ArticleMolecules (Basel, Switzerland)2026
Anti-Inflammatory Potential of 1-Aryl-6,7-Dimethoxy-1,2,3,4-Tetrahydroisoquinolines: Structure-Activity Relationship and COX-2 Binding.
Azizbek A Azamatov, Firuza M Tursunkhodzhaeva, Sherzod N Zhurakulov, Zufar D Boboev, Kuvonchbek F Kuchimov, Urkhiya K Aytmuratova, Ilhomjon S Ortikov, Robiya Sh Abdurazakova, Valentina I Vinogradova, Izzatullo Z Abdullaev and 1 more
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In one paragraphArticle in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 · Who and what moneyAuthors and funding
11 authors.
Azizbek A AzamatovInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.
Firuza M TursunkhodzhaevaInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.ORCID 0000-0002-8404-0952 Sherzod N ZhurakulovInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.ORCID 0000-0002-2857-946X Zufar D BoboevFaculty of Pharmacy and Chemistry, Alfraganus University, Yuqori Qoraqamish Str. 2a, Tashkent 100190, Uzbekistan.ORCID 0000-0001-8328-4034 Kuvonchbek F KuchimovInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.ORCID 0009-0001-0554-4029 Urkhiya K AytmuratovaInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.
Ilhomjon S OrtikovFaculty of Pharmacy and Chemistry, Alfraganus University, Yuqori Qoraqamish Str. 2a, Tashkent 100190, Uzbekistan.
Robiya Sh AbdurazakovaInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.
Valentina I VinogradovaInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 77, Tashkent 100170, Uzbekistan.
Izzatullo Z AbdullaevInstitute of Bioorganic Chemistry, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 87, Tashkent 100143, Uzbekistan.ORCID 0009-0009-9125-2476 Ulugbek G GayibovInstitute of Bioorganic Chemistry, Academy of Sciences of the Republic of Uzbekistan, M. Ulugbek Str 87, Tashkent 100143, Uzbekistan.
Funding
Academy of Sciences Republic of Uzbekistan Budget Program
6 · The paper itselfAbstract
Non-steroidal anti-inflammatory drugs (NSAIDs) are used globally for their pain-relieving and fever-reducing properties. However, excessive intake of NSAIDs can have harmful effects on multiple body systems, including the cardiovascular, gastrointestinal, hepatic, renal, and nervous systems. The anti-inflammatory activity of 34 derivatives of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline was investigated in vivo. A relationship between the activity of the compounds and the nature of their substituents, as well as their positional and mutual arrangement in the C ring (1-Ar-), was established. In silico modeling of these 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives' interaction with the COX-2 (PDB ID: 1PXX) active site revealed that the nitro-derivatives exhibited the highest stability owing to their superior capacity for electrostatic and hydrogen bond formation compared to brominated compounds. These data on the effects of the substituents -NH
Indexed as
Anti-Inflammatory AgentsAnti-Inflammatory Agents, Non-SteroidalCyclooxygenase 2Cyclooxygenase 2 InhibitorsTetrahydroisoquinolinesAnimalsMiceModels, MolecularMolecular Docking SimulationMolecular StructureProtein BindingStructure-Activity RelationshipAnti-Inflammatory AgentsAnti-Inflammatory Agents, Non-SteroidalCyclooxygenase 2Cyclooxygenase 2 InhibitorsTetrahydroisoquinolines1-aryl-1,2,3,4-tetrahydroisoquinolineanti-inflammatory activityCOX-2structure-activity
Identifiers
PMID42280258
PMCPMC13257858
What OpenQuestion holds
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