38895-95-3Relevant academic research and scientific papers
New nicotinic acid-based 3,5-diphenylpyrazoles: design, synthesis and antihyperlipidemic activity with potential NPC1L1 inhibitory activity
Shoman, Mai E.,Aboelez, Moustafa O.,Shaykhon, Montaser Sh. A.,Ahmed, Sanaa A.,Abuo-Rahma, Gamal El-Din A.,Elhady, Omar M.
, p. 673 - 686 (2020/02/25)
Nicotinic acid hydrazide was incorporated into new 4,5-dihydro-5-hydroxy-3,5-diphenylpyrazol-1-yl derivatives. Compounds 6a–h were synthesized, and their antihyperlipidemic activity was evaluated in high cholesterol diet-fed rat model. Compounds 6e, 6f were found to decrease the levels of serum total cholesterol by 14–19% compared to control group. Total triglycerides were also reduced by 24–28% and LDL cholesterol by 16%. As expected from parent niacin, compounds 6e and 6f caused an elevation of HDL cholesterol by 33–41%. Docking study supported the ability of designed compounds to block NPC1L1 active site in a manner similar to that observed with ezetimibe.
Modular access to 1,2-allenyl ketones based on a photoredox-catalysed radical-polar crossover process
Du, Chan,Fang, Jianghua,Fang, Yewen,Lei, Wan,Li, Yan,Liu, Yongjun
supporting information, p. 8502 - 8506 (2021/10/20)
Herein, a new protocol dealing with the preparation of 1,2-allenyl ketones has been successfully developedviathe reactions of enynes with radicals enabled by dual photoredox/copper catalysis. Based on the results of a deuteration experiment and the competition reaction between cyclopropanation and allenation, the mechanism based on a photoredox-neutral-catalysed radical-polar crossover process has been proposed. Synthetic applications of allenes have also been demonstrated.
Synthesis, biological evaluation, quantitative-SAR and docking studies of novel chalcone derivatives as antibacterial and antioxidant agents
Alam, Mohammad Sayed,Rahman, S. M. Mostafizur,Lee, Dong-Ung
, p. 1118 - 1129 (2015/06/08)
In the present study, a series of chalcone derivatives including 17 new compounds were synthesised; their antibacterial activities against eleven bacteria, and their free radical-scavenging activities using DPPH were evaluated. All compounds showed significant antibacterial activities against both Grampositive and Gram-negative bacteria. In particular, compound IIIf strongly inhibited Staphylococcus aureus (JMC 2151) and Enterococcus faecalis (CARS 2011-012) with MIC values of 6.25 μg mL-1 and 12.5 μg mL-1, respectively, which are comparable to that of the standard antibiotic, nalidixic acid. Compound IIIg also inhibited S. aureus with a MIC value similar to that of nalidixic acid (6.25 μg mL-1). Furthermore, like nalidixic acid (MIC value of 25 μg mL-1), compounds IIIa, IIIc and IIId inhibited Listeria monocytogenes (ATCC 43256) with MIC values of 25 μg mL-1, 12.5 μg mL-1 and 25 μg mL-1, respectively. Quantitative structure-activity relationship (Q-SAR) studies using physicochemical calculations indicated that the antibacterial activities of chalcone derivatives correlated well with predicted physicochemical parameters (logP and PSA). Docking simulation by positioning the most active compound IIIf in the active site of the penicillin-binding protein (PBP-1b) of S. aureus was performed to explore the feasible binding mode. Furthermore, most of the compounds synthesised exhibited significant DPPH radical-scavenging activity, although compounds IIc and IIIc exhibited the greatest antioxidant activity with IC50 values of 1.68 μM and 1.44 μM, respectively, comparable to that of the standard antioxidant, ascorbic acid (1.03 μM).
Ecofriendly bromination of chalcones and synthesis of flavones using grinding technique
Jakhar, Komal,Makrandi
, p. 141 - 145 (2013/02/23)
Selective bromination of chalcones and 2'-hydroxychalcones has been carried out with ammonium bromide and ammonium persulphate using grinding technique at RT under aqueous moist condition to give α,β-dibromochalcones and α,β-dibromo-2'- hydroxychalcones respectively. α,β- Dibromo-2'-hydroxychalcones have been cyclodehydrobrominated with barium hydroxide moist and ethanol at RT to give flavones using grinding technique.
Electrophilic bromination of alkenes, alkynes, and aromatic amines with iodic acid/potassium bromide under mild conditions
Khazaei, Ardeshir,Zolfigol, Mohammad Ali,Kolvari, Eskandar,Koukabi, Nadiya,Soltani, Hamid,Bayani, Leyla Sharaf
experimental part, p. 2954 - 2962 (2010/10/20)
Bromination of alkenes, alkynes, and aromatic amines has efficiently been carried out at room temperature in short reaction times using HIO 3/KBr in CH2Cl2/H2O (1:1) to prepare corresponding brominated compounds in excellent yields.
Efficient bromination of alkenes and alkynes using potassium bromide and diacetoxy iodobenzene
Das, Biswanath,Srinivas, Yallamalla,Sudhakar, Chittaluri,Damodar, Kongara,Narender, Ravirala
experimental part, p. 220 - 227 (2009/04/07)
Bromination of alkenes and alkynes has efficiently been carried out at room temperature in short reaction times using KBr and diacetoxy iodobenzene in CH2Cl2-H2O (1:1) to prepare the corresponding trans-dibromo compounds in excellent yields. Copyright Taylor & Francis Group, LLC.
Elctrophilic bromination of alkenes, alkynes, and aromatic amines with potassium bromide/orthoperiodic acid under mild conditions
Khazaei, Ardeshir,Zolfigol, Mohammad Ali,Kolvari, Eskandar,Koukabi, Nadiya,Soltani, Hamid,Komaki, Fatemeh
experimental part, p. 3672 - 3676 (2010/04/05)
Bromination of alkenes, alkynes, and aromatic amines has efficiently been carried out at room temperature in short reaction times using potassium bromide/orthoperiodic acid in dichloromethane-water (1:1) to prepare the corresponding bromo compounds with excellent yields.
Bromination of alkenes and alkynes with (bromodimethyl)sulfonium bromide
Das, Biswanath,Srinivas, Yallamalla,Sudhakar, Chittaluri,Ravikanth, Bommena
experimental part, p. 188 - 190 (2009/07/18)
Alkenes and alkynes were brominated efficiently in high yields with (bromodimethyl)sulfonium bromide in acetonitrile at room temperature. Alkenes produced the corresponding trans-dibromo compounds while alkynes (except phenylacetylene) afforded both the trans-dibromo products (major) and the tetrabromo derivatives (minor). However, phenylacetylene furnished solely the tetrabromo compound.
Solvolytic stereoselective debromination of vic-dibromides with HMPA
Khurana,Bansal,Chauhan
, p. 1089 - 1091 (2007/10/03)
A simple and efficient procedure for the debromination of vic-dibromides has been reported with hexamethylphosphoric triamide at 155-160°C under a nitrogen atmosphere without the aid of any reagent.
