Medicinal chemistry of oxazines as promising agents in drug discovery

Oxazines have brought much synthetic interest due to their extensive biological activities. These are the important category of heterocycles, which may be formally derived from benzene and its reduction products by convenient substitution of carbon (and hydrogen) atoms by nitrogen and oxygen. In the last few decades, oxazine derivatives have documented as worthy synthetic intermediates and also blessed with notable sedative, analgesic, anticonvulsant, antipyretic, antimicrobial, antitubercular, antimalarial, antioxidant, and anticancer activities. Nowadays, it is important to develop new classes of compounds with more effective mechanisms due to drug resistance activity in which the ability of drug to effectively treat disease can be reduced. The aim of the article is to collect and make a more generalized review on the synthesis of oxazine derivatives and their pharmaceutical and biological activities. We hope this review will provide ample references for the researchers concerned with azines in generally and oxazines in particular.     

Evolution of β-catenin-independent Wnt–GSK3–mTOR signalling in regulation of energy metabolism in isoproterenol-induced cardiotoxicity model

Inflammation Research - Isoproterenol (ISO) is widely used agent to study the effects of interventions which could prevent or attenuate the development of myocardial infarction. The sequence of...     

Haemorrhage control beyond Advanced Trauma Life Support (ATLS) protocol in life threatening maxillofacial trauma – experience from a level Ⅰ trauma centre

Maxillofacial injuries are usually not life-threatening and do not get priority over other associated injuries. However, some maxillofacial injuries with active oral or nasal bleeding need immediate management due to threatened airway and blood loss. In the case of major active vascular bleeding, measures such as local pressure, anterior nasal packing, posterior nasal packing, and balloon tamponade are ineffective. In these cases, angiography and transcatheter arterial embolisation (TAE) are used to treat life-threatening haemorrhage caused by maxillofacial trauma. We analysed the medical records of 39 patients with severe maxillofacial trauma and life-threatening haemorrhage that was a result of intractable oral or nasal bleeding. These patients were considered for TAE from January 2010 to December 2019. A total of 1668 patients was admitted, out of which 39 (2.3%) had severe maxillofacial injuries with life-threatening oral or nasal bleeding and underwent TAE. Out of a total of 39 patients, 38 were male and one female. Ages ranged from 16 to 65 years. Road traffic injury was the most common cause of injury (79.5%), Lefort I and II were the most common facial fractures, and traumatic brain injury was the most common associated injury. Embolisation and bleeding control were done successfully in all 39 patients with no procedure-related complications. A total of 17 deaths during the study period were due to severe traumatic brain injuries or haemorrhagic shock.     

Thoracic cord herniation and associated intra-operative nuances: a report

Background

Thoracic cord herniation is a well-established entity in the literature. Majority of the published literature deals with its surgical management in terms of “mere” detethering of cord. However, not much is written about the degree of herniation and ectopic cord tissue and its management.

Case summary

A 58-year-old male presented to us with progressive difficulty in walking. Imaging revealed a cord herniation at T7–8 level. Surgical detethering was planned. However, a significant amount of “ectopic” cord tissue was found outside the dural defect intra-operatively. Simple detethering and repositioning was difficult. Hence, the ectopic tissue was excised under neuro-physiologic monitoring and no major change was recorded intra-operatively/post-operatively.

Conclusions

Thoracic cord herniation surgery may be more than simple detethering and cord repositioning. If encountered in similar situations intra-operatively, surgeons should be able to excise ectopic tissue without grave post-operative deficits. Neuronal plasticity probably plays an important role in the pathophysiology of long-standing cord herniation.

     

Pedicle streaking: A novel and simple aid in pedicle positioning in free tissue transfer

Introduction:The pedicle positioning in free tissue transfer is critical to its success. Long thin pedicles are especially prone to this complication where even a slight twist in the perforator can result in flap loss. Pedicles passing through the long tunnels are similarly at risk. Streaking the pedicle with methylene blue is a simple and safe method which increases the safety of free tissue transfer.Conclusion:This simple and novel method is very reliable for pedicle positioning avoiding any twist necessary for successful free tissue transfer.KEY WORDS: Free flaps, pedicle, perforator     

Simple device to determine the pressure applied by pressure clips for the treatment of earlobe keloids

Background:Keloids of the ear are common problems. Various treatment modalities are available for the treatment of ear keloids. Surgical excision with intralesional steroid injection along with compression therapy has the least recurrence rate. Various types of devices are available for pressure therapy. Pressure applied by these devices is uncontrolled and is associated with the risk of pressure necrosis. We describe here a simple and easy to use device to measure pressure applied by these clips for better outcome.Objectives:To devise a simple method to measure the pressure applied by various pressure clips used in ear keloid pressure therapy.Results:The pressure applied by different clips was variable. The spring clips were adjustable by slight variation in the design whereas the pressure applied by binder clips and magnet discs was not adjustable.Conclusion:The uncontrolled/suboptimal pressure applied by certain pressure clips can be monitored to provide optimal pressure therapy in ear keloid for better outcome.KEY WORDS: Clips, device, earlobe, magnetic discs, measure, pressure therapy, splint