The quinazoline-2,4(1H,3H)-diones skeleton: A key intermediate in drug synthesis

Quinazoline-2,4(1H,3H)-dione is a major class of N-fused heterocyclic with a wide range of biological functions, including anti-HIV, anticancer, antifungal, antibacterial, antimutagenic, anticoccidial, anticonvulsant, anti-inflammatory, antidepressant, antimalarial, antioxidant, antileukemic, and antileishmanial activities, and other activities, has attracted high attention in organic and medicinal chemistry. As a consequence, all chemists and pharmaceutical chemists should be familiar with the various procedures for producing quinazoline-2,4(1H,3H)-dione. The main purpose of this paper is to provide an overview of the many manufacturing methods for various biological compounds based on the quinazoline-2,4(1H,3H)-dione and 2,4-dichloroquinazoline cores.     

Expression analysis of mTOR-associated lncRNAs in multiple sclerosis

Metabolic Brain Disease - mTOR has been shown to be involved in the regulation of immune responses and differentiation of immune cells. This protein is a candidate molecule for unraveling the...     

Association of Lysyl oxidase (LOX) Polymorphisms with the Risk of Keratoconus in an Iranian Population

Background: Keratoconus is a connective tissue-related eye disease with unknown etiology that causes the loss of visual acuity. Lysyl oxidase (LOX) is an amine oxidase that catalyzes the covalent cross-link of collagens and elastin in the extracellular environment, thus determining the mechanical properties of connective tissue. The current study aimed to investigate the possible associations between two LOX polymorphisms, rs1800449 and rs2288393, and susceptibility to keratoconus.

Methods: A total of 262 Iranian subjects including 112 patients with keratoconus and 150 healthy individuals as controls were recruited. Genotyping for the LOX variants was performed using allele-specific PCR.

Results: A significant difference was found between two groups regarding allelic and genotyping distribution of LOX polymorphism at position rs1800449 G>A. The frequency of AA and GA?+?AA genotypes were increased in patients compared to controls (17% versus 8% and 62.5% versus 50%, respectively), showing a statistically significant difference (OR?=?2.827, 95% CI: 1.251–6.391, p?=?0.012). The A allele was associated with an increased risk for keratoconus, with the frequency of 39.9% and 29% in patients and controls, respectively (OR?=?1.614, 95% CI: 1.119–2.326, p?=?0.011). Furthermore, the haplotype analysis revealed that the rs1800449G/rs2288393C is a protective factor against keratoconus (OR?=?0.425, 95% CI?=?0.296–0.609, p?=?0.001). Conversely, the +473A/rs2288393C (OR?=?3.703, 95% CI?=?2.230–6.149, p?=?0.001) and +473G/rs2288393G (OR?=?15.48, 95% CI?=?3.805–63.03, p?=?0.001) haplotypes were identified as risk factors for keratoconus.

Conclusion: Our study demonstrated that the LOX rs1800449 genotypes (AA and GA?+?AA) and allele (A) appears to confer risk for susceptibility to keratoconus.     

Displacement of the Hip Center of Rotation After Arthroplasty of Crowe III and IV Dysplasia: A Radiological and Biomechanical Study

To study the direction and biomechanical consequences of hip center of rotation (HCOR) migration in Crowe type III and VI hips after total hip arthroplasty, post-operative radiographs and CT scans of several unilaterally affected hips were evaluated. Using a three-dimensional model of the human hip, the HCOR was moved in all directions, and joint reaction force (JRF) and abductor muscle force (AMF) were calculated for single-leg stance configuration. Comparing to the normal side, HCOR had displaced medially and inferiorly by an average of 23.4% and 20.8%, respectively, of the normal femoral head diameter. Significant decreases in JRF (13%) and AMF (46.13%) were observed in a presumptive case with that amount of displacement. Isolated inferior displacement had a small, increasing effect on these forces. In Crowe type III and IV hips, the HCOR migrates inferiorly and medially after THA, resulting in a decrease in JRF, AMF, and abductor muscle contraction force.     

The influence of ethnicity on the characteristics of multiple sclerosis: A local population study between Persians and Arabs

Background

Based on previous studies, Iran is located in a low risk area in terms of multiple sclerosis (MS). The objective of this study was to determine and compare the incidence, prevalence and demographic characteristics of MS in two ethnic groups of Persian and Arab over the period spanning 2009 in the Khuzestan province, in the Southwest of Iran.

Methods

A cross-sectional case register study was conducted between January and August 2009. All cases in the region whom were referred to the MS society in the city of Ahwaz were participants in the study. The population data from the Iranian Bureau of Statistics were used to calculate the population at risk based on the 1996 and 2006 census data.

Results

A total of 696 patients were identified according to the McDonald criteria during the last 12 years of which 569 patients were Persian. In 2009 the total prevalence and incidence rates of MS were 16.28 and 2.20 per 100,000 individuals. Based on these values, the female to male ratios were 3.11. The Persians manifested more sensory signs and symptoms (40.2%) but motor deficits (19.1%) and cerebellar findings (18.2%) were seen as being more manifest in Arab individuals. The main difference was observed in the progressive types of MS in which 24.7% of the Arab patients showed progressive type symptoms as compared to 15.9% of the cases in the Persian population.

Conclusion

According to this study the authors conclude that the prevalence and incidence of MS were higher in Persians; however progressive forms of MS with motor and cerebellar signs are more frequent in the Arab ethnic group.     

Electrodegradation of 2,4-dichlorophenoxyacetic acid herbicide from aqueous solution using three-dimensional electrode reactor with G/β-PbO2 anode: Taguchi optimization and degradation mechanism determination

This study aimed to investigate the electro-degradation of 2,4-dichlorophenoxyacetic acid (2,4-D) from aqueous solution using two and three-dimensional electrode (2D and 3D) reactors with graphite(G)/β-PbO₂ anode. To increase the degradation efficiency, affecting parameters on the electro-degradation process were investigated and optimized by adopting the Taguchi design of experiments approach. The structure, morphology and electrochemical properties of the electrodes were studied by X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX), linear sweep voltammetry and cyclic voltammograms. The controllable factors, i.e., electrolysis time, 2,4-D initial concentration, solution pH and current density (j) were optimized. Under optimum conditions, the 2,4-D degradation efficiency was 75.6% using 2D and 93.5% using 3D electrode processes. The percentage contribution of each controllable factor was also determined. The pH of the solution was identified as the most influential factor, and its percentage contribution value was up to 39.9% and 40.4% for 2D and 3D electrode processes, respectively. Considering the parameters of the kinetics, it was found that the degradation of 2,4-D and removal of COD using the G/β-PbO₂ electrode obey the pseudo-first order kinetics. In addition, the mineralization pathway of 2,4-D at G/β-PbO₂ electrode was proposed. The results also demonstrated that the 3D electrode process with G/β-PbO₂ anode can be considered as a useful method for degradation and mineralization of 2,4-D herbicides from aqueous solution.

Optimization of process parameters using the Taguchi method, electrochemical degradation and electrochemical degradation mechanism of 2,4-D herbicide using 2D and 3D reactors with G/β-PbO₂ anode were investigated.