CERIC (IV) AMMONIUM NITRATE CATAYSED HUNTZSCH SYNTHESIS ,CHARACTERIZATION AND ANTIBACTERIAL ACTIVITY OF 1-4 DIHYDROPYRIDINE

1,4-Dihydropyridine (1,4-DHP) is among the most beneficial scaffolds that have revolutionized pharmaceutical research with unprecedented biological properties. 1,4-dihydropyridines are generally synthesized by Huntzsch reaction which involve the condensation of aldehyde, betaketoester, and ammonia or ammonium acetate. A number of improved methods have been reported in the literature for this condensation which involves the use of microwave, ionic liquids, TMSI etc. This work involves the synthesis of Diethyl4-(phenyl)’2,6-dimethyl-1,4-Dihydropyridine-3,5-dicarboxylate by the condensation of ethyl acetoacetate, benzaldehyde and ammonium acetate in presence of an effective catalyst Ceric(IV) Ammonium Nitrate in methanol, characterization of the sample by TLC, column chromatography and NMR. The work involve also the antibacterial activity of 1, 4-dihydropyridine. Huntzsch 1, 4- dihydropyridines and their derivatives have gained great importance in the field of medicinal chemistry since they display a fascinating array of pharmacological properties. 1, 4-dihydropyridines are well known as calcium channel blockers and important classes of drugs for the treatment of several cardiovascula

AMINOARENETHIOLATE-COPPER(I)-CATALYZED AMINATION OF ARYL BROMIDES

A copper-catalyzed electrophilic amination of aryl((2-hydroxymethyl)phenyl)dimethylsilanes with Oacylated hydroxylamines has been createdto manage the cost of the relating anilines in great yields. The synergist response continues easily under gentle conditions and endures a wide scope of utilitarian gatherings

RAPID AMINATION OF METHOXY PYRIDINE WITH ALIPHATIC AMINES

A n-BuLi triggered practical amination protocol of methoxy pyridine derivatives with aliphatic amines was developed. The reaction could finish in 30 min for primary amines and 10 min for secondary amines. The amination is further highlighted by its excellent reactivity and substrate scope.KEYWORDS: amination, methoxy pyridines, n-BuLi, transition-metal-fre

Susceptibility of south Indian strains of Mycobacterium tuberculosis to tuberactinomycin

A total of 114 strains of Mycobacterium tuberculosis isolated from sputum samples of 114 patients of pulmonary tuberculosis in south India, were coded and tested for their in vitro susceptibility to tuberactinomycin (Tum) incorporated in Lowenstein-Jensen (LJ) medium. Of these strains, 95 (83.3%) and 15 (13.2%) were susceptible to Tum at 25 and 50 mg/l respectively. Only 4 (3.5%) strains were inhibited at 100 mg/l or more. Of the 37 drug sensitive strains, 2 (5.4%) were not susceptible to Tum at 25 mg/l compared to 17 (22.1%) of 77 strains-resistant to one or more of antituberculosis drugs (P <0.02). The drug susceptibility pattern of the strains revealed that there was no significant association of resistance between Tum and streptomycin or rifampicin or ethambutol or ethionamide or isoniazid. However, 15 (53.6%) of 28 kanamycin (K) resistant strains were not susceptible to Tum at 25 mg/l. This cross resistance between Tum and K was further studied in 24 and 15 K sensitive and resistant strains respectively, by correlating their proportion resistance at 16 mg/l and it was found to have a significant positive correlation (r = 0.55; X0.01)

High Prevalence of Associated Birth Defects in Congenital Hypothyroidism

Aim. To identify dysmorphic features and cardiac, skeletal, and urogenital anomalies in patients with congenital hypothyroidism. Patients and Methods. Seventeen children with congenital primary hypothyroidism were recruited. Cause for congenital hypothyroidism was established using ultrasound of thyroid and 99mTc radionuclide thyroid scintigraphy. Malformations were identified by clinical examination, echocardiography, X-ray of lumbar spine, and ultrasonography of abdomen. Results. Ten (59%) patients (6 males and 4 females) had congenital malformations. Two had more than one congenital malformation (both spina bifida and ostium secundum atrial septal defect). Five (29%) had cardiac malformations, of whom three had only osteum secundum atrial septal defect (ASD), one had only patent ductus arteriosus (PDA), and one patient had both ASD and PDA. Seven patients (41%) had neural tube defects in the form of spina bifida occulta. Conclusion. Our study indicates the need for routine echocardiography in all patients with congenital hypothyroidism

Performance of blackgram genotypes under moisture deficit stress -Variability in physiological and yield contributing attributes

Abstract Water deficit stress is the most important abiotic stresses which affects the physiological parameters and crop yield. Blackgram (Vigna mungo L. Hepper) is one of the highly prized pluses in India and second most important pulse crop. A field experiment was conducted with seventeen blackgram genotypes during 2014 to assess the impact of water deficit stress on physiological parameters such as Anet, gs, Tr, WUE, SPAD chlorophyll meter reading (SCMR) and yield parameters (i.e.) pod number, seed number, pod weight and seed yield. Imposing water deficit stress at flowering stage, the reduction of physiological and yield parameters were observed. The results indicated that a wide diversity among the genotypes in their physiological and yield related parameters under both moisture levels. The genotype IC398971 was found to be physiologically efficient even with water deficit stress and also recorded moderate seed yield. While the genotype PU-19 with moderate physiological values registered highest seed yield under both well watered and water deficit stress conditions. Among the selected germplasm these two genotypes are having tolerant to water deficit stress with better stability of physiological and yield parameters

Revisiting the susceptibility testing of Mycobacterium tuberculosis to ethionamide in solid culture medium.

BACKGROUND & OBJECTIVES Increase in the isolation of drug resistant phenotypes of Mycobacterium tuberculosis necessitates accuracy in the testing methodology. Critical concentration defining resistance for ethionamide (ETO), needs re-evaluation in accordance with the current scenario. Thus, re-evaluation of conventional minimum inhibitory concentration (MIC) and proportion sensitivity testing (PST) methods for ETO was done to identify the ideal breakpoint concentration defining resistance. METHODS Isolates of M. tuberculosis (n=235) from new and treated patients were subjected to conventional MIC and PST methods for ETO following standard operating procedures. RESULTS With breakpoint concentration set at 114 and 156 µg/ml, an increase in specificity was observed whereas sensitivity was high with 80 µg/ml as breakpoint concentration. Errors due to false resistant and susceptible isolates were least at 80 µg/ml concentration. INTERPRETATION & CONCLUSIONS Performance parameters at 80 µg/ml breakpoint concentration indicated significant association between PST and MIC methods

HIV-infected patients retreated for tuberculosis with intermittent Category II regimen--treatment outcome at 24-month follow-up.

BACKGROUND The management of tuberculosis re-treatment in HIV-infected individuals is complex. The clinical and radiological manifestations in this group and response to Category II treatment is not well described. METHODS We performed a prospective cohort study of HIV-infected patients retreated for TB due to failure, relapse or default after treatment, at Tuberculosis Research Centre, Chennai, between February 2001 to September 2005. The Category II regimen followed in the TB programme in India (RNTCP) was administered (2 months of Streptomycin (S), Ethambutol (E), INH (H), Rifampicin (R), Pyrazinamide (Z)/1 month of EHRZ/5 months of HRE all given thrice weekly). Antiretroviral treatment was not routinely available at that time. RESULTS Of the 42 patients enrolled, 35 (83%) were males. The mean age was 33.2 (SD-6.3) years. Cough was the commonest (67%) presenting symptom and opacities were the commonest (48%) radiographic occurrence. 31 patients were culture-positive at baseline, drug susceptibility results showed that 21 (68%) were fully susceptible to all first line drugs, four patients (13%) had MDR TB and four had resistance to INH alone. Among the 31 culture-positive patients, 15 patients (48.4%) completed treatment and were declared cured, of whom two subsequently relapsed. All four MDR patients died. Six patients who received ART, survived. CONCLUSION Only 50% of HIV-infected, ART-naive patients who were retreated for tuberculosis using an intermittent Category II regimen had a favourable response to treatment. Early detection of MDRTB and concurrent antiretroviral therapy could contribute to improved outcomes

Rift Valley fever virus infection induces activation of the NLRP3 inflammasome

AbstractInflammasome activation is gaining recognition as an important mechanism for protection during viral infection. Here, we investigate whether Rift Valley fever virus, a negative-strand RNA virus, can induce inflammasome responses and IL-1β processing in immune cells. We have determined that RVFV induces NLRP3 inflammasome activation in murine dendritic cells, and that this process is dependent upon ASC and caspase-1. Furthermore, absence of the cellular RNA helicase adaptor protein MAVS/IPS-1 significantly reduces extracellular IL-1β during infection. Finally, direct imaging using confocal microscopy shows that the MAVS protein co-localizes with NLRP3 in the cytoplasm of RVFV infected cells

Novel Molecular Targets of Azadirachta indica Associated with Inhibition of Tumor Growth in Prostate Cancer

Advanced prostate cancer has significant long-term morbidity, and there is a growing interest in alternative and complimentary forms of therapy that will improve the outcomes of patients. Azadirachta indica (common name: neem) contains multiple active compounds that have potent anti-inflammatory and anticancer properties. The present study investigates the novel targets of the anticancer activity of ethanol extract of neem leaves (EENL) in vitro and evaluates the in vivo efficacy in the prostate cancer models. Analysis of the components in the EENL by mass spectrometry suggests the presence of 2′,3′-dehydrosalannol, 6-desacetyl nimbinene, and nimolinone. Treatment of C4-2B and PC-3M-luc2 prostate cancer cells with EENL inhibited the cell proliferation. Genome-wide expression profiling, using oligonucleotide microarrays, revealed genes differentially expressed with EENL treatment in prostate cancer cells. Functional analysis unveiled that most of the up-regulated genes were associated with cell death, and drug metabolism, and the down-regulated genes were associated with cell cycle, DNA replication, recombination, and repair functions. Quantitative PCR confirmed significant up-regulation of 40 genes and immunoblotting revealed increase in the protein expression levels of HMOX1, AKR1C2, AKR1C3, and AKR1B10. EENL treatment inhibited the growth of C4-2B and PC-3M-luc2 prostate cancer xenografts in nude mice. The suppression of tumor growth is associated with the formation of hyalinized fibrous tumor tissue and the induction of cell death by apoptosis. These results suggest that EENL-containing natural bioactive compounds could have potent anticancer property and the regulation of multiple cellular pathways could exert pleiotrophic effects in prevention and treatment of prostate cancer