Author
Asha Kulkarni-Almeida
Bio: Asha Kulkarni-Almeida is an academic researcher. The author has contributed to research in topics: Chemical synthesis & Tumor necrosis factor alpha. The author has an hindex of 3, co-authored 3 publications receiving 106 citations.
Papers
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TL;DR: Three different series of pyrazolo[3,4-b]pyridines and their structural analogues are synthesized using novel synthetic strategy involving one-pot condensation of 5, 6-dihydro-4H-pyran-3-carbaldehyde/2-formyl-3, 4,6-tri-O-methyl-D-glucal/chromone-3
80 citations
TL;DR: Dacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists with varying length of acyl functionality and substitution on aromatic hydroxyls are reported.
30 citations
TL;DR: Two compounds isolated from H. ovalifolium scaffolds may be of interest to develop leads for treating rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease and other inflammatory disorders, but more detailed investigations need to be carried out to explain the efficacy of these compounds as drugs.
14 citations
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TL;DR: This Review summarizes islet GPCR expression, signalling and function, and highlights their potential as targets for the treatment of type 2 diabetes.
Abstract: Islet dysfunction - characterized by a combination of defective insulin secretion, inappropriately high glucagon secretion and reduced beta-cell mass - has a central role in the pathophysiology of type 2 diabetes. Several G protein-coupled receptors (GPCRs) expressed in islet beta-cells are known to be involved in the regulation of islet function, and therefore are potential therapeutic targets. This is evident from the recent success of glucagon-like peptide 1 (GLP1) mimetics and dipeptidyl peptidase 4 (DPP4) inhibitors, which promote activation of the GLP1 receptor to stimulate insulin secretion and inhibit glucagon secretion, and also have the potential to increase beta-cell mass. Other islet beta-cell GPCRs that are involved in the regulation of islet function include the glucose-dependent insulinotropic peptide (GIP) receptor, lipid GPCRs, pleiotropic peptide GPCRs and islet biogenic amine GPCRs. This Review summarizes islet GPCR expression, signalling and function, and highlights their potential as targets for the treatment of type 2 diabetes.
369 citations
TL;DR: 3s was obtained as lead compound with promising anticancer, anti-inflammatory and antioxidant activities and was confirmed to be nontoxic by in vitro cytotoxicity study.
258 citations
TL;DR: These analyses would assist medicinal chemists to design novel and potent IL-6 production and signaling inhibitors, through knowledge- and/or computer-based approaches, for the treatment of complex multifactorial diseases.
183 citations
TL;DR: QSAR study revealed that the presence of electron-withdrawing groups in B-ring and electron-donating groups in A-ring of chalcones was important for inhibition of LPS-induced IL-6 expression, and showed a series of anti-inflammatory chalcone derivatives with potential therapeutic effects in inflammatory diseases.
Abstract: Major anti-inflammatory agents, steroids and cyclooxygenase, were proved to have serious side effects. Here, a series of chalcone derivatives were synthesized and screened for anti-inflammatory activities. QSAR study revealed that the presence of electron-withdrawing groups in B-ring and electron-donating groups in A-ring of chalcones was important for inhibition of LPS-induced IL-6 expression. Further, compounds 22, 23, 26, 40, and 47 inhibited TNF-α and IL-6 release in a dose-dependent manner and decreased LPS-induced TNF-α, IL-1β, IL-6, IL-12, and COX-2 mRNA production. Mechanistically, compounds 23 and 26 interfered with JNK/NF-κB signaling and dose-dependently prevented ERK and p38 activation. In addition, 23 and 26 exhibited a significant protection against LPS-induced death and were able to block high glucose-activated cytokine profiles in macrophages. Together, these data show a series of anti-inflammatory chalcones with potential therapeutic effects in inflammatory diseases.
179 citations
TL;DR: The identification, structure, and pharmacology of these receptors are summarized and an essential overview of the current understanding of their physiological roles is presented.
164 citations