Effectiveness of blended versus fully digital training in primary care psychiatry: A retrospective comparison from India.

Objectives: We compared effectiveness of blended mode (consisting of traditional classroom teaching and e-learning sessions) and fully digital mode (e-learning sessions alone) of primary care psychiatry training for primary care doctors in Chhattisgarh. Materials and Methods: We retrospectively compared the engagement in training, knowledge (K), attitude (A), and practice (P) in primary care psychiatry, and patient identification by primary care doctors (n = 941) from Chhattisgarh region who underwent training through either blended training mode (n = 546) or fully digital training mode (n = 395) for 16 h each, using Clinical Schedules for Primary Care Psychiatry based modules between June 2019 and November 2020 with a tertiary care center (NIMHANS, Bengaluru) as hub. Statistical Analysis: The Statistical Package for the Social Sciences version 27 was used to analyze the data. Continuous variables were analyzed using the independent samples t-test, and discrete variables were analyzed using the Chi-square test. A repeated measures analysis of variance (ANOVA) (two-way mixed design) was used to see the interaction of training type and time of pre- and post-KAP measurement while controlling for years of experience. The number of patients identified by both training groups over 8 months was also compared using the repeated measures ANOVA (two-way mixed design). Results: Engagement inferred by the number of participants completing pre-KAP forms (75%), post-KAP forms (43%), post-session assessments (37- 47%), case presentation (33.9%), and certification (32.1%) was better in the blended group (P < 0.05). The mean gain in KAP scores was significantly higher in the blended group controlling for the years of experience as primary care doctor (PCD) (F = 30.36, P < 0.001). PCDs in the blended training group consistently identified a higher number of patients with mental illness over 8 months of follow-up (F = 6.21, P < 0.001). Conclusion: The blended mode yielded better results in primary care psychiatry training compared to fully digital mode. In-person interactions while provided for a very brief proportion of the training seem to have an unmistakable imprint on the outcomes and seem critical for better consolidation and assimilation of information, which translates into better practice.

Multipronged Phenotyping Approaches to Characterize Sugarcane Root Systems.

Roots are the primary conductors of water and nutrients and play a vital role in sustaining growth and yield under stressful environments. The study of plant roots poses methodological difficulties in in situ assessment and sampling, which is especially true for sugarcane (Saccharum spp.). Traditional methods during the 1920s documented the genotypic variation in sugarcane root systems, after which few studies were reported on sugarcane root traits per se until recently. In addition to morphology, rhizosphere characteristics, including allelopathic effects and/or affinity for microbial symbiosis, determine plant establishment and survival. Ultimately, root systems define the above-ground productivity of sugarcane. With the impetus for climate-resilient varieties, it is becoming more relevant to explore and utilize the variability in root system traits of sugarcane. This paper describes multipronged approaches for sugarcane root phenotyping, including field excavation by trench sampling, the use of a root core sampler, raised platforms for root sampling, and raising plants under hydroponic culture, employed by a team of scientists at the Indian Council of Agricultural Research-Sugarcane Breeding Institute (ICAR-SBI). Field excavation by trench sampling is imperative to assess the plant roots in their natural growing environment. The use of raised platforms simulating field conditions and a root core sampler are alternative approaches, with a considerable reduction in time, uniform sample size, and less loss of root material. Hydroponic plant culture allows the study of morphology, anatomical features, and rhizosphere biology, including the exudation of organic compounds and microbial interactions. Data generated from different experiments using diverse sampling methods add to the wealth of information on the root system traits of sugarcane.

Whole genome analysis and functional characterization of a novel Bacillus thuringiensis (Bt 62) isolate against sugarcane white grub Holotrichia serrata (F).

In this study, we report the whole genome assembly of Bt 62, a novel isolate harbouring cry8 holotype gene identified by us earlier. Sequencing was carried out using a combination of Illumina NextSeq 500 and Oxford Nanopore sequencing Technologies (ONT). The final assembled genome was 6.13 Mb comprising a circular chromosome and four plasmids. The bioassay studies against Holotrichia serrata (F.) (Coleoptera: Scarabaeidae), a polyphagous pest infesting sugarcane and other crops, indicated significant toxicity to first instar grubs over untreated larvae achieving a highest mean mortality of 91.11% for various doses tested. In vitro proteolytic assay and histopathological studies of the midgut of infected white grubs revealed proteolytic processing of the protoxin and extensive degeneration of larval midgut epithelial cells. The results demonstrate that this novel isolate could be used as a biopesticide or its crystal toxin genes could be expressed in sugarcane and other crops for resistance against H. serrata.

Symptomatic post-vaccination SARS-CoV-2 infections in healthcare workers- A multicenter cohort study.

BACKGROUND AND AIMS: During the COVID-19 vaccination program in India, the healthcare workers were given the first priority. There are concerns regarding the occurrence of breakthrough infections after vaccination. We aimed to investigate the effictiveness of COVID-19 vaccines in preventing and reducing the severity of post-vaccination infections. METHODS: This retrospective test-negative case-control study examined 28342 vaccinated healthcare workers for symptomatic SARS-CoV-2 infections between January 16 to June 15, 2021. They worked at 43 Apollo Group hospitals in 24 Indian cities. These cohorts received either ChAdOx nCOV-19 (Recombinant) or the whole virion inactivated Vero cell vaccines. Various demographic, vaccination related and clinical parameters were evaluated. RESULTS: Symptomatic symptomatic post-vaccination infections occurred in a small number of vaccinated cohorts (5.07%, p < 0.001), and these were predominantly mild and did not result in hospitalization (p < 0.0001), or death. Both vaccines provided similar protection, with symptomatic infections in 5.11% and 4.58%, following ChAdOx nCOV-19 (Recombinant) and the whole virion inactivated Vero cell vaccines, respectively (p < 0.001). Nursing and Clinical staff and cohorts >50 years contracted more infections (p < 0.001). Two-dose vaccination has significantly lower odds of developing symptomatic infection (0.83, 95%CI - 0.72 to 0.97). Maximum infections occurred during the peak of the second COVID-19 wave from mid-April to May 2021 (p < 0.001). No significant difference existed in the infection between sex, vaccine type, and the number of vaccine doses received (p ≥ 0.05). CONCLUSION: Symptomatic infections occurred in a small percentage of healthcare workers after COVID vaccination. Vaccination protected them from not only infection but also severe disease.

SARS-CoV-2 infection after COVID-19 immunization in healthcare workers: A retrospective, pilot study.

BACKGROUND & OBJECTIVES: COVID-19 pandemic has taken a significant toll on the health of the people across the globe, including India, and is still continuing with its rapidly evolving second wave. Although the COVID-19 vaccines effectively prevent infection, yet some cases of infections have been reported post-vaccination, raising concerns about their efficacy and safety. This study was aimed to investigate the occurrence of SARS-CoV-2 infection among the symptomatic-vaccinated healthcare workers (HCWs) and to analyze the severity of their disease. METHODS: This retrospective study was done at a single multispecialty hospital, on the HCWs who have had COVID-19 vaccination, during the initial period of the vaccination drive (January 16 to April 24, 2021). The symptomatic post-vaccination infections in these HCWs were evaluated. RESULTS: Eighty five of 3235 (2.63%) vaccinated HCWs acquired the SARS-CoV-2 infection after vaccination, during the study period. Of these, 65 (76.5%) were fully vaccinated (FV), and 20 (23.5%) were partially vaccinated (PV) and the protection rate of vaccination was 97.4 per cent [95 % confidence interval (CI)=96.8-97.9]. The odds ratio of acquiring infection among females was higher at 1.84 (95% CI=1.17-2.88; P=0.008) mainly because of their greater involvement in the patient care as nursing personnel. The chances of infections were the highest in the medical and nursing personnel, as compared to paramedical, administrative and supporting staff (P<0.001). Among the HCWs studied, only two required hospitalization (0.06%), none needed an intensive care unit (ICU) admission and there were no deaths. INTERPRETATION & CONCLUSIONS: The COVID-19 infection after vaccination occurred in a smaller subset (2.63%) of HCWs, in both PV and the FV groups. These infections were primarily minor and did not lead to severe disease. Overall, the vaccination with ChAdOx1 nCoV-19 vaccine (recombinant) prevented SARS-CoV-2 severe infection in the HCWs, leading to ICU admission and deaths.

Perspectives, attitude, and practice of lithium prescription among psychiatrists in India.

INTRODUCTION: Lithium "the magic pill" past its discovery remained the respite for patients with bipolar disorders for decades. The prescriptions of lithium were replaced by other drugs because of the cumbersome monitoring, adverse effect profile, narrow therapeutic index, and frequent comorbidities in patients. The objectives of this study were to understand the knowledge, attitude, and practice of lithium by a subset of psychiatrists in India, which will help us understand the theory-practice gap and for devising strategies to bridge the existing gap. MATERIALS AND METHODS: The current study was an online survey which included 103 psychiatrists from India of either gender and any age group. Predesigned questionnaire about the knowledge, attitude, and practice of lithium use was circulated for 1 month (March 2018). We received 135 responses (31% response rate), of which 32 were incomplete. Hence, the total sample of psychiatrists included in the study was 103. RESULTS: The results suggest that most practitioners included in the survey had knowledge about the effects, adverse effects, and the monitoring protocols and were comfortable in using lithium in patients on outpatient basis. Despite being aware of the indications, the psychiatrists were skeptical in starting lithium due to multitude of perceived barriers such as comorbidities, patient's low adherence to blood monitoring, and adverse effects. CONCLUSIONS: Clinicians should be well aware of the adverse effects, monitoring protocols, which will help them to use lithium in a more appropriate manner.

Buprenorphine/naloxone maintenance for "poppy husk" dependence: A retrospective study.

INTRODUCTION: Despite a significant number of patients dependent on "poppy husk" in India, they are poorly characterized. Moreover, scarce data is available with respect to their treatment. METHODS: A cohort of 148 patients with "poppy husk" dependence receiving substitution treatment with buprenorphine/naloxone were followed up for 4 years, using a retrospective chart-based assessment. Baseline demographic and substance-related characteristics were described. Retention rates (operationally redefined as "6 months of uninterrupted contact anytime during their visits") over the next 4 years and their predictors were assessed. RESULTS: Mean age of onset of "poppy husk" use was found to be 27.51 years, and mean duration of dependence was 18.25 years. Mean amount of poppy husk consumed per month was 3.7 kg. Commonest reasons for initiating and quitting its use were enhancing work efficiency and lack of availability, respectively. Retention rates were 25%. Significant predictors of retention were age more than 40 years (OR = 2.295; 95%CI = 1.015-5.19) and uninterrupted treatment duration for at least 1 month from first contact (for 1 month (OR = 5.625; 95%CI = 2.28-13.89), for 3 months (OR = 10.96; 95%CI = 4.65-25.85), and for 6 months (OR = 52.8; 95%CI:14.08-197.98). DISCUSSION: Factors associated with occupation such as enhancing work efficiency and overcoming fatigue are related to use of "poppy husk." While the amount of intake is considerably large among treatment seekers who are dependent on it, their dependence duration is longer and retention rates lower than those reported for patients with prescription and injectable opioid dependence. Specific strategies to tap patients less than 40 years and to target uninterrupted contact in initial phases of maintenance should be developed.

Internet addiction and daytime sleepiness among professionals in India: A web-based survey.

BACKGROUND: The likelihood of the relation between Internet overuse and comorbid psychiatric conditions is on the rise. However, sleep disturbances are common psychiatric symptoms associated with internet overuse. Our objective was to examine the association of Internet overuse with excessive daytime sleepiness, sleep problems in professionals from India. MATERIALS AND METHODS: This was a web-based cross-sectional study through a predesigned questionnaire which included various professional groups. The information included in the questionnaire was sociodemographic details, Young's internet addiction test (IAT) and Epworth sleepiness scale (ESS). RESULTS: About 1.0% of total sample population had severe internet addiction whereas 13% were in the range of moderate internet addiction and the mean score on IAT was found to be 32 (standard deviation [SD] = 16.42). The mean duration of total night time sleep (5.61 ± 1.17) is significantly lower in participants with moderate and severe internet addiction (6.98 ± 1.12) compared to those with no and mild internet addiction. The mean scores of ESS were significantly higher in individuals with moderate and severe addiction (M = 10.64, SD = 4.79). We found that sleepiness while in 5 of the situations such as driving a car (χ2 = 27.67; P < 0.001), sitting and reading (χ2 = 13.6; P = 0.004), traveling in a car (χ2 = 15.09; P = 0.002), afternoon rest time (χ2 = 15.75; P = 0.001), and postlunch quiet time (χ2 = 24.09; P < 0.001), predicted membership to moderate-to-severe internet addiction, even after controlling for the confounding effects of age and gender. CONCLUSIONS: This study shows an association between Internet overuse, excessive daytime sleepiness, and other sleep problems. Clinicians should be proactive and conscious in scrutinizing the patients for internet addiction and its consequences.

Evaluation of Therapeutic Potential of Eugenol-A Natural Derivative of Syzygium aromaticum on Cervical Cancer

Background: The intendment of this study is to determine the pursuance in ­ vitro anticancer activity and cytotoxicity of Syzygium aromaticum against the human cervical cancer cell line (HeLa) compared to the normal cell lines. Apoptogenic properties of DCM extract of Eugenol was determined in this entire study. Materials and Methods: HeLa cell lines were cultured in DMEM medium and incubated with different concentration of DCM ­ Eugenol extract. MTT assay brought out the way to determine the cell viability and quantification was done with the optical absorbance at 570 nm and 620 nm as reference. Apoptotic cells were affirmed by dual staining using acridine orange bromide. Besides, the morphology of the nucleus was also confirmed by dual staining. Eugenol inhibited 50% growth (IC50) of HeLa cell lines at 200 mg/ml of extract concentration. Results: Inhibitory efficacy of eugenol isolated from Syzyzgyium aromaticum showed the cell ­ viability in time and dose dependent manner with consistent morphological changes. Flow cytometer determined the apoptosis confirming the cytotoxicity value for MTT at IC50 with 81.85% cell viability. Dual staining firmly enacts the damaged cells due to AO indicating apoptosis confirmation by dual staining. Morphological analysis also clearly states that nil apoptosis has been seen in control and similarly in eugenol treated when compared to cancerous HeLa cell ­ line. Conclusion: Evaluation of cytotoxicity effect of eugenol isolated from Syzygium aromaticum showed it can be unrivalled dormant source of prodigious changes in HeLa cell line indicating (revealing) that chemotherapeutic agent.

Molecular evolution and functional divergence of eukaryotic translation initiation factor 2-alpha kinases.

Eukaryotic translation initiation factor 2-alpha kinase (EIF2AK) proteins inhibit protein synthesis at translation initiation level, in response to various stress conditions, including oxidative stress, heme deficiency, osmotic shock, and heat shock. Origin and functional diversification of EIF2AK sequences remain ambiguous. Here we determine the origin and molecular evolution of EIF2AK proteins in lower eukaryotes and studied the molecular basis of divergence among sub-family sequences. Present work emphasized primitive origin of EIF2AK4 sub-family gene in lower eukaryotes of protozoan lineage. Phylogenetic analysis supported common origin and sub-family based classification of EIF2AKs. Functional divergence studies across sub-families revealed several putative amino acid sites, which assist in altered protein interactions of kinase domains. The data can facilitate designing site-directed experimental studies aiming at elucidating diverse functional aspects of kinase domains regarding down-regulation of protein synthesis.

Synthesis, Characterization, Crystal Structure and Molecular Docking Studies of a S-methyldithiocarbazate Derivative: Bis[2-hydroxy- benzylidenehydrazono) (methylthio)methyl]disulfide.

The title compound bis[2-hydroxybenzylidenehydrazono)(methylthio)methyl]disulfide (1), an S-methyldithiocarbazate derivative with a disulfide bond has been synthesized by the condensation of 2-hydroxybenzaldehyde with S-methyldithiocarbazate. It has been characterized by elemental analyses, 1H, 13C NMR and FT-IR spectroscopy and mass spectrometry. The single crystal X-ray structure shows that the compound exists in a tautomeric thione form with the dithiocarbazate fragment adopting an EE configuration with respect to the C=N bond of the benzylidene moiety. The thermal behaviour of the compound has been studied using thermogravimetric analysis (TGA). The molecular geometry of the compound in the ground state has been optimized using density functional theory (DFT/B3LYP) method with the 6-311++G(d,p) basis sets. Molecular docking of the compound with human carbonic anhydrase II has been performed to probe the nature of interaction.

Viral Evolved Inhibition Mechanism of the RNA Dependent Protein Kinase PKR's Kinase Domain, a Structural Perspective.

The protein kinase PKR activated by viral dsRNA, phosphorylates the eIF2α, which inhibit the mechanism of translation initiation. Viral evolved proteins mimicking the eIF2α block its phosphorylation and help in the viral replication. To decipher the molecular basis for the PKR's substrate and inhibitor interaction mechanisms, we carried the molecular dynamics studies on the catalytic domain of PKR in complex with substrate eIF2α, and inhibitors TAT and K3L. The studies conducted show the altered domain movements of N lobe, which confers open and close state to the substrate-binding cavity. In addition, PKR exhibits variations in the secondary structural transition of the activation loop residues, and inter molecular contacts with the substrate and the inhibitors. Phosphorylation of the P+1 loop at the Thr-451 increases the affinity of the binding proteins exhibiting its role in the phosphorylation events. The implications of structural mechanisms uncovered will help to understand the basis of the evolution of the host-viral and the viral replication mechanisms.

A Preliminary Study to Forecast Japanese Encephalitis Vector Abundance in Paddy Growing Area, with the Aid of Radar Satellite Images.

Vector mosquitoes of Japanese encephalitis (JE) breed mostly in rice fields, and human cases occur scattered over extended rural rice-growing areas. From this, one may surmise an ecological connection with the irrigation facilities and paddy cultivation. Furthermore, it has been hypothesized that a particular stage of paddy growth is a premonitory sign that can lead to a markedly increased population of the vector mosquitoes. The present study aimed to forecast the vector abundance by monitoring the paddy growth using remote sensing and geographical information systems. The abundance of the JE vector Culex tritaeniorhynchus peaked when the paddy crop was at its heading stage and dipped when the crop reached the maturing stage. A significant positive correlation was observed between paddy growth and adult density (r = 0.73, p < 0.008). The sigma naught values (σ0) derived from satellite images of paddy fields ranged from -18.3 (during transplantation stage) to approximately -10 (during the noncultivation period). A significant positive correlation was observed between σ0 and paddy growth stages (r = 0.87, p < 0.05) and adult vector density (r = 0.74, p = 0.04). The σ0 value observed during the vegetative and flowering stages of paddy growth ranged from -17.6 to -17.16, at which period the vector density started building up. This could be the spectral signature that denotes the "risk," following which a high vector abundance is expected during heading stage of the paddy.

Synthesis, characterization, and electronic structure of new type of heterometallic boride clusters.

The reaction of [Cp*TaCl(4)], 1 (Cp* = η(5)-C(5)Me(5)), with [LiBH(4)·THF] at -78 °C, followed by thermolysis in the presence of excess [BH(3)·THF], results in the formation of the oxatantalaborane cluster [(Cp*Ta)(2)B(4)H(10)O], 2 in moderate yield. Compound 2 is a notable example of an oxatantalaborane cluster where oxygen is contiguously bound to both the metal and boron. Upon availability of 2, a room temperature reaction was performed with [Fe(2)(CO)(9)], which led to the isolation of [(Cp*Ta)(2)B(2)H(4)O{H(2)Fe(2)(CO)(6)BH}], 3. Compound 3 is an unusual heterometallic boride cluster in which the [Ta(2)Fe(2)] atoms define a butterfly framework with one boron atom lying in a semi-interstitial position. Likewise, the diselenamolybdaborane, [(Cp*Mo)(2)B(4)H(4)Se(2)], 4 was treated with an excess of [Fe(2)(CO)(9)] to afford the heterometallic boride cluster [(Cp*MoSe)(2)Fe(6)(CO)(13)B(2)(BH)(2)], 5. The cluster core of 5 consists of a cubane [Mo(2)Se(2)Fe(2)B(2)] and a tricapped trigonal prism [Fe(6)B(3)] fused together with four atoms held in common between the two subclusters. In the tricapped trigonal prism subunit, one of the boron atoms is completely encapsulated and bonded to six iron and two boron atoms. Compounds 2, 3, and 5 have been characterized by mass spectrometry, IR, (1)H, (11)B, (13)C NMR spectroscopy, and the geometric structures were unequivocally established by crystallographic analysis. The density functional theory calculations yielded geometries that are in close agreement with the observed structures. Furthermore, the calculated (11)B NMR chemical shifts also support the structural characterization of the compounds. Natural bond order analysis and Wiberg bond indices are used to gain insight into the bonding patterns of the observed geometries of 2, 3, and 5.

In vitro antibiotic susceptibility of rapidly growing nontuberculous mycobacteria isolated from patients with microbial keratitis.

PURPOSE: This study was undertaken to determine the antibiotic susceptibility and minimum inhibitory concentrations (MIC) of amikacin, tobramycin, ciprofloxacin, gatifloxacin, azithromycin, and clarithromycin against rapidly growing nontuberculous mycobacteria isolated from patients with keratitis. METHODS: A total of 15 rapidly growing nontuberculous mycobacteria isolated from corneal scrapings of keratitis patients from January 1999 through December 2007 were subjected to antimicrobial susceptibility testing by the E-Test to amikacin, tobramycin, ciprofloxacin, gatifloxacin, azithromycin, and clarithromycin. RESULTS: Out of 15 isolates, 13 were identified as Mycobacterium chelonae complex and 2 as Mycobacterium fortuitum complex. Based on minimum inhibitory concentration (MIC) cut off, all 15 (100%) isolates were sensitive to amikacin, azithromycin, and clarithromycin, 13 (86%) were sensitive to tobramycin, nine (60%) to gatifloxacin, and only 6 (40%) to ciprofloxacin. The MIC range was 0.25-4 microg/ml for amikacin, 0.5-1 microg/ml for azithromycin, 0.125-1 microg/ml for clarithromycin, 0.5-16 microg/ml for ciprofloxacin, and 0.25-16 microg/ml for tobramycin. MIC(90) for amikacin was 2 microg/ml, azithromycin 1 microg/ml, clarithromycin 0.75 microg/ml, ciprofloxacin 8 microg/ml, gatifloxacin 8 microg/ml, and for tobramycin it was 4 microg/ml. CONCLUSIONS: All the isolates were sensitive to amikacin, azithromycin, and clarithromycin, but the MIC values of clarithromycin and azithromycin were lower than amikacin. Based on in vitro susceptibility results it appears that the topical amikacin in combination with oral clarithromycin or azithromycin is the best treatment option for rapidly growing nontuberculous mycobacterial keratitis.

Vertex-fused metallaborane clusters: synthesis, characterization and electronic structure of [(eta5-C5Me5Mo)3MoB9H18].

The reaction of the [(eta(5)-C(5)Me(5))MoCl(4)] complex with [LiBH(4).THF] in toluene at -70 degrees C, followed by pyrolysis at 110 degrees C, afforded dark brown [(eta(5)-C(5)Me(5)Mo)(3)MoB(9)H(18)], 2, in parallel with the known [(eta(5)-C(5)Me(5)Mo)(2)B(5)H(9)], 1. Compound 2 has been characterized in solution by (1)H, (11)B, and (13)C NMR spectroscopy and elemental analysis, and the structural types were unequivocally established by crystallographic studies. The title compound represents a novel class of vertex-fused clusters in which a Mo atom has been fused in a perpendicular fashion between two molybdaborane clusters. Electronic structure calculations employing density functional theory yield geometries in agreement with the structure determinations, and on grounds of density functional theory calculations, we have analyzed the bonding patterns in the structure.

Chlorinated hypoelectronic dimetallaborane clusters: synthesis, characterization, and electronic structures of (eta(5)-C5Me5W)2B5H(n)Cl(m) (n = 7, m = 2 and n = 8, m = 1).

Pyrolysis of (eta(5)-C(5)Me(5)WH(3))B(4)H(8), 1, in the presence of excess BHCl(2) x SMe(2) in toluene at 100 degrees C led to the isolation of (eta(5)-C(5)Me(5)W)(2)B(5)H(9), 2, and B-Cl inserted (eta(5)-C(5)Me(5)W)(2)B(5)H(8)Cl, 3, and (eta(5)-C(5)Me(5)W)(2)B(5)H(7)Cl(2), 4-7 (four isomers). All the chlorinated tungstaboranes were isolated as red and air and moisture sensitive solids. These new compounds have been characterized in solution by (1)H, (11)B, (13)C NMR, and the structural types were unequivocally established by crystallographic analysis of compounds 3, 4, and 7. Density functional theory (DFT) calculations were carried out on the model molecules of 3-7 to elucidate the actual electronic structures of these chlorinated species. On grounds of DFT calculations we demonstrated the role of transition metals, bridging hydrogens, and the effect of electrophilic substitution of hydrogens at B-H vertices of metallaborane structures.

Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.

The syntheses of a number of novel oxazolidinone analogues possessing an urea functionality are reported. While the urea derivatives possessing aliphatic and aromatic groups were prepared by the more conventional isocyanate method, the derivatives possessing heterocyclic rings were synthesized by a relatively uncommon but otherwise efficient carbamate chemistry. Though the SAR resulted in novel compounds possessing in vitro activity equivalent to Linezolid, the compounds possess a range of substituents that are amenable for altering physicochemical properties of the resultant drug. The antibacterial activity was found to be not sensitive to the functional groups attached to the urea site regardless of the size and electronic characteristics. Based on in vivo results, one molecule has been identified as a candidate and additional work such as salt selection, scale-up, etc., are currently underway to take the molecule further through development.