, anti-fungal 9 , anti-inflammatory 10 , anticancer 11 , and an effective treatment for ulcerative colitis , alzheimer's 12 , HIV 13 , as well as in the treatment of infections of the urinary tract, intestines, eyes, and obesity 14 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Some New Pyrazole, Triazole, Oxadiazole, Thiazole, Thiadiazole Derivatives Bearing p-Toluenesulfonamide

Al-Hamad,

Al-Sabawi

2024

Baghdad Sci.J

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تم تشييد سلسلة من المشتقات الحلقية غير المتجانسة الجديدة A15-A5 باستخدام 4- (تولوين -4- سلفينيل امينو) - حمض البنزويك إيثيل استر A2 بوصفة مادة اولية. تم استخدام هذا المركب A2 بنجاح في تخليق بعض المشتقات الجديدة من أوكساديازول ، ديازول ، تريازول ، ثاياديازول ، ثيازول و مركبات حلقية غير متجانسة الملتحمة التي تحوي على بارا-تلوين سلفوناميد في تراكيبها والذي من المفترض أن يكون له أنشطة بيولوجية مهمة. تم استخدام التحليل الطيفي البروتون و الكاربون 13 النووي المغناطيسي والاشعة تحت الحمراء لدعم تشخيص المركبات المحضرة.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Some New Pyrazole, Triazole, Oxadiazole, Thiazole, Thiadiazole Derivatives Bearing p-Toluenesulfonamide

Al-Hamad,

Al-Sabawi

2024

Baghdad Sci.J

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“…Therefore, it is important to find new sources for the synthesis of safer and inexpensive antioxidants [17][18][19] . Some sulphonamide derivatives were screened for their antioxidant activity, which showed good results [20][21][22][23] . Sulphonamides chemically containing sulfamoyl (-SO 2 NH-) group are derivatives of amide.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterisation, biological evaluation andin silicostudies of sulphonamide Schiff bases

Durgun

Türkeş

Işık

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, 13 C NMR, 1 H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxidant activity was determined using different bioanalytical assays such as radical scavenging tests with ABTS þ , and DPPH þ as well as metal-reducing abilities with CUPRAC, and FRAP assays. All compounds showed satisfactory enzyme inhibitory potency in nanomolar concentrations against AChE and CA isoforms with K I values ranging from 10.14 ± 0.03 to 100.58 ± 1.90 nM. Amine group containing derivatives showed high metal reduction activity and about 70% ABTS radical scavenging activity. Due to their antioxidant activity and AChE inhibition, these novel compounds may be considered as leads for investigations in neurodegenerative diseases.

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“…Moreover, thioureas possess antibacterial activity against planktonic bacteria . TU have strong antifungal activities comparable to that observed for common antifungal antibiotic ketoconazole . Eweis et al.…”

Section: Introductionmentioning

confidence: 99%

“…[22] TU have strong antifungal activities comparable to that observed for common antifungal antibiotic ketoconazole. [23] Eweis et al reported chitosan-based benzoyl TU and their antifungal efficacy against sugar-beet pathogens. The tested TU derivatives showed antifungal activity higher than the native chitosan.…”

Section: Introductionmentioning

confidence: 99%

Novel N‐Acyl‐1H‐imidazole‐1‐carbothioamides: Design, Synthesis, Biological and Computational Studies

Aziz

Saeed

Khan

et al. 2020

Chemistry & Biodiversity

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The present study reports the convenient synthesis, spectroscopic characterization, bio‐assays and computational evaluation of a novel series of N‐acyl‐1H‐imidazole‐1‐carbothioamides. The screened derivatives displayed excellent antioxidant activity, moderate antibacterial and antifungal potential. The screened derivatives were found to be highly biocompatible against hRBCs. Molecular docking ascertained the mechanism and mode of action towards the molecular target delineating that ligands and complexes were stabilized at the active site by electrostatic and hydrophobic forces in accordance to the corresponding experimental results. Docking simulation provided additional information about the possibilities of inhibitory potential of the compounds against RNA. Computational evaluation predicted that N‐acyl‐1H‐imidazole‐1‐carbothioamides 5c and 5g can serve as potential surrogates for hit to lead generation and design of novel antioxidant and antibacterial agents.

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Synthesis, spectral characterization, docking studies and biological activity of urea, thiourea, sulfonamide and carbamate derivatives of imatinib intermediate

Cited by 13 publications

References 46 publications

Synthesis and Characterization of Some New Pyrazole, Triazole, Oxadiazole, Thiazole, Thiadiazole Derivatives Bearing p-Toluenesulfonamide

Synthesis and Characterization of Some New Pyrazole, Triazole, Oxadiazole, Thiazole, Thiadiazole Derivatives Bearing p-Toluenesulfonamide

Synthesis, characterisation, biological evaluation andin silicostudies of sulphonamide Schiff bases

Novel N‐Acyl‐1H‐imidazole‐1‐carbothioamides: Design, Synthesis, Biological and Computational Studies

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