New metal complexes of sulfonamide: Synthesis, characterization, in-vitro anticancer, anticholinesterase, antioxidant, and antibacterial studies
APPLIED ORGANOMETALLIC CHEMISTRY
Authors: Danish, Muhammad; Raza, Muhammad Asam; Khalid, Hirra; Iftikhar, Umara; Arshad, Muhammad Nadeem
Abstract
In this research work a sulfonamide from tranexamic acid has been synthesized followed by its metal complexation.p-Bromo benzene sulfonyl chloride was used to synthesize sulfonamide using eco-friendly atmosphere. The sulfonamide prepared from tranexamic acid has been utilized for the preparation of metal complexes with various metals like Ni, Cu, Co, Mn, Pb, Cd, Cr, Fe, Sn, and Sr. All synthesized compounds were characterized by applying different spectral techniques such as Fourier-transform infrared (FTIR), mass spectrometry, and X-ray diffraction (XRD) analysis. The biological activities such as radical scavenging activity, enzyme inhibition, antifungal, antibacterial, and anticancer were performed. It was concluded from the results that compounds showed moderate to good activity. Cu complex of sulfonamide showed the highest antioxidant potential (87.69 +/- 1.8% with IC(50)137 +/- 1.0 mu g) while Cr complex depicted the highest activity against both enzymes; AChE (73.51 +/- 1.7% with IC(50)165 +/- 1.1 mu g) and BChE (70.05 +/- 1.3% with IC(50)152 +/- 1.8 mu g). Mn complex showed good results against six bacterial strains comparable with standard drug. Cr complex depicted highest anticancer activity against MCF7 and human corneal epithelial cell (HCEC) cell lines 45.73% and 25.40%, respectively. These results concluded that metal complexes of sulfonamide may be good induction in the future for medical purposes.
Pharmacological management of dementia with Lewy bodies with a focus on zonisamide for treating parkinsonism
EXPERT OPINION ON PHARMACOTHERAPY
Authors: Panza, Francesco; Lozupone, Madia; Watling, Mark; Imbimbo, Bruno P.
Abstract
Introduction Dementia with Lewy bodies (DLB) has no approved symptomatic or disease-modifying treatments in the US and Europe, despite being the second most common cause of neurodegenerative dementia. Areas covered Herein, the authors briefly review the DLB drug development pipeline, providing a summary of the current pharmacological intervention studies. They then focus on the anticonvulsant zonisamide, a benzisoxazole derivative with a sulfonamide group and look at its value for treating parkinsonism in DLB. Expert opinion Several new compounds are being tested in DLB, the most innovative being those aimed at decreasing brain accumulation of alpha-synuclein. Unfortunately, new drug testing is challenging in terms of consistent diagnostic criteria and lack of reliable biomarkers. Few randomized controlled trials (RCTs) are well-designed, with enough power to detect significant drug effects. Levodopa monotherapy can treat the parkinsonism in DLB, but it can cause agitation or visual hallucination worsening. Two Phase II/III RCTs of DLB patients recently reported a statistically significant improvement in motor function in those receiving zonisamide as an adjunctive treatment to levodopa. New biomarker strategies and validated outcome measures for DLB or prodromal DLB may enhance clinical trial design for the development of specific disease-modifying treatments.