Structure based rational drug design of selective phosphodiesterase-4 ligands as anti-inflammatory molecules

Phosphodiesterase-4 enzyme (PDE4) has been gaining increasing attention for the last two decades as a pharmacotherapeutic target, as it is involved in the etiology of a variety of pathologies that comprise a majority of inflammation problems concerning respiratory pathway in major aspect. Intense efforts have been directed towards the development of effective and selective PDE4b inhibitors, but not much success has been reported till yet. This is because of the structural similarity between the two isoforms of PDE4, PDE4b (therapeutic effect) and PDE4d (side effect of emesis). Analogues of 1,2-dihydroxy-xanthen-9H-one were designed as selective ligands for PDE4b using the structure based drug design. The selectivity was determined by docking of xanthone analogues in PDE4b and PDE4d active sites respectively using GLIDE docking programme from Schrodinger Inc. ADME properties of the designed ligands were also predicted using QikProp from Schrodinger Inc. Interpretation of protein-ligand interactions and binding modes of xanthone analogues showed that these ligands are more selective for PDE4b than for PDE4d.info:eu-repo/semantics/publishedVersio

Entrapment of Suprascapular Artery between Split Parts of Right Inferior Belly of Omohyoid Muscle - A Rare Case Report

Inferior belly of omohyoid is used as a landmark for endoscopic exploration of the brachial plexus. Variation of inferior belly of omohyoid muscle has immense clinical significance because of its relation to brachial plexus, external jugular vein, suprascapular nerve, vessels and phrenic nerve. The need to understand muscular variation is of greater importance because of the increased number of endoscopic surgeries and images for diagnosis. A number of variations of omohyoid muscle such as the absence of muscle, unusual sites of origin and insertion, and multiple bellies have been reported. Doubling or splitting of superior belly of the omohyoid has been reported several times. However, the splitting of the inferior belly of the omohyoid muscle is rarely reported. Herein we report a case of unusual splitting of inferior belly of omohyoid muscle. During the dissection for undergraduate students at AIIMS Bhubaneswar, unusual morphology of inferior belly of omohyoid muscle was observed in formalin embalmed 60-year-old male cadaver. The inferior belly of omohyoid was split. Another important finding observed was suprascapular artery entrapment between the split upper and lower parts of belly of inferior omohyoid with slight indentation mark on the artery suggestive of chronic compression. This muscle is used for various important clinical procedures and is an important landmark for radical neck dissection. So, the knowledge of possible anomalies of omohyoid is important

IMPORTANCE OF VIPASSANA (BUDDHIST MEDITATION) IN THE PANDEMIC OF COVID-19: A REVIEW

Today, we are living in the era of developed science and technology in which human being has no utopia and generally human being now days, thinks logically and will not accept anything unless the results are beneficial, tangible, vivid and personal. In ancient times, ritual and magical practices were humanity's crucial forms of health care. Vipassana (Buddhist meditation) is one of the India's prehistoric meditative practices with the help of which Siddharth Gautama became the Buddha 2,500 years ago. Meaning of Vipassana is “Insight”, (Mindfulness meditation) and it is a Pali word. Though, human being is now living in the era of developed science and technology but at the same time world is facing serious problems which threaten all mankind. After the WWII, the Coronavirus Covid-19 outbreak has become the most devastated disaster for human and its socio-economic development in the world. It seems that only Vipassana meditation has the capacity to eradicate total sufferings of human being. Anicca (Impermance), Dukkha (suffering) and Anatta (non-substantiality) are the basic teachings of the Buddha which is the foundation of Vipassana meditation. It is said that change is the only constant thing in this universe and Crises such as the Covid-19 pandemic has proved it. Vipassana can provide an approach to live life with this constant change. Demands for unconventional forms of medicine have increasing day by day and it is being proving that there are numerous health benefits of Vipassana meditation. This paper briefly reviews the Vipassana (Buddhist meditation) and its benefits for human beings during this Covid-19 pandemic

Development of pharmacophoric model of condensed pyridine and pyrimidine analogs as hydroxymethyl glutaryl coenzyme A reductase inhibitors

32-36Quantitative structure-activity relationship (QSAR) has been established on a series of thirty-eight compounds of four different sets of condensed pyridine and pyrimidine analogs, for their hydroxymethyl glutaryl coenzyme (HMG-CoA) reductase inhibitor activity, in order to understand the essential structural requirement for binding with receptor, in terms of common biophoric and secondary sites employing APEX-3D software. Among several 3D pharmacophoric models with different sizes and arrangements, one model was selected based on r² = 0.8, chance<0.001, match equivalent to 0.38 and all the 38 compounds were considered. The results suggest that hydrophobicity, hydrogen acceptor and optimum steric refractivity play a dominant role in the inhibition of HMG-CoA reductase. The information obtained from the present study can be used to design and predict more potent molecules as HMG-CoA reductase inhibitors, prior to their synthesis

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Not AvailableThe present investigation was undertaken to delineate agricultural prime, moderate prime and marginallands in Nagpur district Maharashtra based on land use, slope and soil characteristics. The extent ofprime lands in the district is about 470418.30 ha (47.5% of TGA) to which Kuhi, Mauda, Saoner andBhiwapur tehsils contribute, 61378.70 ha, 57051.69 ha, 41038.90 ha, and 41020.58 ha, respectively. Theextent of moderate prime lands is about 85096.00 ha (8.60% of TGA), which may be utilized throughadoption of appropriate agro-management. Out of 74699.73 ha (7.55 % of TGA) marginal lands, Katolcontributes large area (23205.20 ha) followed by Kalmeshwar (8337.75 ha), Hingna (8240.43 ha) andNarkhed (8151.97 ha) tehsils. The study also indicate that prime agricultural lands are mostly locatedaround the 4th and 5th stream orders and hence, stream order may be used as an indicator for identificationand delineation of prime agriculture lands. The delineation of prime lands will be helpful in land useplanning, protection of prime lands and sustainable utilization of lands. The quantification will help inprioritizing the area and judging the magnitude of efforts required to overcome the constraints.Not Availabl