Synthesis of novel ciprofloxacin-avibactam conjugates for the development of second-generation non-ß-lactam-ß-lactamase inhibitors.

To overcome the antibiotic resistance challenge, we synthesized a novel class of conjugates based on ciprofloxacin and avibactam, covalently linked by diverse amino acids. In vitro studies of these conjugates have shown improved antibacterial efficacy of avibactam when used alone against some ESKAPE pathogens, i.e., S. aureus, E. coli, and A. baumannii. Further, ceftazidime was screened in combination with all conjugates and found to be less synergistically effective than avibactam-ceftazidime co-dosing against K. pneumoniae and E. coli bacterial strains. Subsequently, the top-ranked active conjugates were investigated against the commercially available ß-lactamase-II (Penicillinase from Bacillus cereus) through in vitro studies. These studies elucidated two conjugates i.e, 9 (IC50 = 1.69±0.35 nM) and 24b (IC50 = 57.37±5.39 nM), which have higher inhibition profile than avibactam (IC50 = 141.08±12.20 nM). These outcomes allude to avibactam integration with ciprofloxacin is a novel and fruitful approach to discovering clinically valuable next-generation non-ß-lactam-ß-lactamase inhibitors.

Recent progress in the homogeneous gold-catalysed cycloisomerisation reactions.

In the last two decades, interest in reactions catalysed by gold complexes has tremendously increased due to their ability to tolerate a variety of functional groups and their capability to activate various unsaturated groups. In this review, gold-catalysed cycloisomerisation reactions of ynamides, diynes and 1,n-enynes have been summarized. These gold-catalysed cycloisomerisation reactions open new opportunities for synthesising a range of new complex polycyclic chemical moieties in one step. Gold-catalysed cycloisomerisation is a valuable way for synthesising fused spiro carbocycles, BODIPY cores, bicyclo[3.2.1]oct-2-ene, dihydro benzo[b]thiepine, disubstituted furans, spiroindolines, bridged [n.2.1] skeletons, etc.

Effect of Intravenous Calcium Gluconate on Prevention of Post Spinal Hypotension during Spinal Anaesthesia for Caesarean Section: A Randomized Double-Blind Controlled Study.

BACKGROUND: Calcium, a physiological ion, causes vasoconstriction and has a positive ionotropic action on heart. Its use to prevent post-spinal hypotension has been suggested but never formally evaluated for patients undergoing caesarean section. This study investigated the hemodynamic effects of calcium administration in parturients with the primary aim of comparing the incidence of post-spinal hypotension. METHODS: Sixty healthy full-term pregnant patients scheduled for caesarean section were randomly allocated to two equal groups to receive either calcium gluconate or normal Saline bolus over 20min by syringe infusion pump under electrocardiography monitoring immediately after the patient was turned supine following spinal anaesthesia. Blood pressure and heart rate were recorded at baseline, and at regular intervals following spinal. Maternal calcium levels were estimated before and after infusion. Neonatal blood gas analysis and calcium level were analyzed. Total mephentermine requirement was recorded in both groups. RESULTS: The heart rate values remained comparable to baseline value in group calcium gluconate while in group normal Saline, it decreased significantly at 8,12 and 16min. Blood pressure decreased significantly as compared to the baseline value from 4min onwards in both the groups. However, it was comparable in the two groups at all time points(0.622). Nineteen patients(63.33%) required mephentermine infusion in group calcium gluconate as compared to 23 patients(76.6%) in group normal Saline for maintenance of systolic blood pressure.(p=0.791) Umbilical venous pH (p=0.038) and partial pressure of carbon dioxide(p=0.038) were significantly better in group calcium gluconate. CONCLUSIONS: Calcium used for prophylaxis of hypotension in healthy parturients undergoing caesarean section reduced the vasopressor requirements and total mephenteramine dose, but the difference did not attain statistical significance.

MedHypChain: A patient-centered interoperability hyperledger-based medical healthcare system: Regulation in COVID-19 pandemic.

Recently, an infectious disease, coronavirus disease 2019 (COVID-19), has been reported in Wuhan, China, and spread worldwide within a couple of months. There have been seen an outbreak of COVID-19 in many countries, where the infected patients' rate overwhelmed the inadequate medical services. The push of patient-centered interoperability (PCI) from medical institution-centered interoperability may defeat the current and post resultant disease of the COVID-19 pandemic. This paper proposes a state-of-the-art privacy-preserving medical data sharing system based on Hyperledger Fabric (MedHypChain), where each transaction is secured via an Identity-based broadcast group signcryption scheme. We proved that MedHypChain achieves confidentiality, anonymity, traceability, and unforgeability. Besides, we regularize the MedHypChain to implement the PCI healthcare system, where the patient manages its health-related information in the blockchain that can be accessible to the authorized entity. We also use the Hyperledger caliber as a benchmark tool to analyze the performance of MedHypChain in three metrics (latency time, execution time, and throughput) for up to 20 permissioned nodes. Finally, we compare MedHypChain with related blockchain-based healthcare systems and found that the proposed scheme needs the least computation cost and communication cost and achieves all security features, such as authenticity, scalability, and access control.

Prakriti Analysis of COVID 19 Patients: An Observational Study.

RATIONALE & OBJECTIVE: The concept of Prakriti is unique to Ayurveda, which is used for deciding the preventive and curative strategy to be adopted in the treatment of patients. It is the total of anatomical, physiological, and psychological domains of an individual. The diseases often manifest by susceptibility that depends upon Prakriti of individuals. COVID 19 is a new disease, where the status of the susceptibility of its victim in terms of Prakriti is not known. This study has been undertaken to determine the Prakriti of COVID 19 positive patients. METHOD: The validated instrument CCRAS Prakriti assessment scale has been applied to the COVID 19 positive patients admitted between 16 May 2020 to 10 June 2020 at COVID hospital. RESULT: Data of 117 patients aged 10 to 80 years have been analyzed. The ratio of male-female patients was 1.8:1. Most patients belonged to Vata-KaphaPrakriti (27%).Individuals with their Prakriti found in order of frequency were Pitta-Kapha (21%), Kapha (20%), Vata (13%), Vata-Pitta (11%), Sama (4%) and Pitta (3%). CONCLUSION: Patients with Vata-Kapha, Pitta-Kapha, and Kapha dominant Prakriti have been found more in COVID19. The treatment strategies can be accordingly decided in respect of each patient.

Effect of phytohormones on seed germination and seedling growth of Coriandrum sativum L.

Coriander commonly known as Dhania or Chinese parsley is generally grown for its use in soups, salads, dressing vegetables, seasoning and chutney. Effect of two phytohormones viz. GA3 and 2,4-D on seed germination, seedling growth and various physiological and biochemical parameters were studied. The hormones were applied individually in different concentrations (10, 50 and 100 µM concentrations). Both the hormones enhanced the germination percentage, seedling growth (root and shoot length), leaf area, chlorophyll and carotenoid content. The application of these hormones also decreased the germination time. Maximum germination, shoot length, leaf area and carotenoid content was observed in 100 µm concentration of GA3. Root length, chl. a and chl. b was maximum in 50 µM of 2,4-D and 100 µm GA3, respectively. The application of two hormones exhibited a marked increase on all the parameters studied as compared to the control.

Cobalt, nickel, copper and zinc complexes with 1,3-diphenyl-1H-pyrazole-4-carboxaldehyde Schiff bases: antimicrobial, spectroscopic, thermal and fluorescence studies.

Two new Schiff bases of 1,3-diphenyl-1H-pyrazole-4-carboxaldehyde and 4-amino-5-mercapto-3-methyl/H-1,2,4-triazole [HL(1-2)] and their Cobalt, Nickel, Copper and Zinc complexes have been synthesized and characterized by elemental analyses, spectral (UV-vis, IR, (1)H NMR, Fluorescence) studies, thermal techniques and magnetic measurements. A square planar geometry for Cu(II) and octahedral geometry for Co(II), Ni(II) and Zn(II) complexes have been proposed. In order to evaluate the biological activity of Schiff bases and to assess the role of metal ion on biological activity, the pyrazole Schiff bases and their metal complexes have been studied in vitro antibacterial against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa and antifungal against Aspergillus niger, and Aspergillus flavus. In most of the cases higher activity was exhibited upon coordination with metal ions.

Cardiorenal syndrome.

Very often, physicians confront with patients who have concomitant heart and kidney failure. The coexistence of kidney and heart failure carries an extremely bad prognosis. The exact cause of deterioration of kidney function and the mechanism underlying this interaction are complex, multifactorial in nature, and still not completely understood. Both the heart and the kidney act in tandem to regulate blood pressure, vascular tone, diuresis, natriuresis, etc. An extension to the Guytonian model of volume and blood pressure control is proposed called cardiorenal connection. Regulating actions of Guyton's model were coupled to their extended actions on structure and function of the heart and the kidney changes in the rennin-angiotensin-aldosterone system, the imbalance between nitric oxide and reactive oxygen species, the sympathetic nervous system, and inflammation are the cardiorenal connectors to develop cardiorenal syndrome. Imbalance in this closed complex will often lead to deterioration of both cardiac and kidney function. The World Congress of Nephrology emphasized vast interrelated derangements that can occur in cardiorenal syndrome and proposed that the recent definition of cardiorenal syndrome be modified into categories whose labels reflect the likely primary and secondary pathology and time frame. For management, drugs that impair kidney function are undesirable, particularly in a population with already compromised or at risk of kidney function. In severe volume-loaded patients who are refractory to diuretics, management of cardiorenal dysfunction is challenging. In the absence of definitive clinical trials, treatment decision must be based on a combination of patient's condition and understanding of individual treatment options.