Structural manifestations and biological screening for newly synthesized heteroleptic bismuth(V) bis-carboxylates

被引:4
作者
Andleeb, Sohaila [1 ]
Imtiaz-ud-Din [2 ]
Rauf, Muhammad Khawar [3 ]
Ul-Haq, Ihsan [4 ]
Schipper, Desmond [5 ]
机构
[1] Natl Univ Technol, Sch Appl Sci & Humanities, Islamabad 44000, Pakistan
[2] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
[3] Govt Post Grad Coll Shakargarh, Dept Chem, Shakargarh, Pakistan
[4] Quaid I Azam Univ, Dept Pharm, Islamabad, Pakistan
[5] Rice Univ, Chem Dept, Houston, TX USA
关键词
Bismuth; carboxylates; X-ray structure; human lymphocytes; antileishmanial; ANTILEISHMANIAL ACTIVITY; HELICOBACTER-PYLORI; DICARBOXYLATES; COMPLEXES; DERIVATIVES; CHEMISTRY; LIGANDS;
D O I
10.1080/00958972.2021.2011250
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Six new heteroleptic tri-organobismuth(V) complexes (1-6), of general formula, R3Bi(OOCR')(2) where R = C6H5 (1-3), p-CH3C6H4 (4-6) and R' represents deprotonated 2-(methylthio)nicotinic acid (1, 4); 3-thiophenecarboxylic acid (2, 5) and 4-chlorosalicylic acid (3, 6) have been synthesized and characterized by FT-IR, NMR (H-1, C-13) and single crystal XRD techniques in addition to elemental analyses. The solid-state structure for 3 has also been elucidated by crystallographic data, manifesting its distorted trigonal bipyramidal molecular geometry with a five-coordinate bismuth center. The carboxylate ligand(s) assume a monodentate coordination mode as predicted by IR and then confirmed by XRD data. The antibacterial, antifungal and antileishmanial potential for 1-6 have been evaluated and the preliminary screening data suggest significant to average biological activities. The antileishmanial activity data manifest comparatively lower IC50 value for 5 than the standard drug. A comprehensive study for 1-6 was also undertaken to testify their stability both in solid and solution phases as well as in leishmanial culture M199, which demonstrate high degree of stability that may ensure their significant antileishmanial effect. The % viability values of the organobismuth(V) bis-carboxylates highlight their role as significantly effective compounds, having potential candidature for future drug discovery and development processes.
引用
收藏
页码:3002 / 3017
页数:16
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