Neuroimmunomodulatory properties of laquinimod

Laquinimod (ABR-215062) is a quinolone-3-carboxamide derivative, which is an orally active immunostimulatory drug molecule and is being developed for multiple sclerosis cases like relapsing-remitting multiple sclerosis (RRMS) and chronic progressive multiple sclerosis (CPMS). Laquinimod may mediate its effects by regulating pro-inflammatory immune responses and interfering with cell trafficking, in addition to possibly acting directly in the central nervous system to prevent demyelination and axonal injury. Nowadays, its benefits are extended further to various other neurodegenerative illnesses. Recently, it was found that laquinimod can exert only minimal effects in the clinical trials for both PPMS and RRMS making it not suitable for the treatment. However, cannot be completely neglected its pharmacological effect for curing disease progression in MS. Modification of the core structure can contribute to a better candidate for the treatment of MS. We have systematically reviewed the literature reported and highlighted the effect of laquinimod therapy not only on multiple sclerosis (MS) patients but also on a variety of other neurodegenerative disorders. Hence, this review can aid the research community in the design and development of novel chemical entities for the effective treatment of neurodegenerative disorders (NDDs)

Design, synthesis and biological evaluation of novel N1,N8-bis(((4-((5-aryl-1,3,4-oxadiazol-2-yl)methoxy)phenyl)amino)oxy)-1-naphthamide derivatives

<p>A new series of 1,8-bis(4-((5-phenyl-1,3,4-oxadiazol-2-yl) methoxy)-substituted aryl) naphthalene-1,8-dicarboxamide derivatives (<b>6a–j)</b> were synthesized in the presence of POCl₃ and obtained good yields. All the synthesized novel compounds were characterized by IR, ¹H NMR, ¹³C NMR, HRMS spectroscopic data and elemental analysis. All the synthesized compounds evaluated for their antibacterial and antifungal activities. The antibacterial activity screened against Gram-positive bacteria <i>Staphylococcus aureus</i> and Gram-negative bacteria <i>Escherichia coli</i> and used standard reference drug ciprofloxacin. The antifungal activity screened against two pathogenic fungal strains <i>Aspergillus niger</i> and <i>Candida albicans</i> used a reference standard drug Voriconazole. All these compounds (<b>6a–j)</b> demonstrate good antibacterial and antifungal activity. Among them, compounds <b>6h</b> and <b>6c</b> show highest antibacterial and antifungal activity.</p