A series of 2-Substituted (1,3,4) thiadiazolo quinazolines were synthesized by the cyclocondensation of 3-amino-2-mercapto quinazolin-4(3H)-ones with various one-carbon donors and screened for their CNS activities (analgesic, anti-inflammatory, sedative-hypnotic and anticonvulsant). Compound III showed good CNS depressant activity, and it is comparable with the reference standard diazepam. While all the test compounds offered significant protection against strychnine-induced and hypoxic induced convulsion, compound III exhibited equivalent activity with the standard diazepam at the dose tested, and it was found to be significant when compared to control.
Purpose of the paper: Quinazolinone derivatives have been found to possess a wide range of biological activity, a series of 2{[2-(4-chlorophenyl)-4-oxoquinazolin-3(4H)-yl]amino}-N-(substitutedphenyl) acetamides have been taken to study the molecular properties and bio-activity score that shall aid in designing newer compounds.Design/methodology/approach: Molinspiration software was used for the calculation of Mi Log P values and all other biological data of the compounds. Findings:It was found that the values were in the range of 5 that means these compounds have good permeability across cell membrane. TPSA in the range of 76.02 to 121.85 (well below 160) and molecular mass<500. Number of violations is 0 and rotb < 7 .Number of hydrogen bond donors < 5 (The sum of OHs and NHs) and hydrogenbond acceptor <7 (The sum of Os and Ns). These observation showed that the compounds can easily bind to receptor and weretaken further for the calculation of bioactivity score. Research limitations/implications:The result of bioactivity score of GPCR ligand, ion channel modulator,nuclear receptor ligand, inhibitor activities towards enzymes, protease and kinase showed that the compounds exhibit moderate score towards all the receptors. Hence, these compounds shall be taken for further studies to evaluate their biological profile. Practical implications:A series of similar analogs shall be considered for evaluating the bioactivity score and compared for designing newer compounds.Social Implications: Designing of newer derivatives based on the bioactivity score of these reported compounds shall have profound biological activity.What is original/value of paper: The article deals with evaluation of bioactivity score of a series of quinazolinone derivatives.
Silver nanoparticles (AgNPs) have gained much attention in the treatment of dental caries due to their excellent antimicrobial activities. In this study, we have biosynthesised chitooligosaccharide coated silver nanoparticles (COS-AgNPs) using a rapid microwave-assisted method. The physical and chemical characterisations of biosynthesised COS-AgNPs were investigated using UV–visible spectroscopy (UV–vis), dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), X-Ray diffraction (XRD), field emission scanning electron microscopy (FE-SEM) and transmission electron microscopy (TEM) equipped with selected area electron diffraction (SAED). Further, the developed COS-AgNPs were assessed for antimicrobial activity on Streptococcus mutans. From the DLS analysis, the average particle size of the COS-AgNPs was found to be ∼32 nm. The morphologies of the COS-AgNPs were monodisperse and spherical in shape. XRD peaks are coherent with the standard peaks of AgNPs. Antimicrobial activity of COS-AgNPs showed a significant zone of inhibition due to the synergistic effect of COS-AgNPs. Furthermore, the antibacterial potential of developed COS-AgNPs-Ca(OH)2 paste was checked against Streptococcus mutans, Staphylococcus aureus, and Enterococcus faecalis. COS-AgNPs based composite paste showed better inhibition zone against the tested microbes. Hence, COS-AgNPs and COS-AgNPs-Ca(OH)2 based paste materials will be promising biomaterials for pulp therapy in paediatric dentistry.
A healthy-women during the period of conception has higher chances of a successful delivery and a healthy child 1 .At the time of maternity, the mother's oral health has a direct relationship to the birth outcome and simultaneously, the infant's oral health. Gingival and periodontal diseases are the most commonly observed diseases found in mothers who neglect their dental hygiene. These conditions, if left untreated in the mother have significant implications on the infant which comprises of preterm birth, preeclampsia and delivery of low-birth weight babies 2. Oral microbiota which comprises of Streptococcus mutans as the most cariogenic microorganism has a unique property of vertical transmission from the mother to the foetus. Consequently, there are higher chances of infants being prone to early development of caries in mothers with higher cariogenic flora 2 .There are large proportions of low-birth weight babies resulting from inadequate nutrition during pregnancy. The demand for nutrition increases during the course of pregnancy and insufficient nutrition can have both short-and long-term effects on the developing foetus. It is therefore imperative for a mother to consume adequate nutrients in adequate proportions. In order to avoid complications, the mother should be referred to a nutritionist by the gynaecologist to counsel them regarding the importance of maintaining a balanced diet. Further complications in infants can be attributed to preconception underweight or overweight and micro nutrient deficiencies in mothers 3 .The nutritional deficiencies in a mother can have significant implications on the developing dentition and the associated periodontium of a child. There is a lack of awareness in pregnant women regarding the importance of prenatal counseling and nutrition during the preconception period. Health care professionals are in a position to take initiative and impart knowledge about preconception-pregnancy related nutrition. Discussions regarding healthy eating guidelines, dietary supplement intake and maintenance of healthy weight should be included in the preconception counseling. Educating pregnant mothers about the different aspects of prenatal and postnatal care should be the aim of oral health promotion 4. Postnatal care includes early referral of the child to pedodontists to prevent diseases and to treat the pre-existing ones if present 2. Therefore, there is a need for an interdisciplinary collaboration among gynaecologists, pediatricians, nutritionists and pedodontists during preconception, conception and postconception 4 .
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