224817-03-2Relevant academic research and scientific papers
Synthesis, computational predictions of selective bioactive nicotinamide derivatives and in vitro biological evaluations
Thirunavukarasu, Jayaprakash,Begam, Rosina,Shajahan
, p. 518 - 526 (2019/07/09)
A series of nicotinamide derivatives were designed and studied in silico molecular docking predictions against inflammatory responsible enzymes (cyclooxygenase-1(1PGG) and cyclooxygenase-2 (4-COX)). The well-predicted compounds were synthesized, characterized by the spectroscopic techniques namely, Proton Nuclear Magnetic Resonance, Carbon Nuclear Magnetic Resonance and the in vitro biological studies namely, anti-inflammatory activity and anti-diabetic activity. Furthermore, Density Functional Theory Calculations and Frontier Molecular Orbital by molecular electrostatic potential were investigated.
SAR based design of nicotinamides as a novel class of androgen receptor antagonists for prostate cancer
Yang, Su Hui,Song, Chin-Hee,Van, Hue Thi My,Park, Eunsook,Khadka, Daulat Bikram,Gong, Eun-Yeung,Lee, Keesook,Cho, Won-Jea
supporting information, p. 3414 - 3418 (2013/06/05)
Molecular knowledge of pure antagonism and systematic SAR study offered a direction for structural optimization of DIMN to provide nicotinamides as a novel series of AR antagonists. Nicotinamides with extended linear scaffold bearing sterically bulky alkoxy groups on isoquinoline end were synthesized for H12 displacement. AR binding affinity and molecular basis of antiandrogenic effect establish the optimized derivatives, 7au and 7bb, as promising candidates of second generation AR antagonists for advanced prostate cancer.
NEW NICOTINAMIDE DERIVATIVES WITH ANTI-ANDROGEN EFFECTS, PROCESSES OF PREPARING, AND ANTIANDROGENS COMPRISING THE SAME
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Page/Page column 11; 13, (2010/12/29)
Provided are novel nicotinamide derivatives and pharmaceutically acceptable salts thereof with anti-androgen effects, preparing processes of the same and antiandrogens containing the same as active ingredients. More particularly, the said nicotinamide derivatives have anti-androgen activity, so that they can be effectively used as a preventive or therapeutic agent for androgen-related diseases such as prostatic disease, androgenic alopecia and acne.
Diacylglycerol Acyltransferase Inhibitors
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Page/Page column 13-14, (2010/05/13)
Provided herein are compounds of the formula (I): were R1 is phenyl, R2 is hydrogen, halogen or lower alkyl, X is carbon on nitrogen, and R3 is isoquinoline, -amino, or a 4- to 6-membered heterocycloalkyl ring and pharmaceutically acceptable salts thereof, which are active as DGAT inhibitors and therefore find uses in treatment of diseases associated with abnormal metabolism of triglicerides such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Substituted pyridine compounds and methods of use
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, (2008/06/13)
Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF- alpha , IL-1 beta , IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
