Dattatraya G. Raut, S. Patil, P. Choudhari, Vikas D. Kadu, A. Lawand, M. Hublikar, R. Bhosale
{"title":"新型苯并噻唑类抗氧化抗炎药物POCl3介导的合成、药理评价及分子对接研究","authors":"Dattatraya G. Raut, S. Patil, P. Choudhari, Vikas D. Kadu, A. Lawand, M. Hublikar, R. Bhosale","doi":"10.2174/2212796813666191118100520","DOIUrl":null,"url":null,"abstract":"\n\nThe present research work is focused on the development of alternative\nantioxidant and anti-inflammatory agents. The review of the literature reveals that many\nbenzofused thiazole analogues have been used as lead molecules for the design and development\nof therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral.\nThe synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant,\nanti-inflammatory activities and molecular docking study. Thus, the present research work\naims to synthesize benzofused thiazole derivatives and to test their antioxidant and antiinflammatory\nactivities.\n\n\n\nTo design and synthesize an alternative antioxidant and anti-inflammatory agents.\n\n\n\nThe substituted benzofused thiazoles 3a-g were prepared by cyclocondensation reaction\nof appropriate carboxylic acid with 2-aminothiophenol in POCl3 and heated for about\n2-3 h to offer benzofused thiazole derivatives 3a-g. All the newly synthesized compounds\nwere in vitro screened for their anti-inflammatory and antioxidant activities by using a\nknown literature method.\n\n\n\nAt the outset, the study of in vitro indicated that the compounds code 3c, 3d and 3e\npossessed distinct anti-inflammatory activity as compared to a standard reference. All the\ntested compounds show potential antioxidant activity against one or more reactive (H2O2,\nDPPH, SO and NO) radical scavenging species. Additionally, docking simulation is further\nperformed to the position of compounds 3d & 3e into the anti-inflammatory active site to determine\nthe probable binding model.\n\n\n\nNew anti-inflammatory and antioxidant agents were needed; it has been proved\nthat benzofused thiazole derivatives were 3c, 3d and 3e constituted as an interesting template\nfor the evaluation of new anti-inflammatory agents and an antioxidant’s work also may provide\nan interesting template for further development.\n","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"50 1","pages":"58-68"},"PeriodicalIF":0.0000,"publicationDate":"2020-02-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"5","resultStr":"{\"title\":\"POCl3 Mediated Syntheses, Pharmacological Evaluation and Molecular Docking Studies of Some Novel Benzofused Thiazole Derivatives as a Potential Antioxidant and Anti-inflammatory Agents\",\"authors\":\"Dattatraya G. Raut, S. Patil, P. Choudhari, Vikas D. Kadu, A. Lawand, M. Hublikar, R. Bhosale\",\"doi\":\"10.2174/2212796813666191118100520\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\nThe present research work is focused on the development of alternative\\nantioxidant and anti-inflammatory agents. The review of the literature reveals that many\\nbenzofused thiazole analogues have been used as lead molecules for the design and development\\nof therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral.\\nThe synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant,\\nanti-inflammatory activities and molecular docking study. Thus, the present research work\\naims to synthesize benzofused thiazole derivatives and to test their antioxidant and antiinflammatory\\nactivities.\\n\\n\\n\\nTo design and synthesize an alternative antioxidant and anti-inflammatory agents.\\n\\n\\n\\nThe substituted benzofused thiazoles 3a-g were prepared by cyclocondensation reaction\\nof appropriate carboxylic acid with 2-aminothiophenol in POCl3 and heated for about\\n2-3 h to offer benzofused thiazole derivatives 3a-g. All the newly synthesized compounds\\nwere in vitro screened for their anti-inflammatory and antioxidant activities by using a\\nknown literature method.\\n\\n\\n\\nAt the outset, the study of in vitro indicated that the compounds code 3c, 3d and 3e\\npossessed distinct anti-inflammatory activity as compared to a standard reference. All the\\ntested compounds show potential antioxidant activity against one or more reactive (H2O2,\\nDPPH, SO and NO) radical scavenging species. Additionally, docking simulation is further\\nperformed to the position of compounds 3d & 3e into the anti-inflammatory active site to determine\\nthe probable binding model.\\n\\n\\n\\nNew anti-inflammatory and antioxidant agents were needed; it has been proved\\nthat benzofused thiazole derivatives were 3c, 3d and 3e constituted as an interesting template\\nfor the evaluation of new anti-inflammatory agents and an antioxidant’s work also may provide\\nan interesting template for further development.\\n\",\"PeriodicalId\":10784,\"journal\":{\"name\":\"Current Chemical Biology\",\"volume\":\"50 1\",\"pages\":\"58-68\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-02-29\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"5\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Chemical Biology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/2212796813666191118100520\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Chemical Biology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/2212796813666191118100520","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
POCl3 Mediated Syntheses, Pharmacological Evaluation and Molecular Docking Studies of Some Novel Benzofused Thiazole Derivatives as a Potential Antioxidant and Anti-inflammatory Agents
The present research work is focused on the development of alternative
antioxidant and anti-inflammatory agents. The review of the literature reveals that many
benzofused thiazole analogues have been used as lead molecules for the design and development
of therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral.
The synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant,
anti-inflammatory activities and molecular docking study. Thus, the present research work
aims to synthesize benzofused thiazole derivatives and to test their antioxidant and antiinflammatory
activities.
To design and synthesize an alternative antioxidant and anti-inflammatory agents.
The substituted benzofused thiazoles 3a-g were prepared by cyclocondensation reaction
of appropriate carboxylic acid with 2-aminothiophenol in POCl3 and heated for about
2-3 h to offer benzofused thiazole derivatives 3a-g. All the newly synthesized compounds
were in vitro screened for their anti-inflammatory and antioxidant activities by using a
known literature method.
At the outset, the study of in vitro indicated that the compounds code 3c, 3d and 3e
possessed distinct anti-inflammatory activity as compared to a standard reference. All the
tested compounds show potential antioxidant activity against one or more reactive (H2O2,
DPPH, SO and NO) radical scavenging species. Additionally, docking simulation is further
performed to the position of compounds 3d & 3e into the anti-inflammatory active site to determine
the probable binding model.
New anti-inflammatory and antioxidant agents were needed; it has been proved
that benzofused thiazole derivatives were 3c, 3d and 3e constituted as an interesting template
for the evaluation of new anti-inflammatory agents and an antioxidant’s work also may provide
an interesting template for further development.
期刊介绍:
Current Chemical Biology aims to publish full-length and mini reviews on exciting new developments at the chemistry-biology interface, covering topics relating to Chemical Synthesis, Science at Chemistry-Biology Interface and Chemical Mechanisms of Biological Systems. Current Chemical Biology covers the following areas: Chemical Synthesis (Syntheses of biologically important macromolecules including proteins, polypeptides, oligonucleotides, oligosaccharides etc.; Asymmetric synthesis; Combinatorial synthesis; Diversity-oriented synthesis; Template-directed synthesis; Biomimetic synthesis; Solid phase biomolecular synthesis; Synthesis of small biomolecules: amino acids, peptides, lipids, carbohydrates and nucleosides; and Natural product synthesis).