Convergent Synthesis, Kinetics, and Computational Studies of Indole(Phenyl)Triazole Bi-Heterocycles Modified With Propanamides as Elastase Inhibitors.

Biological screening combined with the synthesis of heterocyclic compounds with numerous functions is the most effective approach available for pharmacological assessment of potential future medications. In the under taken research that is presented here, 4-(1H-indol-3-yl)butanoic acid was sequentially converted into 4-(1H-indol-3-yl)butanoate, 4-(1H-indol-3-yl)butanohydrazide, and 5-[3-(1H-indol-3-yl)propyl]-1,2,4-triazole-2-thiol as a nucleophile. By treating aryl amines with 3-bromopropanoyl chloride in a series of parallel reactions, different electrophiles were created, leading to the formation of N-(aryl)-3-bromopropanamides.

The Oncological Safety of Submental Flap Reconstruction in Head-and-Neck Cancers: An Extended Follow-up Study.

Introduction: The oncological safety of a submental (SM) flap is thought to be controversial. The objective of our study was to validate our previous study regarding the oncological safety of SM flaps in oral cavity reconstruction.

Materials And Methods: An electronic database was searched from 2015 to 2021 for all head-and-neck tumor patients, where reconstruction was performed using a SM flap.

Effectiveness of spaced repetition for clinical problem solving amongst undergraduate medical students studying paediatrics in Pakistan.

Background: Studies using spaced repetition for teaching and learning in undergraduate clinical rotations such as paediatrics are limited, even more so in the South Asian region. Therefore, this study aimed to identify the effectiveness of utilizing spaced repetition compared to traditional learning methods among undergraduate medical students during their paediatric rotation at a medical university in Pakistan.

Methods: Bahria University Medical and Dental College (BUMDC) conducted quasii-experimental research in Karachi.

Exploring chalcone-sulfonyl piperazine hybrids as anti-diabetes candidates: design, synthesis, biological evaluation, and molecular docking study.

To address the escalating rates of diabetes mellitus worldwide, there is a growing need for novel compounds. The demand for more affordable and efficient methods of managing diabetes is increasing due to the inevitable side effects associated with existing antidiabetic medications. In this present research, various chalcone-sulfonyl piperazine hybrid compounds (5a-k) were designed and synthesized to develop inhibitors against alpha-glucosidase and alpha-amylase.

Design of potent tyrosinase inhibiting -arylated-4-yl-benzamides bearing 2-aminothiazole-triazole bi-heterocycles: mechanistic insight through enzyme inhibition, kinetics and computational studies.

By using a convergent methodology, a unique series of -arylated 4-yl-benzamides containing a bi-heterocyclic thiazole-triazole core was synthesized and the structures of these hybrid molecules, 9a-k, were corroborated through spectral analyses. The studies of these multi-functional molecules demonstrated their potent mushroom tyrosinase inhibition relative to the standard used. The kinetics mechanism was exposed by lineweaver-burk plots which revealed that, 9c, inhibited mushroom tyrosinase non-competitively by forming an enzyme-inhibitor complex.

Effectiveness of blended pedagogy for radiographic interpretation skills in operative dentistry - a comparison of test scores and student experiences at an undergraduate dental school in Pakistan.

Background: Utilizing Blended pedagogy (BP) in radiographic skills may prove to be an effective teaching strategy. However, studies on the use of BP in dentistry are quite limited in Pakistan, where teaching has mostly been via traditional Didactic Lectures (DL); and radiographic interpretation skills of undergraduate dental students are suboptimal. Therefore, this study aims to assess whether utilizing BP to teach radiographic interpretation skills is an effective teaching methodology in Pakistan.

Short Implants: Their Role in Implant Reconstruction.

Short dental implant placement has become a more popular surgical option for the reconstruction of the dentoalveolar region. In this article, we briefly discuss the considerations that the clinician must take into account when considering the use of short dental implants.

Survival Outcomes and Patterns of Failure in Maxillary Alveolus Squamous Cell Carcinoma.

 Squamous cell carcinoma (SCC) of the maxillary alveolus is a relatively rare disease. There is lack of data on this subsite as compared with other sites. The factors that affect survival in cases of maxillary alveolar SCC are tumor stage, local and cervical metastases, histological grading, and the margin status.

Application Of New WHO Classification On Malignancies Of Sinonasal Tract: Correlation With Epidemiology And Survival In Pakistani Population.

Objectives: To analyse the clinicopathological characteristics of sinonasal malignancies in the light of the updates regarding head and neck tumours.

Methods: The retrospective study was conducted at the Shaukat Khanum Memorial Cancer Hospital and Research Centre, Lahore, Pakistan, and comprised data of patients diagnosed with primary malignant tumours of the sinonasal tract between 2015 and 2020. Slides related to biopsies and resection specimens were retrieved from the institutional database and reviewed by two pathologists.

Recent Development on Sensing Strategies for Small Molecules Detections.

Sensors play a critical role in the detection and monitoring of various substances present in our environment, providing us with valuable information about the world around us. Within the field of sensor development, one area that holds particular importance is the detection of small molecules. Small molecules encompass a wide range of organic or inorganic compounds with low molecular weight, typically below 900 Daltons including gases, volatile organic compounds, solvents, pesticides, drugs, biomarkers, toxins, and pollutants.

Synthesis and Computational Exploration of Morpholine Bearing Halogenated Sulfonamides as Potential Tyrosinase Inhibitors.

In the presented work, a new series of three different 4-((3,5-dichloro-2-[(2/4-halobenzyl)oxy]phenyl)sulfonyl)morpholines was synthesized and the structure of these compounds were corroborated by H-NMR & C-NMR studies. The in vitro results established all the three compounds as potent tyrosinase inhibitors relative to the standard. The Kinetics mechanism plots established that compound 8 inhibited the enzyme non-competitively.

γ-Glutamyltranspeptidase (GGT) Sensitive Fluorescence Probes for Cancer Diagnosis; Brief Review.

Millions of deaths occur each year due to the late diagnosis of abnormal cellular growth within the body. However, the devastating impact of this can be significantly reduced if cancer metastasis is detected early through the use of enzymatic biomarkers. Among several biomarkers, γ-glutamyltranspeptidase (GGT) stands out as a member of the aminopeptidase family.

Synthesis and Molecular Docking Studies of Novel Biheterocyclic Propanamides as Antidiabetic Agents Having Mild Cytotoxicity.

The aim of this work was to bring forth some new hybrid molecules having pharmacologically potent indole and 1,3,4-oxadiazole heterocyclic moieties unified with a propanamide entity. The synthetic methodology was initiated by esterification of 2-(1-indol-3-yl)acetic acid () in a catalytic amount of sulfuric acid and ethanol in excess, to form ethyl 2-(1-indol-3-yl)acetate (), which was converted to 2-(1-indol-3-yl)acetohydrazide () and further transformed to 5-(1-indole-3-yl-methyl)-1,3,4-oxadiazole-2-thiol (). 3-Bromopropanoyl chloride () was reacted with various amines (-) in aqueous alkaline medium to generate a series of electrophiles, 3-bromo--(substituted)propanamides (-), and these were further reacted with nucleophile in DMF and NaH base to yield the targeted -(substituted)-3-{(5-(1-indol-3-ylmethyl)-1,3,4-oxadiazol-2-yl)sulfanyl}propanamides (-).

Secretory carcinoma of minor salivary glands of buccal mucosa: A case report and review of the literature.

Introduction And Importance: Secretory carcinoma (SC) is an uncommon salivary gland neoplasm of the oral cavity that microscopically may mimic acinic cell carcinoma (ACC) and mucoepidermoid carcinoma (MEC). Secretory carcinoma (SC) of the salivary gland has been recently added in fourth edition of the head and neck world health organization. Most of these tumors are located on the parotid gland with very few cases reported in the minor salivary glands of the buccal mucosa.

Convergent synthesis, kinetics insight and allosteric computational ascriptions of thiazole-(5-aryl)oxadiazole hybrids embraced with propanamides as alkaline phosphatase inhibitors.

Considering the varied pharmacological prominence of thiazole and oxadiazole heterocyclic moieties, a unique series of bi-heterocyclic hybrids, 8a-h, was synthesized in a convergent manner. The structures of newly synthesized compounds were characterized by H-NMR, C-NMR, and IR spectral studies. The structure-activity relationship of these compounds was predicted by examining their inhibitory effects against alkaline phosphatase, whereby all these molecules exhibited superb inhibitory potentials relative to the standard used.

Design and synthesis of thiadiazole-oxadiazole-acetamide derivatives: Elastase inhibition, cytotoxicity, kinetic mechanism, and computational studies.

Considering the biological significance of 1,3,4-thiadiazole/oxadiazole heterocyclic scaffolds, a novel series of 1,3,4-thiadiazole-1,3,4-oxadiazole-acetamide derivatives (7a-j) was designed and synthesized using molecular hybridization. The inhibitory effects of the target compounds on elastase were evaluated, and all of these molecules were found to be potent inhibitors compared to the standard reference oleanolic acid. Compound 7f exhibited the excellent inhibitory activity (IC = 0.

Assessing Risk Factors for Prolonged Intensive Care Unit Stay After Surgery for Adult Congenital Heart Disease: A Study From a Lower-Middle-Income Country.

Background Prolonged post-surgery intensive care unit (ICU) stay for congenital heart disease (CHD) has been explored in the pediatric population. However, there is limited data for adult CHD (ACHD), also called grown-up congenital heart (GUCH) disease, especially in low-resource countries where intensive care beds are scarce. This study identifies factors associated with prolonged ICU stay following surgery for ACHD in Pakistan, a lower-middle-income country (LMIC).

Diagnostic value of bronchoscopy in Sars-Cov-2 infection: A systematic review.

Objective: To investigate the diagnostic performance of bronchoscopy in patients with coronavirus disease 2019 infection.

Methods: The systematic review was conducted in April 2021 and comprised search of published articles and preprint servers for original articles assessing diagnostic performance of bronchoscopy in patients with suspected coronavirus disease 2019 infection. The primary outcome of interest was diagnostic sensitivity of bronchoalveolar lavage in the patients.

Synthesis and discovery of potential tyrosinase inhibitor of new coumarin-based thiophenyl-pyrazolylthiazole nuclei: In vitro evaluation, cytotoxicity, kinetic, and computational studies.

A well-known key enzyme in melanogenesis and hyperpigmentation is tyrosinase. The present study introduces a novel series of thiophenyl-pyrazolylthiazole-coumarin hybrids (6a-6h) as tyrosinase inhibitors. The in-vitro tyrosinase inhibition results indicated that all compounds have strong tyrosinase inhibitory activity, particularly compound 6g (IC  = 0.

Synthesis, kinetic studies and investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors.

Deposition of hydroxyapatite (HA) or alkaline phosphate crystals on soft tissues causes the pathological calcification diseases comprising of end-stage osteoarthritis (OA), ankylosing spondylitis (AS), medial artery calcification and tumour calcification. The pathological calcification is symbolised by increased concentration of tissue non-specific alkaline phosphatase (TNAP). An efficient therapeutic strategy to eradicate these diseases is required, and for this the alkaline phosphatase inhibitors can play a potential role.