Sharma Shalabh, Singh Tripti, Mittal Rajan, Saxena K K, Srivastava Virendra Kishore, Kumar Ashok
Medicinal Chemistry Division, Department of Pharmacology, Lala Lajpat Rai Memorial Medical College, Meerut, India.
Arch Pharm (Weinheim). 2006 Mar;339(3):145-52. doi: 10.1002/ardp.200500215.
In the present study, some naphthalene derivatives have been synthesized by incorporating azetidinyl and thiazolidinyl moieties at its alpha- or beta-positions such as alpha-(3-chloro-2-oxo-4-substituted)aryl-1-azetidinyl)naphthalenes 6-10, alpha-((substituted)aryl-4-oxo-1,3-thiazolidin-3-yl)naphthalenes 11-15, beta-(3-chloro-2-oxo-4-substituted aryl-1-azetidinyl)naphthalenes 21-25, and beta-(substituted aryl-4-oxo-1,3-thiazolidin-3-yl)naphthalenes 26-30. These compounds have also been screened for acute toxicity and anti-inflammatory and analgesic activities. Compounds which showed better anti-inflammatory and analgesic activities were also examined for their ulcerogenic liability and underwent a cyclooxygenase assay. Two compounds, 12 and 28, were found to exhibit potent anti-inflammatory activity as compared to the standard drugs phenylbutazone and naproxen.
在本研究中，通过在萘的α-或β-位引入氮杂环丁烷基和噻唑烷二酮基部分合成了一些萘衍生物，如α-(3-氯-2-氧代-4-取代)芳基-1-氮杂环丁烷基)萘6-10、α-((取代)芳基-4-氧代-1,3-噻唑烷-3-基)萘11-15、β-(3-氯-2-氧代-4-取代芳基-1-氮杂环丁烷基)萘21-25和β-(取代芳基-4-氧代-1,3-噻唑烷-3-基)萘26-30。还对这些化合物进行了急性毒性、抗炎和镇痛活性的筛选。对表现出较好抗炎和镇痛活性的化合物也进行了致溃疡倾向检查，并进行了环氧化酶测定。与标准药物保泰松和萘普生相比，发现两种化合物12和28具有强效抗炎活性。
