6% and 29.6%, respectively. CONCLUSION Structure-based virtual screening using a molecular docking approach is a useful method for the identification of new transsialidase inhibitors. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. OBJECTIVE The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. METHODS Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. RESULTS Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). CONCLUSION These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND We found an excellent review in the literature of the Biginelli reaction that addresses the methodologies for obtaining enantiopure dihydropyrimidinones (DHPMs). In 1992, optically pure DHPMs were obtained by fractional crystallization of the diastereomeric ammonium salt derivative with (S)-(-) and (R)-(+)--methylbenzylamine and by other chiral resolution techniques, such chiral high-performance liquid chromatography (HPLC). Asymmetric syntheses of these compounds are also found in the literature. The main strategy uses acid catalysts such as organophosphates, organometallic complexes, amines and diamines, nanocomposites, and chiral ionic liquids, e.g., L-prolinium sulfate (Pro2SO4). OBJECTIVE To study the Biginelli reaction with a chiral aldehyde. METHODS A mixture of ethyl acetoacetate (0.26 g, 3 mmol), urea (0.18 g, 3 mmol) and ethyl lactate (EL) (1 mL) is left under heating at 70 °C and stirring for 1 h. Next, (-)-(1R)-myrtenal (0.45 g, 3 mmol) is added, and the medium is heated for 5 h more unelli reaction. In addition, the process has the advantage of using EL as a green solvent. The product was characterized by 1H, 13C, and 2D NMR and IR spectroscopy, MS, HRMS, and X-ray crystallography. https://www.selleckchem.com/products/guanidine-thiocyanate.html Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.The natural beauty and purity of our planet has been contaminated deeply due to human selfish activities such as pollution, improper waste management, and various industrial and commercial discharges of untreated toxic by-products into the lap of nature. The collective impact of this hazardous suspension into the natural habitat is very deadly. Challenges due to human activity on the environment have become ubiquitous. The chemical industry has a major role in human evolution and, predictably, opened gates of increased risk of pollution if the production is not done sustainably. In these circumstances, the notion of Green Chemistry has been identified as the efficient medium of synthesis of chemicals and procedures to eradicate the toxic production of harmful substances. Principles of Green Chemistry guide the scientist in their hunt towards chemical synthesis which requires the use of solvents. These solvents contaminate our air, water, land and surrounding due to its toxic properties. Even though sufficient waste product and will remain human and nature friendly. During designing compounds for a particular reaction it is difficult to give assurance regarding the toxicity and biodegradability of the method. Chemists are still far away from predicting the various chemical and biological effects of the compounds on the **** of the envelope. To achieve that point is formidable task but it will definitely act as inspiration for the coming generation chemists. The green solvents are undoubtedly a far better approach to eliminate the negative impacts and aftermath of any chemical synthesis on the environment. Our study in this review covers an overview of green solvents, their role in safer chemical synthesis with reference to some of the important green solvents and their detail summarization. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.Triple Negative Breast Cancer (TNBC) is the most aggressive and prevailing breast cancer subtype. The chemotherapeutics used in the treatment of TNBC suffer with chemoresistance, dose limiting toxicities and off-target side effects. As a result, conventional chemotherapeutics are unable to prevent tumor growth, metastasis and result in failure of therapy. Various new targets such as BCSCs surface markers (CD44, CD133, ALDH1), signaling pathways (IL-6/JAK/STAT3, notch), pro and anti-apoptotic proteins (Bcl-2, Bcl-xL, DR4, DR5), hypoxic factors (HIF-1α, HIF2α) and drug efflux transporters (ABCC1, ABCG2 and ABCB1) have been exploited to treat TNBC. Further, to improve the efficacy and safety of conventional chemotherapeutics, researchers have tried to deliver anticancer agents specifically to the TNBCs using nanocarrier based drug delivery. In this review, an effort has been made to highlight the various factors responsible for the chemoresistance in TNBC, novel molecular targets of TNBC and nano-delivery systems employed to achieve site specific drug delivery to improve efficacy and reduce off-target side effects.
6% and 29.6%, respectively. CONCLUSION Structure-based virtual screening using a molecular docking approach is a useful method for the identification of new transsialidase inhibitors. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. OBJECTIVE The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. METHODS Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. RESULTS Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). CONCLUSION These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND We found an excellent review in the literature of the Biginelli reaction that addresses the methodologies for obtaining enantiopure dihydropyrimidinones (DHPMs). In 1992, optically pure DHPMs were obtained by fractional crystallization of the diastereomeric ammonium salt derivative with (S)-(-) and (R)-(+)--methylbenzylamine and by other chiral resolution techniques, such chiral high-performance liquid chromatography (HPLC). Asymmetric syntheses of these compounds are also found in the literature. The main strategy uses acid catalysts such as organophosphates, organometallic complexes, amines and diamines, nanocomposites, and chiral ionic liquids, e.g., L-prolinium sulfate (Pro2SO4). OBJECTIVE To study the Biginelli reaction with a chiral aldehyde. METHODS A mixture of ethyl acetoacetate (0.26 g, 3 mmol), urea (0.18 g, 3 mmol) and ethyl lactate (EL) (1 mL) is left under heating at 70 °C and stirring for 1 h. Next, (-)-(1R)-myrtenal (0.45 g, 3 mmol) is added, and the medium is heated for 5 h more unelli reaction. In addition, the process has the advantage of using EL as a green solvent. The product was characterized by 1H, 13C, and 2D NMR and IR spectroscopy, MS, HRMS, and X-ray crystallography. https://www.selleckchem.com/products/guanidine-thiocyanate.html Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.The natural beauty and purity of our planet has been contaminated deeply due to human selfish activities such as pollution, improper waste management, and various industrial and commercial discharges of untreated toxic by-products into the lap of nature. The collective impact of this hazardous suspension into the natural habitat is very deadly. Challenges due to human activity on the environment have become ubiquitous. The chemical industry has a major role in human evolution and, predictably, opened gates of increased risk of pollution if the production is not done sustainably. In these circumstances, the notion of Green Chemistry has been identified as the efficient medium of synthesis of chemicals and procedures to eradicate the toxic production of harmful substances. Principles of Green Chemistry guide the scientist in their hunt towards chemical synthesis which requires the use of solvents. These solvents contaminate our air, water, land and surrounding due to its toxic properties. Even though sufficient waste product and will remain human and nature friendly. During designing compounds for a particular reaction it is difficult to give assurance regarding the toxicity and biodegradability of the method. Chemists are still far away from predicting the various chemical and biological effects of the compounds on the back of the envelope. To achieve that point is formidable task but it will definitely act as inspiration for the coming generation chemists. The green solvents are undoubtedly a far better approach to eliminate the negative impacts and aftermath of any chemical synthesis on the environment. Our study in this review covers an overview of green solvents, their role in safer chemical synthesis with reference to some of the important green solvents and their detail summarization. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.Triple Negative Breast Cancer (TNBC) is the most aggressive and prevailing breast cancer subtype. The chemotherapeutics used in the treatment of TNBC suffer with chemoresistance, dose limiting toxicities and off-target side effects. As a result, conventional chemotherapeutics are unable to prevent tumor growth, metastasis and result in failure of therapy. Various new targets such as BCSCs surface markers (CD44, CD133, ALDH1), signaling pathways (IL-6/JAK/STAT3, notch), pro and anti-apoptotic proteins (Bcl-2, Bcl-xL, DR4, DR5), hypoxic factors (HIF-1α, HIF2α) and drug efflux transporters (ABCC1, ABCG2 and ABCB1) have been exploited to treat TNBC. Further, to improve the efficacy and safety of conventional chemotherapeutics, researchers have tried to deliver anticancer agents specifically to the TNBCs using nanocarrier based drug delivery. In this review, an effort has been made to highlight the various factors responsible for the chemoresistance in TNBC, novel molecular targets of TNBC and nano-delivery systems employed to achieve site specific drug delivery to improve efficacy and reduce off-target side effects.
0 Commenti
0 condivisioni
18 Views
0 Anteprima
