• Analysis of the GHSR screening data for inactive library mem

  2021-12-28

  

  Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr

• Although our knowledge of how FAs

  2021-12-28

  

  Although our knowledge of how FAs affect GLP-1-producing L-cells is sparse and incomplete, increased intracellular ceramide [6], ER stress [12], and increased production of ROS [9] are indicated mediators of the lipotoxicity induced by SFA (16:0). However, the role for/interaction between these medi

• br Acknowledgments The breast cancer

  2021-12-28

  

  Acknowledgments The breast cancer laboratory is supported by the Australian National Health and Medical Research Council (NHMRC) grants no. 1016701, no. 1024852, no. 1086727; NHMRC IRIISS; the Victorian State Government through VCA funding of the Victorian Breast Cancer Research Consortium and Op

• A phase I clinical trial has

  2021-12-28

  

  A phase I clinical trial has been completed for assessing CEP-26401 in cognitive impairment in healthy individuals without disclosing any results (NCT01903824). Although CEP-26401 is under clinical trial study, several projects are in progress for synthesizing novel irdabisant analogs in order to im

• Sometime ago we have described diamino triazines

  2021-12-28

  

  Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by Semaxanib and zymosan. In this work we describe new deriv

• Another important outcome of reducing

  2021-12-28

  

  Another important outcome of reducing hypothalamic HIF in DIO was the increase in gliosis and hypothalamic inflammation. Both experimental and human studies have shown that hypothalamic inflammation plays an important role in obesity by inducing resistance to anorexigenic signals, such as insulin an

• Benzene metabolism occurs primarily in the liver where benze

  2021-12-28

  

  Benzene metabolism occurs primarily in the liver where benzene is converted into phenol, catechol, hydroquinone (HQ). HQ is further converted to 1,4-benzoquinone (1,4-BQ) in the bone marrow which is the primary organ of benzene toxicity (Bolton et al., 2000). 1,4-BQ is an important benzene metabolit

• Taken together this study provides the proof of concept that

  2021-12-28

  

  Taken together, this study provides the proof of concept that our novel heterologous human/rat HER2-specific T cell vaccine HuRt-TEXO, which is capable of stimulating both humoral and CTL responses leading to potent antitumor immunity through the circumvention of HER2 tolerance in double transgenic

• The initial beta carboline derivatives used in the in

  2021-12-28

  

  The initial beta-carboline derivatives used in the in silico docking experiments were prepared using the procedure outlined in . Harmol, , was -alkylated with -Boc-protected alkylamines in the presence of cesium carbonate to give and . The carbamate protecting group was removed under acidic conditio

• These to date remain the only two

  2021-12-28

  

  These to date remain the only two reports of mutations in GC-C found in humans. Perhaps this once again emphasized the critical requirement of the presence of an optimally functional GC-C in the intestine, since neither its loss, nor its hyperactivity, can be tolerated in humans without severe conse

• The imidazopyridines and related imidazopyrimidines and were

  2021-12-28

  

  The imidazopyridines and related imidazopyrimidines – and – were constructed from the key amine intermediates – ( X=CH and Ar=2-FPh, X=N and Ar=2-FPh, X=CH and Ar=5-pyrimidine, X=CH and Ar=2-methyl-5-pyrimidine, and X=CF and Ar=2-methyl-5-pyrimidine). These were synthesized a modified Horner–Em

• 279 3 As comparators compounds and were made using the pyraz

  2021-12-28

  

  As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it

• br Results and discussion br Conclusions In summary

  2021-12-28

  

  Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10

• br Author s contributions br Conflict of interest br Acknowl

  2021-12-28

  

  Author's contributions Conflict of interest Acknowledgements This work was supported in part by a grant from Department of Biotechnology (DBT), Government of India (Sanction Order No.: BT/563/NE/U-Excel/2016). MC, PDG and SKM acknowledge the Ministry of Human Resource and Development (MHRD)

• Since the late s synthetic

  2021-12-28

  

  Since the late 1940s, synthetic GC (e.g. prednisone, prednisolone, dexamethasone) have been used extensively in the treatment of chronic inflammatory conditions such as rheumatoid arthritis and asthma, and for their immunosuppressant action in preventing organ rejection post transplantation. Cortico

15408 records 499/1028 page Previous Next First page 上5页 496497498499500 下5页 Last page