189882-31-3Relevant academic research and scientific papers
Three-component reaction involving metal-free heteroannulation of N-Boc-3-amido indole, aryl aldehydes, and aromatic alkynes under microwave conditions: Synthesis of highly diversified δ-carbolines
Sharma, Sudhir K.,Mandadapu, Anil K.,Saifuddin, Mohammad,Gupta, Sahaj,Agarwal, Piyush K.,Mandwal, Ashok K.,Gauniyal, Harsh M.,Kundu, Bijoy
experimental part, p. 6022 - 6024 (2010/11/18)
An efficient synthesis toward highly diversified δ-carbolines via one-pot multicomponent reaction using N-Boc-3-amido indoles, aryl aldehydes, and aromatic terminal alkynes under microwave conditions has been described.
Design, synthesis, and biological evaluation of substituted-N-(thieno[2,3-b]pyridin-3-yl)-guanidines, N-(1H-pyrrolo[2,3-b]pyridin-3-yl)-guanidines, and N-(1H-indol-3-yl)-guanidines
Bahekar, Rajesh H.,Jain, Mukul R.,Goel, Ashish,Patel, Dipam N.,Prajapati, Vijay M.,Gupta, Arun A.,Jadav, Pradip A.,Patel, Pankaj R.
, p. 3248 - 3265 (2008/02/07)
Sulfonylureas stimulate insulin secretion independent of the blood glucose concentration and therefore cause hypoglycemia in type 2 diabetic patients. Over the last years, a number of aryl-imidazoline derivatives have been identified that stimulate insulin secretion in a glucose-dependent manner. In the present study, we have developed three series of substituted N-(thieno[2,3-b]pyridin-3-yl)-guanidine (2a-l), N-(1H-pyrrolo[2,3-b]pyridin-3-yl)-guanidine (3a-l), and N-(1H-indol-3-yl)-guanidine (4a-l) as new class of antidiabetic agents. In vitro glucose-dependent insulinotropic activity of test compounds 2a-l, 3a-l, and 4a-l was evaluated using RIN5F (Rat Insulinoma cell) based assay. All the test compounds showed concentration-dependent insulin secretion, only in presence of glucose load (16.7 mmol). Some of the test compounds (2c, 3c, and 4c) from each series were found to be equipotent to BL 11282 (standard aryl-imidazoline), which indicated that the guanidine group acts as a bioisostere of imidazoline ring system.
4-Piperidinecarboxamide modulators of vanilloid VR1 receptor
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Page/Page column 51, (2010/11/08)
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.
