Patent
Role of novel carbazole linked 1, 2, 3- triazole analogs in alleviating methylglyoxal-mediated late diabetic vascular complications
| العنوان: | Role of novel carbazole linked 1, 2, 3- triazole analogs in alleviating methylglyoxal-mediated late diabetic vascular complications |
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| Patent Number: | 11925,622 |
| تاريخ النشر: | March 12, 2024 |
| Appl. No: | 17/408006 |
| Application Filed: | August 20, 2021 |
| مستخلص: | The present intervention identifies the antiglycating inhibitors from a series of carbazole-linked 1,2,3 triazole derivatives through in vitro MGO-mediated glycating BSA model. Derivatives 12, and 13 established a remarkable antiglycation activity at the receptor level in human monocytes. These compounds were found non-toxic, and possess the potential to halt AGE-RAGE/ROS-mediated NF-kB-dependent COX-2, and its proinflammatory product, PGE2, production in monocytes. Hence, carbazole-linked 1,2,3 triazole derivatives provide treatment modalities to delay or prevent the onset of late diabetic micro- and macro-vascular complications in diabetic patients. |
| Inventors: | Jahan, Humera (Karachi, PK); Choudhary, Mohammad Iqbal (Karachi, PK); Siddiqui, Nimra Naz (Karachi, PK); Basha, Fatima Z. (Karachi, PK); Iqbal, Shazia (Karachi, PK) |
| Claim: | 1. A method for reducing the development of diabetes-associated late vascular impairment diabetic atherogenesis progression comprising administration to diabetic patients in need for such treatment, an effective dose of a carbazole-linked 1,2,3-triazole compounds, in a pharmaceutical formulation. |
| Claim: | 2. The method of claim 1 , wherein the carbazole-linked 1,2,3-triazole compounds are 2-(4-((9H-Carbazole-9-yl)methyl)-1H-1,2,3-triazole-1-yl)-1-(4-nitrophenyl)ethan-1-one and 9-((1-(2-(2-Methyl-5-nitro-1H-imidazol-1-yl)ethyl)-1H1,2,3-triazol-4-yl)methyl)-9H-carbazole. |
| Claim: | 3. The method of claim 1 , wherein the diabetes-associated late vascular impairment and diabetic atherogenesis progression comprise AGEs formation, pro-inflammatory biomarkers, COX-2, or associated PGE2 formation. |
| Patent References Cited: | 20160244435 August 2016 Eckmann |
| Other References: | Miyamoto et al., “Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity”, 2013, Proceedings of the National Academy of Sciences of the United States of America, 110(43), pp. 17564-17569. (doi/10.1073/pnas. 1302664110) (Year: 2013). cited by examiner Iqbal et al., “New carbazole linked 1,2,3-triazoles as highly potent non-sugar (alpha)-glucosidase inhibitors”, 2017, Bioorganic Chemistry, vol. 74, pp. 72-81. (http://dx.doi.org/10.1016/j.bioorg.2017.07.006) (Year: 2017). cited by examiner Iqbal et al., “Synthesis of new bicarbazole-linked triazoles as noncytotoxic reactive oxygen species (ROS) inhibitors”, 2019, Synthetic Communications, 49(18), pp. 2330-2341. (https://doi.org/10.1080/00397911.2019.1620281) (Year: 2019). cited by examiner Jahan et al., “Suppression of COX-2/PGE2 levels by carbazole-linked triazoles via modulating methylglyoxal-AGEs and glucose-AGEs—induced ROS/NF-KB signaling in monocytes”, 2022, Cellular Signalling, 97(110372), pp. 1-13. (https://doi.org/10.1016/j.cellsig.2022.110372) (Year: 2022). cited by examiner Shaikh et al., “Carbazole-Linked 1,2,3-Triazoles: In Vitro β-Glucuronidase Inhibitory Potential, Kinetics, and Molecular Docking Studies”, 2019, ChemistrySelect, 4(20), pp. 6181-6189. (DOI: 10.1002/slct.201900647) (Year: 2019). cited by examiner |
| Primary Examiner: | Tran, My-Chau T. |
| رقم الانضمام: | edspgr.11925622 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |