2-Methylxanthen-9-one

In the title compound, C14H10O2, the tricycle is not planar, being bent with a dihedral angle of 4.7 (1)° between the two benzene rings. In the crystal, π–π inter­actions between the six-membered rings of neighbouring mol­ecules [centroid–centroid distances = 3.580 (3) and 3.605 (3) Å] form stacks propagating along [101]

THE CURRENT STATUS AND PERSPECTIVES FOR THE EMERGING PANDEMIC: COVID-19

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of the extremely communicable viral infection coronavirus disease 19 (covid-19). Initially the virus was found at Wuhan, china which spread across the world exponentially and in a very short span. This outbreak has turned out to be a global health crisis and recently WHO regarded it as pandemic. The origin of the virus is predicted as either the natural selection in animal host prior to the transfer of the pathogen from animals to humans or the natural selection in humans and following transfer. Nevertheless, there is an extensive spread of virus by human to human transfer in the form of droplets. A few antiviral drugs are at the stage of clinical trials to eradicate the covid-19. In this review, a comprehensive approach is put forth to scrutinise the etiology, pathogenicity and transmission of SARS CoV-2. The review also deliberates broadly on the diagnosis and status of therapeutic treatment developed. It also focuses on the preventive and controlling measures from different sectors of the society. The review covers the details reported in 70 studies which were chosen after keyword searches carried out leading to over 884 resulting articles

Efficacy of 5-(2-aroyl)aryloxy methyl-2-phenyl-1,3,4-oxadiazoles as antibacterial and antifungal agents

Research and development of potent and effective antimicrobial agents represent one of the most important advances in therapeutics; the main aim of these efforts is not only control the serious infections, but also prevention and treatment of some infectious complications of other therapeutic modalities. A series of 5-(2-aroyl)aryloxy methyl-2-phenyl-1,3,4-oxadiazoles were screened for their antibacterial and antifungal activities. Anti-bacterial activity against B. cereus, S. aureus, B. subtilis, S. aureus (MRSA), E. aerogenes, M. luteus, K. pneumonia, P. aeruginosa, S. typhimurium, E. coli, paratyphi-B, P. vulgaris bacterial strains and anti-fungal activity against C. albicans, A.niger, F.solani, A.flavus, B.cinerea, C.krusei, M. pachydermatis, C.parapsilosis, F.moniliforme, C.gloeosporioides fungal strains were carried out. The bioassays indicated that most of the synthesized compounds showed potential antibacterial and anti-fungal activity

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Anti-inflammatory and antioxidant activity of salicylic acid conjugated dihydropyrazoline analogues

Syntheses of substituted salicylic acid appended pyrazoline analogues (7a-j) via 1,3-dipolar cycloaddition were reported earlier. In the present investigation we have performed the anti-inflammatory activity by phospholipase A2 (PLA2) inhibition and in vitro antioxidant activity by 2,2-diphenyl-1-picrylhydrazyl, nitric oxide, hydroxyl radical scavenging assay and ferrous ion chelating assay wherein compounds 7d, 7h, 7i and 7j have shown maximum anti-inflammatory activity. Further, compounds 7d, 7f and 7h were proved to be excellent free radical scavengers

Competent synthesis of biaryl analogs via asymmetric Suzuki-Miyaura cross-coupling for the development of anti-inflammatory and analgesic agents

Based on the core structure of diflunisal drug, herein, we report a resembling series of biaryl analogs (3a-j) containing halogens, nitro, and methoxy substituents. They were designed and synthesized via a Suzuki-Miyaura cross-coupling reaction using Pd (OH)(2) as a catalyst at a temperature of 65 degrees C with an intent to obtain improved and safer anti-inflammatory and analgesic agents. Suzuki-Miyaura transformation is the most significant among the cross-coupling reactions since its practical advantages include the commercially available low toxic reagents, mild reaction conditions, and functional group compatibility. On the other hand, a few conditions can be used to cross-couple aryl boronic acids or esters with aryl halides, especially 2-benzyl halides. Because of this, a novel Suzuki-Miyaura protocol is investigated that facilitates the selective conversion of halo aromatics, with an emphasis on the reaction to convert substituted bromobenzene to conjugated biphenyls. Finally, the obtained biaryl analogs (3a-j) were tested for in vitro and in vivo anti-inflammatory and analgesic applications. The results showed that compound 3b performed better than the standard drug with IC50 values comparable to that of the standard drug for COX-1 and COX-2 inhibition. Finally, molecular docking tests for the effective compound were carried out

Inhibitory effect of banana (Musa sp. var. Nanjangud rasa bale) flower extract and its constituents Umbelliferone and Lupeol on α-glucosidase, aldose reductase and glycation at multiple stages

Postprandial hyperglycaemia is characterized as the earliest symptom of diabetes and its management attenuates several of the associated secondary complications. In this context, we investigated the role of ethanol extract of banana flower (EF) for its antihyperglycaemic effects. The EF showed a strong inhibition towards α-glucosidase and pancreatic amylase which play a vital role in clinical management of postprandial hyperglycaemia. The major active compounds present in EF were identified as Umbelliferone (C1) and Lupeol (C2) using various spectroscopic methods. C1 (IC50: 7.08±0.17μg/ml) and C2 (IC50: 7.18±0.14μg/ml) were found to inhibit α-glucosidase in a non-competitive mode of inhibition, with low Ki values. Further, in vitro glycation assays showed that EF and its compounds prevented each stage of protein glycation and formation of its intermediary compounds. EF, C1 and C2 also exhibited a potent inhibition on aldose reductase with IC50 values of 2.25±0.29, 1.32±0.22 & 1.53±0.29μg/ml respectively. Our results suggest that, the observed potential of EF in antihyperglycaemic activity via inhibition of α-glucosidase and in antidiabetogenic effect by inhibition of polyol pathway and protein glycation is more likely to be attributed to the presence of C1 and C2