Search Results - "PATEL, Jayendra Z"

Docking-Based 3D-QSAR Studies for 1,3,4-oxadiazol-2-one Derivatives as FAAH Inhibitors by Zięba, Agata, Laitinen, Tuomo, Patel, Jayendra Z., Poso, Antti, Kaczor, Agnieszka A.

“…This work aimed to construct 3D-QSAR CoMFA and CoMSIA models for a series of 31 FAAH inhibitors, containing the 1,3,4-oxadiazol-2-one moiety. The obtained…”
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Biochemical and pharmacological characterization of the human lymphocyte antigen B-associated transcript 5 (BAT5/ABHD16A) by Savinainen, Juha R, Patel, Jayendra Z, Parkkari, Teija, Navia-Paldanius, Dina, Marjamaa, Joona J T, Laitinen, Tuomo, Nevalainen, Tapio, Laitinen, Jarmo T

“…Human lymphocyte antigen B-associated transcript 5 (BAT5, also known as ABHD16A) is a poorly characterized 63 kDa protein belonging to the α/β-hydrolase domain…”
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Repurposing the Sphingosine-1-Phosphate Receptor Modulator Etrasimod as an Antibacterial Agent Against Gram-Positive Bacteria by Zore, Matej, Gilbert-Girard, Shella, San-Martin-Galindo, Paola, Reigada, Inés, Hanski, Leena, Savijoki, Kirsi, Fallarero, Adyary, Yli-Kauhaluoma, Jari, Patel, Jayendra Z.

“…New classes of antibiotics are urgently needed in the fight against multidrug-resistant bacteria. Drug repurposing has emerged as an alternative approach to…”
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Synthesis and Biological Evaluation of Fingolimod Derivatives as Antibacterial Agents by Zore, Matej, Gilbert-Girard, Shella, Reigada, Inés, Patel, Jayendra Z, Savijoki, Kirsi, Fallarero, Adyary, Yli-Kauhaluoma, Jari

“…We recently identified fingolimod as a potent antibiofilm compound by screening FDA-approved drugs. To study if the antibacterial activity of fingolimod could…”
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Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) by Korhonen, Jani, Kuusisto, Anne, van Bruchem, John, Patel, Jayendra Z., Laitinen, Tuomo, Navia-Paldanius, Dina, Laitinen, Jarmo T., Savinainen, Juha R., Parkkari, Teija, Nevalainen, Tapio J.

“…[Display omitted] The key hydrolytic enzymes of the endocannabinoid system, fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), are potential…”
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Food-Grade Bacteria Combat Pathogens by Blocking AHL-Mediated Quorum Sensing and Biofilm Formation by Savijoki, Kirsi, San-Martin-Galindo, Paola, Pitkänen, Katriina, Edelmann, Minnamari, Sillanpää, Annika, van der Velde, Cim, Miettinen, Ilkka, Patel, Jayendra Z, Yli-Kauhaluoma, Jari, Parikka, Mataleena, Fallarero, Adyary, Varmanen, Pekka

“…Disrupting bacterial quorum sensing (QS) signaling is a promising strategy to combat pathogenic biofilms without the development of antibiotic resistance…”
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Combined Effect of Naturally-Derived Biofilm Inhibitors and Differentiated HL-60 Cells in the Prevention of Staphylococcus aureus Biofilm Formation by Reigada, Inés, Guarch-Pérez, Clara, Patel, Jayendra Z, Riool, Martijn, Savijoki, Kirsi, Yli-Kauhaluoma, Jari, Zaat, Sebastian A J, Fallarero, Adyary

“…Nosocomial diseases represent a huge health and economic burden. A significant portion is associated with the use of medical devices, with 80% of these…”
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Strategies to Prevent Biofilm Infections on Biomaterials: Effect of Novel Naturally-Derived Biofilm Inhibitors on a Competitive Colonization Model of Titanium by Staphylococcus aureus and SaOS-2 Cells by Reigada, Inés, Pérez-Tanoira, Ramón, Patel, Jayendra Z, Savijoki, Kirsi, Yli-Kauhaluoma, Jari, Kinnari, Teemu J, Fallarero, Adyary

“…Biofilm-mediated infection is a major cause of bone prosthesis failure. The lack of molecules able to act in biofilms has driven research aimed at identifying…”
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Design and synthesis of etrasimod derivatives as potent antibacterial agents against Gram-positive bacteria by Zore, Matej, San-Martin-Galindo, Paola, Reigada, Inés, Hanski, Leena, Fallarero, Adyary, Yli-Kauhaluoma, Jari, Patel, Jayendra Z.

“…The emergence of multidrug-resistant bacteria along with a declining pipeline of clinically useful antibiotics has led to the urgent need for the development…”
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Chloroquine fumardiamides as novel quorum sensing inhibitors by Beus, Maja, Savijoki, Kirsi, Patel, Jayendra Z., Yli-Kauhaluoma, Jari, Fallarero, Adyary, Zorc, Branka

“…[Display omitted] Quorum sensing inhibitors (QSIs) that specifically interfere with bacterial cell-to-cell communication are considered as an alternative…”
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Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid α/β‑Hydrolase Domain 6 (ABHD6) by Mardon, Karine, Patel, Jayendra Z., Savinainen, Juha R., Stimson, Damion H. R., Oyagawa, Caitlin R. M., Grimsey, Natasha L., Migotto, Mary-anne, Njiru, Grace F. M., Hamilton, Brett R., Cowin, Gary, Yli-Kauhaluoma, Jari, Vanduffel, Wim, Blakey, Idriss, Bhalla, Rajiv, Cawthorne, Christopher, Celen, Sofie, Bormans, Guy, Thurecht, Kristofer J, Ahamed, Muneer

“…Multimodal imaging provides rich biological information, which can be exploited to study drug activity, disease associated phenotypes, and pharmacological…”
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Chiral 1,3,4-Oxadiazol-2-ones as Highly Selective FAAH Inhibitors by Patel, Jayendra Z, Parkkari, Teija, Laitinen, Tuomo, Kaczor, Agnieszka A, Saario, Susanna M, Savinainen, Juha R, Navia-Paldanius, Dina, Cipriano, Mariateresa, Leppänen, Jukka, Koshevoy, Igor O, Poso, Antti, Fowler, Christopher J, Laitinen, Jarmo T, Nevalainen, Tapio

“…In the present study, identification of chiral 1,3,4-oxadiazol-2-ones as potent and selective FAAH inhibitors has been described. The separated enantiomers…”
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Comparative molecular field analysis and molecular dynamics studies of α/β hydrolase domain containing 6 (ABHD6) inhibitors by Kaczor, Agnieszka A., Targowska-Duda, Katarzyna M., Patel, Jayendra Z., Laitinen, Tuomo, Parkkari, Teija, Adams, Yahaya, Nevalainen, Tapio J., Poso, Antti

“…The endocannabinoid system remains an attractive molecular target for pharmacological intervention due to its roles in the central nervous system in learning,…”
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Loratadine analogues as MAGL inhibitors by Patel, Jayendra Z., Ahenkorah, Stephen, Vaara, Miia, Staszewski, Marek, Adams, Yahaya, Laitinen, Tuomo, Navia-Paldanius, Dina, Parkkari, Teija, Savinainen, Juha R., Walczyński, Krzysztof, Laitinen, Jarmo T., Nevalainen, Tapio J.

“…[Display omitted] Compound 12a (JZP-361) acted as a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46nM), and was found to have almost…”
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Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors by Patel, Jayendra Z., van Bruchem, John, Laitinen, Tuomo, Kaczor, Agnieszka A., Navia-Paldanius, Dina, Parkkari, Teija, Savinainen, Juha R., Laitinen, Jarmo T., Nevalainen, Tapio J.

“…[Display omitted] This article describes our systematic approach to exploring the utility of the 1,3,4-oxadiazol-2-one scaffold in the development of ABHD6…”
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Chemoproteomic, biochemical and pharmacological approaches in the discovery of inhibitors targeting human α/β-hydrolase domain containing 11 (ABHD11) by Navia-Paldanius, Dina, Patel, Jayendra Z., López Navarro, Miriam, Jakupović, Hermina, Goffart, Steffi, Pasonen-Seppänen, Sanna, Nevalainen, Tapio J., Jääskeläinen, Tiina, Laitinen, Tuomo, Laitinen, Jarmo T., Savinainen, Juha R.

“…ABHD11 (α/β-hydrolase domain containing 11) is a non-annotated enzyme belonging to the family of metabolic serine hydrolases (mSHs). Its natural substrates and…”
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Optimization of 1,2,5-Thiadiazole Carbamates as Potent and Selective ABHD6 Inhibitors by Patel, Jayendra Z., Nevalainen, Tapio J., Savinainen, Juha R., Adams, Yahaya, Laitinen, Tuomo, Runyon, Robert S., Vaara, Miia, Ahenkorah, Stephen, Kaczor, Agnieszka A., Navia-Paldanius, Dina, Gynther, Mikko, Aaltonen, Niina, Joharapurkar, Amit A., Jain, Mukul R., Haka, Abigail S., Maxfield, Frederick R., Laitinen, Jarmo T., Parkkari, Teija

“…At present, inhibitors of α/β‐hydrolase domain 6 (ABHD6) are viewed as a promising approach to treat inflammation and metabolic disorders. This article…”
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Diaryl Dihydropyrazole-3-carboxamides with Significant In Vivo Antiobesity Activity Related to CB1 Receptor Antagonism:  Synthesis, Biological Evaluation, and Molecular Modeling in the Homology Model by Joharapurkar, Amit, Raval, Saurin, Patel, Jayendra Z, Soni, Rina, Raval, Preeti, Gite, Archana, Goswami, Amitgiri, Sadhwani, Nisha, Gandhi, Neha, Patel, Harilal, Mishra, Bhupendra, Solanki, Manish, Pandey, Bipin, Jain, Mukul R, Patel, Pankaj R

“…A number of analogues of diaryl dihydropyrazole-3-carboxamides have been synthesized. Their activities were evaluated for appetite suppression and body weight…”
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1,3,4-Oxadiazol-2-ones as fatty-acid amide hydrolase and monoacylglycerol lipase inhibitors: Synthesis, in vitro evaluation and insight into potency and selectivity determinants by molecular modelling by Käsnänen, Heikki, Minkkilä, Anna, Taupila, Susanna, Patel, Jayendra Z., Parkkari, Teija, Lahtela-Kakkonen, Maija, Saario, Susanna M., Nevalainen, Tapio, Poso, Antti

“…Inhibition of the key hydrolytic enzymes of the endocannabinoid system, fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), has been proposed…”
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Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect by Srivastava, Brijesh Kumar, Soni, Rina, Patel, Jayendra Z., Joharapurkar, Amit, Sadhwani, Nisha, Kshirsagar, Samadhan, Mishra, Bhupendra, Takale, Vijay, Gupta, Sunil, Pandya, Purvi, Kapadnis, Prashant, Solanki, Manish, Patel, Harilal, Mitra, Prasenjit, Jain, Mukul R., Patel, Pankaj R.

“…A few thienyl substituted pyrazole derivatives were synthesized to aid in the characterization of the cannabinoid receptor antagonist and also to serve as…”
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