Small molecule innate immune modulators in cancer therapy.

Immunotherapy has proved to be a breakthrough in cancer treatment. So far, a bulk of the approved/late-stage cancer immunotherapy are antibody-based. Although these antibody-based drugs have demonstrated great promise, a majority of them are limited due to their access to extracellular targets, lack of oral bioavailability, tumor microenvironment penetration, induction of antibody dependent cytotoxicity etc.

Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.

New antibiotics with either a novel mode of action or novel mode of inhibition are urgently needed to overcome the threat of drug-resistant tuberculosis (TB). The present study profiles new spiropyrimidinetriones (SPTs), DNA gyrase inhibitors having activity against drug-resistant (), the causative agent of TB. While the clinical candidate zoliflodacin has progressed to phase 3 trials for the treatment of gonorrhea, compounds herein demonstrated higher inhibitory potency against DNA gyrase (e.

Use of complementary medicines and lifestyle approaches by people living with dementia: Exploring experiences, motivations and attitudes.

Background: Lack of effective treatments for chronic conditions is associated with high rates of complementary medicine (CM) use. However, little is known about CM use for dementia.

Aims And Objectives: The aim of this study was to explore the experiences, motivations, and attitudes towards CM use by people living with dementia in an Australian setting.

Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity.

Fusidic acid (FA) is a potent congener of the fusidane triterpenoid class of antibiotics. Structure-activity relationship (SAR) studies suggest the chemical structure of FA is optimal for its antibacterial activity. SAR studies from our group within the context of a drug repositioning approach in tuberculosis (TB) suggest that, as with its antibacterial activity, the C-21 carboxylic acid group is indispensable for its anti-mycobacterial activity.

Antimalarial Pyrido[1,2- a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies.

A novel series of pyrido[1,2- a]benzimidazoles bearing Mannich base side chains and their metabolites were synthesized and evaluated for in vitro antiplasmodium activity, microsomal metabolic stability, reactive metabolite (RM) formation, and in vivo antimalarial efficacy in a mouse model. Oral administration of one of the derivatives at 4 × 50 mg/kg reduced parasitemia by 95% in Plasmodium berghei-infected mice, with a mean survival period of 16 days post-treatment. The in vivo efficacy of these derivatives is likely a consequence of their active metabolites, two of which showed potent in vitro antiplasmodium activity against chloroquine-sensitive and multidrug-resistant Plasmodium falciparum ( P.

Decadal Experience of Renal Cell Carcinoma from a Tertiary Care Teaching Institute in North India.

To study the current trends of renal cell carcinoma (RCC) in terms of demographic characteristics, clinical presentation, staging, mode of management, histopathology, and survival characteristics from a high volume tertiary care teaching institute in North India. We retrospectively reviewed the records of all patients of RCC between January 2006 and December 2015 and variables like age, gender, symptoms, tumor size/location/number, stage, type of surgery, histopathology, and survival characteristics were studied. One hundred forty-four patients were included in the study.

Assessment of quality of life in patients of urethral stricture on clean intermittent catheterization following direct vision internal urethrotomy.

Context: Clean intermittent catheterization (CIC) after direct vision internal urethrotomy (DVIU).

Aims: The aim is to assess the quality of life (QOL) in patients with urethral strictures on CIC following DVIU.

Settings And Design: Prospective study.

Identification of essential surgical competencies to be imparted in urological residency: A survey-based study.

Introduction: There are variations in surgical procedures included in urology residency curricula across various programs. We conducted a survey of practicing urologists to determine which procedures are considered essential to a core urology residency curriculum.

Materials And Methods: A web-based survey was conducted between October 2016 and February 2017 using SurveyMonkey.

Prospective study to evaluate the clinical outcome of intralesional interferon-α2b in the management of Peyronie's disease.

Context: Interferon (IFN)-α2b in Peyronie's disease (PD).

Aims: This study aims to evaluate clinical efficacy of the IFN-α2b in both subjective and objective manner for the treatment of PD and compared with previously used intralesional verapamil in terms of cost-benefit analysis.

Settings And Design: Prospective study.

Page kidney: A rare but surgically treatable cause of hypertension.

The Page kidney is a rare phenomenon. External renal parenchymal compression is the culprit. We report two cases of young males with flank pain, renal mass, and hypertension with history of blunt abdominal trauma.

Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis.

Novel reversed isoniazid (RINH) agents were synthesized by covalently linking isoniazid with various efflux pump inhibitor (EPI) cores and their structural motifs. These RINH agents were then evaluated for anti-mycobacterial activity against sensitive, isoniazid mono-resistant and MDR clinical isolates of M. tuberculosis and a selected number of compounds were also tested ex vivo for intracellular activity as well as in the ethidium bromide (EB) assay for efflux pump inhibition efficacy.

Evaluation of Impact of Voiding Posture on Uroflowmetry Parameters in Men.

Purpose: To evaluate the impact of voiding position on uroflowmetry parameters and to assess its potential clinical implications.

Materials And Methods: We conducted a prospective study from 2013 to 2015 and included men between 18 and 77 years old who were either healthy volunteers with an International Prostate Symptom Score (IPSS) ≤7 or men with benign prostate enlargement that were on alpha-blocker medication and had an IPSS <10. Participants underwent uroflowmetry and post-void residual urine (PVRU) measurements twice, once in a sitting position and once in a standing position.

A Prospective Study to Evaluate Sexual Dysfunction and Enlargement of Seminal Vesicles in Sexually Active Men Treated for Benign Prostatic Hyperplasia by Alpha-blockers.

Objective: To evaluate sexual dysfunction and enlargement of seminal vesicles in sexually active men who were treated by α1-blockers for benign prostatic hyperplasia and its possible clinical application.

Materials And Methods: This is a prospective cohort study from January 2015 to December 2016. We enrolled sexually active men above the age of 40 years having moderate to severe lower urinary tract symptoms (LUTS).

Does prostate size predict the urodynamic characteristics and clinical outcomes in benign prostate hyperplasia?

Aims: Bladder outlet obstruction (BOO) in large and small prostates is managed in a similar manner despite considerably different pathophysiology, which can result in higher failure rates. We investigate the clinical and urodynamic features and study the outcome of patients with benign prostate hyperplasia (BPH) according to their prostate size.

Subjects And Methods: We prospectively analyzed 100 BPH patients undergoing urodynamic study between January 2015 and August 2016 and divided them into two groups according to their prostate size: small (≤30 mL) and large prostate (>30 mL) groups.

Nephrolithisis in a newborn: a rare case and review of literature.

Nephrolithiasis, although a common entity in adults, is less common in children and rare in newborns. The evaluation and management strategies of renal stones in neonates are unclear. We report a rare scenario of renal calculus in a newborn aged 3 days presenting with decreased urine output, fever and crying during micturition.

Emphysematous pyelonephritis: Changing trend of clinical spectrum, pathogenesis, management and outcome.

Objective: To highlight changing trend of clinical spectrum, comparing management options and predictors of outcome of emphysematous pyelonephritis.

Material And Methods: This study included patients who were diagnosed as emphysematous pyelonephritis between August, 2001 to July, 2015. We excluded other possible causes of gas in renal system.

What is the fate of insignificant residual fragment following percutaneous nephrolithotomy in pediatric patients with anomalous kidney? A comparison with normal kidney.

Pediatric population has increasing incidence of renal calculus and it is estimated to be around 50/10,000 population. The treatment of choice for large and complex stone in anomalous kidney is percutaneous nephrolithotomy (PCNL). The fate of insignificant residual fragment after PCNL in pediatric patients is not well documented.

Antischistosomal Activity of Pyrido[1,2-a]benzimidazole Derivatives and Correlation with Inhibition of β-Hematin Formation.

The extensive use of praziquantel against schistosomiasis raises concerns about drug resistance. New therapeutic alternatives targeting critical pathways within the parasite are therefore urgently needed. Hemozoin formation in Schistosoma presents one such target.

Rare association of congenital penile urethrocutaneous fistula with Y-type urethral duplication.

A 24-year-old man presented with symptoms of difficulty in passage of urine, mixed with gas and stool from penoscrotal junction since birth. He had a history of surgery (posterior sagittal anorectoplasty) for imperforate anus in first week of his life. On physical examination, external meatus was adequate with small 5×5 mm fistulous opening noted at penoscrotal junction with normal anal tone and opening.

Outcomes of transurethral resection and holmium laser enucleation in more than 60 g of prostate: A prospective randomized study.

Aim: Transurethral resection of prostate (TURP) is considered a gold standard surgical procedure. The management of benign prostatic hyperplasia (BPH) has undergone tremendous change in recent years and shifted from open to minimal invasive procedure. With the advancement in technology and skills of surgeons, lasers have been used more liberally, particularly holmium laser.

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Further structure-activity relationship (SAR) studies on the recently identified pyrido[1,2-a]benzimidazole (PBI) antimalarials have led to the identification of potent, metabolically stable compounds with improved in vivo oral efficacy in the P. berghei mouse model and additional activity against parasite liver and gametocyte stages, making them potential candidates for preclinical development. Inhibition of hemozoin formation possibly contributes to the mechanism of action.

Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents.

A series of novel fusidic acid (FA) derivatives was synthesized by replacing the carboxylic acid group with various ester and amide groups and evaluated in vitro for their antiplasmodial activity against the chloroquine-sensitive NF54 and multidrug-resistant K1 strains of the malarial parasite Plasmodium falciparum. Most of these derivatives showed a 4-49 and 5-17-fold increase in activity against NF54 and KI strains, respectively, as compared to FA and had a good selectivity index. These derivatives are stable over the incubation period and do not appear to be prodrugs of fusidic acid.

Is normal saline the best irrigation fluid to be used during percutaneous nephrolithotomy in renal failure patient? A prospective randomized controlled trial.

Objective: Endoscopic procedures like percutaneous nephrolithotomy (PCNL) needs continuous irrigation for better vision and to wash away stone fragments and blood clots. Systemic absorption of irrigation fluids may lead to fluid overload and electrolyte disequilibrium. Renal failure patients are more prone to these electrolyte disturbances.

Electromyography needle breaks within the perineum: a rare complication of urodynamics not reported earlier and lesson learnt.

The urodynamic study (UDS) is nowadays frequently used by the urologist worldwide to aid in the diagnosis of various urological disorders and electromyography (EMG) is an integral part of it. EMG is performed either by using surface electrodes or concentric needle electrodes. We report an unusual case in which the concentric EMG needle was accidentally broken within the perineum of a man aged 60 years undergoing urodynamics.