Effect of Methods and Catalysts on the One-pot Synthesis of Tetrahydropyridine Derivatives: A Mini-Review

As heterocyclic nitrogen molecules, tetrahydropyridines have been recognized as significant constituents of many natural and synthetic compounds, many of which have interesting biological and pharmacological properties. Tetrahydropyridines (THPs) play a pivotal role in synthesizing a range of remedial compounds. They have exhibited impressive curative efficacy for the treatment of numerous diseases. Due to this reason, they are attractive synthetic targets for organic chemists. Several techniques and schemes have been adopted for the synthesis of these molecules. Among these, multicomponent reactions (MCRs) are proved to be one of the best tools for achieving compounds containing complex diversity in a single step and production of their vast libraries. Along with this, the employment of various catalysts makes this technique more vibrant. This review article discussed different catalysts adopted in the synthesis of tetrahydropyridine derivatives via multicomponent reactions to provide information for the development of new-fangled processes aiming at less reaction time, better yield, and minimum side effects. DOI: http://dx.doi.org/10.17807/orbital.v13i4.158

Utility of bone marrow aspiration and trephine biopsy in various haematological malignancies

Background: The bone marrow examination is a useful and cost-effective diagnostic procedure in haematological practice for the diagnosis of haematological disorders. It may either confirm the clinically suspected disease or may provide the previously unsuspected diagnosis. The bone marrow examination can be done by bone marrow aspiration as well as by performing bone marrow biopsy. The aim of the study is to compare the diagnostic accuracy and rate of concordance between two modalities of bone marrow examination in diagnosis of haematological malignancies. Methods: The study was conducted at haematology section of the Department of Pathology, Government Medical College, Jammu spanned over a period of 2.5 years from June 2020 to December 2022. The clinical data along with physical examination, relevant haematological, biochemical and radiological investigations were also reviewed. After taking the informed consent bone marrow aspiration and bone marrow biopsy were done under aseptic precautions. Results: A total of 250 cases of haematological malignancies were studied over a 2.5 year period. The most common haematological malignancy was found to be leukemia 194 (77.6%) cases, followed by plasma cell dyscrasia with 30 (12%) cases, lymphomas and myeloproliferative disorders each with 11 (4.4%) cases and metastatic deposits 4 (1.6%) cases. In the present study, 64/250 (25.6%) patients underwent BMA and trephine biopsy simultaneously. A positive concordance was seen in 46 (71.8%) of the cases between the two methods and diagnostic discordance was observed in 10 (16.3%) of the cases. Conclusions: Bone marrow aspiration and biopsy both complement each other and should be evaluated simultaneously. This study emphasizes the need for greater vigilance in the early diagnosis and an interdisciplinary approach for the effective management of patients as well as inclusion of trephine biopsy as regular procedure for complete evaluation of patients with haematological malignancies

Assessment of labor room communication skills among postgraduate students of obstetrics and gynecology

Background: “Communication with patients” is an important skill needed for every physician in their clinical practice.  These soft skills are required in dealing with patients at every step which include history taking from the patients, explaining them the diagnosis, the prognosis of the disease with associated complications. Dealing with empathy, taking informed consent, explaining the operative procedure and the complications associated with surgery, the art of breaking bad news are the mandatory skills for a good clinician. Labouring women like other patients also require special attention and empathy. So, the residents working in labor room need commitment to develop these soft skills in order to improve the labor room experience of expectant mothers. Objective of this study was to analyse role of a formal training in labor room communication skills among post graduate students of the department of obstetrics and gynecology.Methods: Faculty and students’ sensitization was done after approval from institutional ‘ethics committee’ for conducting this study. Pre-workshop assessment of residents for communication skills attitude and effective communication was done through ‘communication skill attitude scale’ (CSAS) and ‘GAP-KALAMAZOO scale’. Workshop for communication skills on the framework of Calgary Cambridge patient interview model and online teaching of students through what’s app videos, role-play demonstrations was followed by reassessment of the residents through above used scales.Results: Results depicted both improvements in attitude and effective communication skills among residents. 100% of the students were convinced and opined that good communication skills necessary for perfect clinical practice.Conclusions: The skill to communicate with patients is a fine art and needs to be mastered to be a good clinician. A formal training in effective communication skills is absolutely necessary to bring professionalism in medical practice

A prospective randomized study to compare dexmedetomidine and dexamethasone as an adjunct to bupivacaine in transversus abdominis plane block for post-operative analgesia in caesarean delivery

Background: Caesarean section is most frequently performed surgery worldwide. Patients experience moderate to severe pain in the first 48 hours post-operatively. Aim of this study was to evaluate the efficacy of dexmedetomidine and dexamethasone as an adjunct to bupivacaine in ultrasound guided TAP block for postoperative analgesia in patients of caesarean section.Methods: A total 120 ASA I and II patients undergoing elective and emergency caesarean section under subarachnoid block were randomly divided into three groups B, BDM, BDX to receive bupivacaine alone or dexmedetomidine or dexamethasone as an adjunct to bupivacaine in ultrasound guided TAP block. Postoperatively, the patients were evaluated for pain level at rest and on movement with a 10 cm visual analog scale (VAS) pain score (0 = no pain and 10 = worst pain), time to demand of first analgesic request, number of analgesic requirements, nausea or vomiting, sedation and patient satisfaction at 0 hours and at 2, 4, 6, 12, 18, and 24 hours.Results: VAS score was significantly higher in group B in comparison to BDM and BDX, and higher in BDX in comparison to group BDM. Mean duration of analgesia was significantly higher in group BDM in comparison to group B and BDX. Total number of rescue analgesic demands were significantly lower in group BDM in comparison to group B and BDX. Sedation score and satisfaction score was higher in group BDM as compared to group B and BDX.Conclusions: Addition of dexmedetomidine and dexamethasone as an adjunct to bupivacaine reduces postoperative pain, prolongs analgesia, decreases demand for additional analgesics and provides better maternal satisfaction as compared to plain bupivacaine group in TAP block in patients undergoing caesarean section under subarachnoid block. Among dexmedetomidine and dexamethasone, dexmedetomidine had prolonged analgesia as compared to dexamethasone group

GW627368X inhibits proliferation and induces apoptosis in cervical cancer by interfering with EP4/EGFR interactive signaling

PGE2, the major product of cyclooxygenases implicated in carcinogenesis, is significantly upregulated in cervical cancer. PGE2 via prostanoid receptor EP4 stimulates proliferation and motility while inhibiting apoptosis and immune surveillance. It promotes angiogenesis by stimulating the production of pro-angiogenic factors. The present study demonstrates GW627368X, a highly selective competitive EP4 antagonist, which hinders cervical cancer progression by inhibiting EP4/Epithelial Growth Factor Receptor (EGFR) interactive signaling. GW627368X reduced Protein Kinase A (PKA) phosphorylation which in turn leads to decreased cAMP response element-binding protein (CREB) activation. Decreased PKA phosphorylation also directly enhanced Bax activity and in part reduced glycogen synthase kinase 3 (GSK3)β phosphorylation. Owing to the interactive signaling between EP4 and EGFR, GW627368X lowered EGFR phosphorylation in turn reducing Akt, Mitogen-activated Protein Kinase (MAPK) and GSK3β activity significantly. Sublethal dose of GW627368X was found to reduce the nuclear translocation of β-catenin in a time dependent manner along with time-dependent decrease in cytoplasmic as well as whole-cell β-catenin. Decreased CREB and β-catenin transcriptional activity restricts the aberrant transcription of key genes like EP4, cyclooxygenase (COX)-2, vascular endothelial growth factor and c-myc, which ultimately control cell survival, proliferation and angiogenesis. Reduced activity of EGFR resulted in enhanced expression of 15-hydroxyprostaglandin dehydrogenase increasing PGE2 degradation thereby blocking a positive feedback loop. In xenograft model, dose-dependent decrease in cancer proliferation was observed characterized by reduction in tumor mass and volume and a marked decrease in Ki67 expression. A diminished CD31 specific staining signified decreased tumor angiogenesis. Reduced expression of pAkt, pMAPK, pEGFR and COX-2 validated in vitro results. GW627368X therefore effectively inhibits tumor survival, motility, proliferation and angiogenesis by blocking EP4/EGFR interactive signaling. EP4 is a potent therapeutic target in cervical cancer and can be explored in combination with conventional therapies to attain superior outcomes and to overcome complications associated with organ toxicities, therapeutic resistance and disease relapse

Designing of bentonite based nanocomposite hydrogel for the adsorptive removal and controlled release of ampicillin

© 2020 In pharmacy, semisynthetic antibiotics with beta-lactam ring are the most prominently used drugs. The use of these drugs for humans and animals is continuously expanding. Their presence in the water system even at low concentrations can prove to be fatal to living beings. Also, they can even grow antibiotic-resistant bacteria and thus elimination of such drugs becomes very essential. Our study is focused on batch experiments for adsorptive removal of ampicillin (AMP) and its cumulative release in different solutions using xanthan gum-cl-poly(itaconic acid)/bentonite (XG-cl-poly(IA)/BN) nanocomposite hydrogel. It was synthesized by facile microwave method. The adsorption data of AMP was analyzed using various isotherm models such as Langmuir, Freundlich, Temkin and kinetic models such as Pseudo-first order, Pseudo-second order and Intraparticle diffusion. The maximum adsorption capacity as determined from Langmuir model was 245.09 mg/g at 318 K and solution pH 7. Also, XG-cl-poly(IA)/BN nanocomposite hydrogel was evaluated for AMP release in distilled water and at different pH solutions (2.2, 5.4, 7.4 and 9.4). The maximum AMP release was observed at pH 2.2 (37%)

Biliary sludge and recurrent ketoacidosis: a case report

A five year old boy, weighing 14 kg with no family history of diabetes, presented in frank diabetic ketoacidosis. He recovered, but continued to have episodes of ketoacidosis. He was diagnosed to have biliary sludge, which recovered with insulin treatment