Synthesis and Pharmacological Profile of Benzimidazoles

Benzimidazoles are a class of heterocyclic, aromatic compounds which share a fundamental structural characteristic of six-membered benzene fused to five-membered imidazole moiety. Molecules having benzimidazole motifs showed promising application in biological and clinical studies. Nowadays it is a moiety of choice which possesses many pharmacological properties extensively explored with a potent inhibitor of various enzymes involved in a wide range of therapeutic uses which are antidiabetic, anticancer, antimicrobial, antiparasitic, analgesics, antiviral, and antihistamine, as well as used in cardiovascular disease, neurology, endocrinology, ophthalmology, and more. The increased interest for benzimidazole compounds has been due to their excellent properties, like increased stability, bioavailability, and significant biological activity. This book chapter mainly discussed recent synthetic methods developed for the benzimidazole derivatives and their pharmacological properties exemplified on several derivatives

Efficient Synthesis of O-Succinimidyl-(tert-Butoxycarbonylamino)methyl Carbamates Derived from α-Amino Acids Accelerated by Ultrasound: Application to the Synthesis of Ureidodipeptides

The synthesis of O-succinimidyl-(tert-butoxycarbonylamino)methyl carbamates employing isocyanates made through the Curtius rearrangement of Boc-amino acid azides in the presence of N-hydroxysuccinimide under the influence of ultrasound is described

Studies on Xyloglucanase during the Germination of Seeds of Tamarindus Indica

Germinating seeds of Tamarindus indicacontain endo-β-1, 4-xyloglucanases which degrade tamarind xyloglucan, but notcarboxymethylcellulose (CMC). The xyloglucanases are isolated from thegerminating tamarind seeds using 50 mM acetate buffer, pH 5.5 containing 0.5 MNaCl. The Km value is 0.667 g/liter and the enzyme is optimally active at pH5.5 and stable between pH 4 - 6.5. The optimum temperature is 45C and is quitestable upto 50C. The activity declined by 50% at 60C and is completelyinactivated at 70C. Highest xyloglucanase activity and specific activity areobserved on the 23rd day of germination. The polyacrylamide gel electrophoresis(PAGE) indicated the presence of five isozymes of xyloglucanases which arevisualized by activity staining separately with congo red and grams iodine.Isozyme 2 is the major xyloglucanase present throughout the germination period

Analysis of Laughter in Cohesive Groups

Group cohesion describes the tendency of the group members’ shared commitment to group tasks and the interpersonal attraction among them. This paper presents a preliminary analysis of occurrence of laughter with respect to group cohesion using a corpus of multi-party interactions. Results indicate that the occurrence of laughter is higher in cohesive segments and a strong positive correlation exists between the perceived level of cohesion and laughter

The early definitive internal fixation of Complex Pelvic Fracture and its outcome: our experience in level 1 trauma care centre.

Background: Complex pelvic fractures have high mortality and morbidity hence required urgent resuscitation, haemodynamic stabilization and fracture fixation. Keeping in mind the various schools of thought regarding definitive management, there is need to study the outcomes of complex pelvic fractures after internal fixation surgery.Methods: Twenty patients with complex pelvic fractures treated with internal fixation surgery in between 1st June 2018-31st December 2019 with at least 12 months follow-up were included. Clinical and functional outcome of these patients was studied and evaluated using Majeed and Hannover scoring systems.Results: Of 20 patients, 19 had closed while 1 had open pelvic fracture while 11 had tile type B and 9 had tile type C fracture. After 12 months of follow up, 72% patients of tile B fractures and 55.6% in tile C had excellent Majeed score with rest having good score. Hannover score was very good in 36.4% tile B cases and 22.2% tile C cases and good in 63.6% tile B cases and 77.8% tile C cases. Type of fracture (type B or type C) had a statistically significant co-relation with chronic pain (p=0.016). It was also found that urogenital injury and sexual dysfunction (p=0.007) had a significant co-relation.Conclusions: Early definitive internal fixation in patients with complex pelvic fracture had very good clinical and functional outcome. Most common associated injuries in complex pelvic fractures are urogenital injuries due to close proximity. In the outcomes chronic pain and sexual dysfunction are major issues. The sexual dysfunction patients usually associated fracture of pubic rami or pubic diastasis

Application of novel, efficient and agro-waste sourced catalyst for Knoevenagel condensation reaction

258-270A greener, economic and eco-friendly method for Knoevenagel condensation of aromatic aldehyde, salicylaldehyde with active methylene compounds like malononitrile and Meldrum’s acid to synthesize benzylidinemalononitrile and 3-carboxy coumarin derivatives respectively is demonstrated. The reaction has been carried out in the absence of external base using agro-waste sourced green catalyst WENBA {Water Extract of Nilgiri Bark Ash (Eucalyptus)} as an efficient natural catalytic medium. WENBA is a novel, ecologically safe and inexpensive green catalyst obtained from the agro-waste feedstock. The synthesized compounds benzylidinemalononitrile and 3-carboxy coumarin (2-oxo-2H-1-benzopyran) backbone have multiple applications in medicinal chemistry for the synthesis of bioactive molecules. Thus, a wide number of methodologies have been developed for the synthesis of this class of organic molecules. However, some of the methods reported are associated with hazardous materials and are toxic to the environment. They have longer reaction times, poor yields, and with lower purity of final isolated compound. In spite of a large number of methodologies available for this bioactive molecule synthesis, there is still demand for the development of newer reagents, which give environmentally friendly protocols, mild reaction conditions, inexpensive catalyst and final product isolation in pure form with good yields

Microwave accelerated efficient synthesis of N-fluorenylmethoxycarbonyl/t-butoxycarbonyl/benzyloxycarbonyl-5- oxazolidinones

The synthesis of N-protected 5-oxazolidinones using amino acids, paraformaldehyde and p-toluene sulfonic acid in a minimum amount of toluene accelerated by microwave irradiation for 3 min in high yield is described. © 2002 Elsevier Science Ltd. All rights reserved

Analysis of Laughter in Cohesive Groups

Group cohesion describes the tendency of the group members’ shared commitment to group tasks and the interpersonal attraction among them. This paper presents a preliminary analysis of occurrence of laughter with respect to group cohesion using a corpus of multi-party interactions. Results indicate that the occurrence of laughter is higher in cohesive segments and a strong positive correlation exists between the perceived level of cohesion and laughter

Interaction of large scale strucutres in high Re round jets

International audienceThe dynamical significance of vortical structures in the near field of round jets, viz. the vortex rings and the stream-wise vortices, has been known for several decades (Ho & Huerre, 1984). A fundamental understanding of their interactions , especially in turbulent jets at high Reynolds number (Re), is expected to provide an impetus to devising control strategies; for instance in improving combustion efficiency and reducing jet noise. One such possible interaction was recently observed in Davoust et al. (2012) that involved production of additional streamwise vorticity, as a result of an influence of the fluctuations of streamwise vorticity on those of azimuthal vorticity in high Re jets. This additional vorticity showed up in streamwise vorticity correlations in the form of radial organization as opposed to its azimuthal organization classically found. In further exploring this possibility, we have observed in our experiments, that strengthening the vortex rings relative to the streamwise vortices, renders them less susceptible to an influence from the streamwise vortices. This paper presents the results for a Re = 1.5 × 10 5 and low Mach number round jet in which the most energetic vortex rings are acoustically excited at different excitation amplitudes. A comparison of the relative strengths of the two structures with increasing excitation levels, corroborates the interaction proposed in Davoust et al. (2012)

Characterization of Esterases of Tamarindus Indica Seeds

Germinating seeds of Tamarindus indicasynthesizes various enzymes which are required for the degradation of seedreserves such as xyloglucans, fatty acid esters and proteins. Among these,esterases, belonging to a group of hydrolytic enzymes catalyze the hydrolysisof various types of esters. They play an important role in cell expansion aswell as detoxification of xenobiotics and many agrochemicals and insecticides.The esterases are extracted from the germinating tamarind seeds using 50 mMphosphate buffer, pH 7. The Km with α-naphthyl acetate as the substrate is19.23 μM and the enzymes are optimally active at pH 7.0 to 7.5 and are stablebetween pH 5.0 to 9.0. The optimum temperature of esterase activity of tamarindseed is between 37C - 50C and is stable up to 40C. The activity declined by30% at 60C and about 90% at 70C. Highest esterase activity and specificactivity are observed on the 21st day of germination. The polyacrylamide gelelectrophoresis (PAGE) indicated the presence of nine isozymes of esterases.Band numbers 1, 5 and 6 are the major esterolytic bands present throughout thegermination period while band numbers 2 & 3 are minor bands present onlyduring the latter period of the germination. Based on substrate and inhibitorspecificity in conjunction with electrophoresis, the esterases 1 to 8 have beenclassified as carboxylesterases sensitive to organophosphate inhibitor (OP) andPCMB (p-chloromercuribenzoate) while esterase 9 is classified as carboxylesterasesensitive to OP. These esterases are unaffected by carbamate inhibitor, eserinesulphate