Synthesis and Anti-Inflammatory Activity of Fused 1,2,4-triazolo-[3,4-b][1,3,4]thiadiazole Derivatives of Phenothiazine

被引:0
作者
Maddila, S. [1 ]
Gorle, S. [2 ]
Singh, M. [2 ]
Lavanya, P. [3 ]
Jonnalagadda, S. B. [1 ]
机构
[1] Univ KwaZulu Natal, Sch Chem & Phys, ZA-4000 Durban, South Africa
[2] Univ KwaZulu Natal, Sch Life Sci, Discipline Biochem, ZA-4000 Durban, South Africa
[3] JNT Univ, Annamacharya Inst Technol & Sci, Dept Chem, Tirupati 517502, Andhra Pradesh, India
关键词
Anti-inflammatory activity; Phenothiazine; Synthesis; 1,2,4-Triazole-3-thiol; 1,2,4-Triazolo[3,4-b][1,3,4]thiadiazole; ANTIOXIDANT ACTIVITY; ANTIVIRAL ACTIVITY; 10H-PHENOTHIAZINES; 1,2,4-TRIAZOLE; CYTOTOXICITY; INHIBITION; ARTHRITIS; ANALOGS; BINDING; DRUGS;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new series of 10-((6-(substitutedphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl) methyl)-10H-phenothiazine derivatives (7a-k) moiety was prepared using intermediate compound 5-((10H-phenothiazin-10-yl)methyl)-4-amino-4H-1,2,4-triazole-3-thiol (5). The structures of newly synthesized compounds were confirmed on the basis of their H-1 NMR, C-13 NMR, LCMS mass, FT-IR and elemental analysis data results. All the compounds were screened for their significant anti-inflammatory activity of inhibition in paw oedema at 3h and 5h respectively, compared to the standard drug indomethacin. The Compounds 7k and 7d showed potent activity, while compounds 7g, 7b, 7j, 7i and 7c exhibited significant activity when compared to the standard drug, due to the presence of mild electron withdrawing groups such as difluoro, fluorine, chlorofluoro, nitro and chlorine derivatives which are attached to the benzene rings.
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收藏
页码:977 / 983
页数:7
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