Newer Patents in Antimycobacterial Therapy

Abstract

Tuberculosis caused by Mycobacterium tuberculosis is a global health emergency. This deadly disease has far-reaching social and economic implications. Diseased individuals need prolonged polypharmacy which is not without ill effects. Treatment compliance is often compromised contributing to rising resistance. HIV co-infection has further worsened the scenario. On the other hand, no new anti-TB drug has hit the market in last 4-5 decades. After a long latency, only the last few years have witnessed growing research in this direction and a widening anti-TB drug clinical pipeline. The compounds in preclinical stage of development have also shown a heartening increase. The present review is an attempt to discuss novel promising patents in this field.

Combined Atomistic Molecular Calculations and Experimental Investigations for the Architecture, Screening, Optimization, and Characterization of Pyrazinamide Containing Oral Film Formulations for Tuberculosis Management

“…This computation was atomistic and related to the effect of fluctuations in surrounding humidity on the systemic E T of the matrix. The various hydrated matrices were built using the single frame packing task, density = 1 g/cm 3 , temperature = 25 °C, loading steps = 1000, time step = 0.1 fs, and external pressure = 0.1 MPa. Subsequently, the constructed hydrated oral film was geometrically optimized and subjected to systematic dynamics and mechanics calculations employing the Forcite tool.…”

“…Tuberculosis (TB) is a highly contagious, airborne disease mainly caused by the bacillus Mycobacterium tuberculosis which most commonly infects the lungs (pulmonary TB) and rarely any other part of the body (extrapulmonary TB). − It is considered a serious, life threatening infection worldwide, and it remains one of the world’s most lethal communicable diseases. , An estimate of 9 million new TB cases occur annually, and about 1.5–2 million of these cases have been fatal. , Nonetheless, the disease can be successfully treated and also prevented in highly susceptible individuals by employing existing anti-TB drugs, however, poor patient compliance with recommended treatment regimens is a major challenge impeding successful pharmacotherapeutic outcomes. − This constitutes a major contributing factor to the rising incidence of various types of resistance such as multidrug resistance (MDR), single drug resistance (SDR), and extensive drug resistance (XDR) which are the major causes of multiple deaths globally. , Additionally, TB coinfection in HIV (human immunodeficiency virus) patients has significantly amplified the severity of the disease, complicated its management processes and decreased the life expectancy of such individuals. , …”

“…1−4 This constitutes a major contributing factor to the rising incidence of various types of resistance such as multidrug resistance (MDR), single drug resistance (SDR), and extensive drug resistance (XDR) which are the major causes of multiple deaths globally. 3,4 Additionally, TB coinfection in HIV (human immunodeficiency virus) patients has significantly amplified the severity of the disease, complicated its management processes and decreased the life expectancy of such individuals. 3,5 Drug treatment still remains the most effective way of curing TB-infected individuals, averting fatality and relapse, preventing its spread to healthy populations, and stopping the development and transmission of drug resistant strains.…”

“…3,4 Additionally, TB coinfection in HIV (human immunodeficiency virus) patients has significantly amplified the severity of the disease, complicated its management processes and decreased the life expectancy of such individuals. 3,5 Drug treatment still remains the most effective way of curing TB-infected individuals, averting fatality and relapse, preventing its spread to healthy populations, and stopping the development and transmission of drug resistant strains. 1,2,6 Pyrazinamide (PYZ), also known as pyrazinecarboxamide, is a synthetic analogue of nicotinamide.…”

“…All component molecules were loaded into a single frame cubic lattice under periodic boundary conditions. Computer-aided construction of the films was atom-based and performed under ambient conditions (temperature = 25 °C, intrinsic system pressure = 0.1 MPa) and a density of 1 g/ cm 3 . Simulations were performed systematically until the point of convergence characterized by the lowest energy level.…”