Therapeutic potential of oxazole scaffold: a patent review (2006–2017)

ABSTRACT

Introduction: Oxazoles are oxygen and nitrogen containing five membered heterocyclic ring systems that are present in various anticancer, antimicrobial, antihyperglycemic, anti-inflammatory agents etc. of natural origin. These pharmacologically active oxazole derivatives have attracted numerous researchers to explore this scaffold for the design and development of newer potential therapeutic agents. A large number of synthetic oxazole containing molecules have been reported over the period that exhibited wide spectrum of pharmacological profiles. Some of them have shown promising therapeutic potential and have qualified for both preclinical and clinical evaluations.

Areas covered: In this review, the patents (published during 2006–2017) focusing on the biological potential of oxazoles have been covered. Therapeutic applications and various techniques/assays employed for the in vitro/in vivo evaluation of patented derivatives have been discussed majorly.

Expert opinion: Chemically oxazole offers three positions for substitution. These substituted oxazole derivatives of natural as well as synthetic origin have numerous pharmacological applications including anticancer, anti-Alzheimer’s, anti-hyperglycemic, anti-inflammatory, antibacterial etc. Their pharmacological actions are mainly mediated through enzyme/receptor involved in the particular disease. The flexible nature of this ligand for various molecular level targets (enzyme/receptor) make this heterocylce an attractive scaffold for development of effective and clinically relevant oxazole containing therapeutic agents.     

Can lubrication of the eyelid speculum reduce overall pain perception associated with cataract surgery by phacoemulsification performed under topical anesthesia?

Purpose:This study aimed to evaluate the effect of using the lubricated eyelid speculum on the overall pain perception by the subject patients who underwent cataract surgery by phacoemulsification technique under topical anesthesia.Methods:A prospective interventional randomized comparative study was conducted at the tertiary eye care center, wherein adult patients scheduled for bilateral cataract surgery with phacoemulsification techniques under topical anesthesia were randomized to undergo surgery with two different modes of eyelid speculum insertion, either with or without lubrication of the eyelid speculum. Fifty percent of the patients underwent surgery with eyelid speculum without lubrication, and 50% with lubrication of the eyelid speculum. The primary outcome was to compare the level of overall pain perception among the subject patients of the two groups by using the Visual Analogue Scale (VAS) in the immediate postoperative period.Results:The study included 130 patients who underwent bilateral cataract surgery (n = 260 eyes) under topical anesthesia, wherein n = 130 eyes underwent surgery using lubricated eyelid speculum and n = 130 eyes underwent surgery with dry eyelid speculum. Pain perception score assessed on the VAS (0–10 cm) ranged from 0.5 to 6, with a mean ± standard deviation of 2.06 ± 1.12. A significant correlation was found with two different methods of eyelid speculum insertion with reduced overall pain perception in patients with the use of lubricated eyelid speculum compared to the dry eyelid speculum (P = 0.0001).Conclusion:The overall pain perception associated with cataract surgery performed by phacoemulsification technique under topical anesthesia can be further minimized by lubricating the eyelid speculum prior to insertion for exposing the globe.     

Isolated cardiac metastasis in a patient with neuroendocrine carcinoma of pancreas discovered on 68Ga-DOTANOC PET/CT

We present an interesting image that demonstrates utility of ⁶⁸Ga-DOTANOC PET/CT for demonstrating rare metastatic sites of neuroendocrime tumor.     

The American Brachytherapy Society consensus statement for accelerated partial breast irradiation

PurposeTo develop clinical guidelines for the quality practice of accelerated partial breast irradiation (APBI) as part of breast-conserving therapy for women with early-stage breast cancer.Methods and MaterialsMembers of the American Brachytherapy Society with expertise in breast cancer and breast brachytherapy in particular devised updated guidelines for appropriate patient evaluation and selection based on an extensive literature search and clinical experience.ResultsIncreasing numbers of randomized and single and multi-institution series have been published documenting the efficacy of various APBI modalities. With more than 10-year followup, multiple series have documented excellent clinical outcomes with interstitial APBI. Patient selection for APBI should be based on a review of clinical and pathologic factors by the clinician with particular attention paid to age (≥50 years old), tumor size (≤3 cm), histology (all invasive subtypes and ductal carcinoma in situ), surgical margins (negative), lymphovascular space invasion (not present), and nodal status (negative). Consistent dosimetric guidelines should be used to improve target coverage and limit potential for toxicity following treatment.ConclusionsThese guidelines have been created to provide clinicians with appropriate patient selection criteria to allow clinicians to use APBI in a manner that will optimize clinical outcomes and patient satisfaction. These guidelines will continue to be evaluated and revised as future publications further stratify optimal patient selection.     

Does Tweeting Improve Citations? One-Year Results From the TSSMN Prospective Randomized Trial

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Intrahepatic biliary duct branching patterns,cystic duct anomalies,and pancreas divisum in a tertiary referral center: A magnetic resonance cholangiopancreaticographic study

Background

Knowledge about anatomic variations in intrahepatic biliary ducts (IHBD) is relevant for performing biliary drainage and for avoiding bile duct injury during cholecystectomy and liver resections. Low insertion of cystic duct (LICD) is a common anatomic variant. Pancreas divisum is the commonest congenital anomaly of pancreas; it has been causally linked with recurrent acute pancreatitis (RAP).

Methods

Magnetic resonance cholangiopancreaticography (MRCP) images of 500 consecutive patients were reviewed for anatomic variants of IHBD, cystic duct, and pancreatic duct.

Results

Anatomy of IHBD could be evaluated in 458 MRCP’s, of these 301 (65.72 %) had ‘typical’ anatomy. The variant in 157 persons included ‘triple confluence’ in 56 (12.23 %), ‘right posterior segmental duct (RPSD) draining to left hepatic duct (LHD)’ in 64 (14 %), ‘RPSD to common hepatic duct (CHD)’ in 20 (4.4 %), ‘RPSD to cystic duct’ in 2 (0.4 %), ‘accessory duct to CHD’ in 3 (0.7 %), ‘accessory duct to right hepatic duct (RHD)’ in 1 (0.2 %), ‘segment 2 and 3 separately to CHD’ in 1 (0.2 %), and complex variants in 10 (2.2 %). Cystic duct could be evaluated in 338 patients; of these, 15 (4.4 %) had LICD. Patients with RAP had pancreas divisum more often than those without any pancreatic disease, (?/?,10 % and ?/?, 0.8 %; p?=?0.004).

Conclusions

Nearly one third of MRCPs showed atypical IHBD pattern with RPSD draining to LHD being the commonest. LICD was the most common cystic duct variant. Pancreas divisum was more frequent in patients with RAP than in persons without pancreatic disease.