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Efficient synthesis of 2,3-diarylbenzo[ b ]thiophene molecules through palladium (0) Suzuki–Miyaura cross-coupling reaction and their antithrombolyitc, biofilm inhibition, hemolytic potential and molecular docking studies
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-06-02 , DOI: 10.1007/s00044-020-02568-7
Nosheen Sial , Nasir Rasool , Komal Rizwan , Ataf Ali Altaf , Shaukat Ali , Ayesha Malik , Muhammad Zubair , Arusa Akhtar , Samia Kausar , Syed Adnan Ali Shah

A series of 2,3-diaryldibenzo[b]thiophene derivatives have been synthesized via Suzuki coupling reactions in moderate to good yields (59–79%). The synthesized compounds were evaluated for their antithrombolytic, biofilm inhibition, and hemolytic potential. All compounds showed significant biological potential. Compound (4k) revealed excellent antithrombolytic (87.24%) and biofilm inhibition (99.64%) activity. While compound (4i) exhibited an outstanding hemolytic potential (84.53%). The docking studies uncovered that studied compounds interact with streptokinase and plasminogen via hydrogen bonding, π-anion, π–π stacked interactions, and π-sigma bonding type interactions. The results revealed that synthesized benzo[b]thiophene derivatives could be a potential source of therapeutic agents.

中文翻译:

通过钯(0)Suzuki-Miyaura交叉偶联反应有效合成2,3-二芳基苯并[b]噻吩分子及其抗血栓溶解性,生物膜抑制,溶血潜力和分子对接研究

通过Suzuki偶联反应已合成了一系列2,3-二芳基二苯并[b]噻吩衍生物,产率中等至良好(59-79%)。评价了合成的化合物的抗血栓形成,生物膜抑制和溶血潜力。所有化合物均显示出显着的生物学潜力。化合物(4k)具有出色的抗血栓溶解性(87.24%)和生物膜抑制作用(99.64%)。虽然复合(4i)具有出色的溶血潜力(84.53%)。对接研究发现,所研究的化合物通过氢键,π阴离子,π-π堆积相互作用和π-sigma键类型相互作用与链激酶和纤溶酶原相互作用。结果表明,合成的苯并[b]噻吩衍生物可能是治疗剂的潜在来源。
更新日期:2020-06-02
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