19143-12-5Relevant academic research and scientific papers
Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity
Oezdemir, Ahmet,Altintop, Mehlika Dilek,Kaplancikli, Zafer Asim,Turan-Zitouni, Guelhan,Ciftci, Guelsen Akalin,Yildirim, Safak Ulusoylar
, p. 1221 - 1227 (2013)
In the present study, 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (1-6) were synthesized via the ring closure reaction of 1-(2-thienyl)-3-aryl-2-propen-1-ones with hydrazine hydrate in acetic acid. The chemical structures of the compounds were
Structural identification of pyrazoles and pyrimidines using 2D HMBC NMR and single-crystal X-ray diffraction
Al-Bogami
, p. 4611 - 4614 (2015)
A facile and highly efficient microwave-assisted synthesis of functionalized pyrazoles and pyrimidines based on the regiospecific synthesis is reported. The present work provides unambiguous evidence of the pyrazoles was determined using 2D HMBC NMR. The structure for pyrimidine have been confirmed by single-crystal X-ray diffraction.
Microwave-assisted synthesis and bioevaluation of new sulfonamides
Gul, Halise Inci,Yamali, Cem,Yesilyurt, Fatma,Sakagami, Hiroshi,Kucukoglu, Kaan,Gulcin, Ilhami,Gul, Mustafa,Supuran, Claudiu T.
, p. 369 - 374 (2017)
In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13C N
Synthesis of arylidene-based benzoxazine derivatives as promising antimicrobial materials
Al-Ghamdi, Youssef O.,Alamry, Khalid A.,Alzahrani, Abdullah Y.,Elfaky, Mahmoud A.,Hussein, Mahmoud A.,Hussien, Mostafa A.,Musa, Abdulrahman
supporting information, (2021/12/10)
The current study is focused on the synthesis of two novel arylidene-based benzoxazines namely: 3-(3-phenyl-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)-1-(thiophen-2-yl)-2-propenone (PTP), and 3-(3-phenyl-3,4-dihydro-2H-benzo[e][1,3]-oxazin-6-yl)-1-(pyridin-2-yl)-2-propenone (PPP). The benzoxazines were obtained as condensation products of the reaction of each of the phenol analogs: [3-(4-hydroxyphenyl)-1-(2-thiophenyl)-2-propenone] (HTP), and [3-(4-hydroxyphenyl)-1-(2-pyridinyl)-2-propenone] (HPP), with aniline, and paraformaldehyde, respectively. PTP and PPP were structurally confirmed using analysis such as ultraviolet (UV) spectroscopy, together with FTIR, and 1H-NMR and 13C-NMR spectral analyses, respectively. The benzoxazine derivatives revealed an excellent antimicrobial activity against the selected bacterial (including Gram-positive & Gram-negative) and fungi. The antimicrobial activity was also investigated using the agar diffusion approach. The qualitative assay of the biological study from the inhibition zones for the PTP, PPP, and PBO revealed interesting results. The examinations revealed some levels of antimicrobial efficacy against the selected bacterial strains used. However, the biological efficacy of PTP appeared to be better with larger zones of inhibition against the growth of the micro-organisms. Moreover, the molecular docking studies of PTP, PPP, and PBO derivatives were screened against the “5FSA” protein. PPP derivative displayed a good activity than the other derivatives PTP and PBO in docking with 5FSA protein. The obtained values were ?7.34, ?7.70, and ?5.70 Kcal/Mol for PPP, PTP, and PBO respectively compared to Fluconazole reference value ?7.86 Kcal/Mol.
Synthesis, characterization, and antioxidant activity of some new benzodiazepine derivatives
Bhat, K. Ishwar,Kumar, Abhishek
, p. 397 - 400 (2018/09/29)
A series of novel 4-(substituted phenyl)-2-(2-thienyl)-2,3-dihydro-1H-benzo[b] [1,4] diazepines (MB1-MB8) has been synthesized from 3-(substituted phenyl)-1-(2-thienyl)prop-2-en-1ones (MC1-MC8). The latter compo
Mesomorphism Dependence of Chalconyl Derivatives on Position of -CH=CH- Unit
Rakhasia,Bhola,Bhoya
, p. 81 - 89 (2016/04/05)
A novel homologous series of heterocyclic chalconyl esters (C1 to C16) has been synthesized and studied with a view to understanding and establishing the effects of molecular structure on liquid crystal (LC) properties and the degree of liquid crystallinity. The C1 to C6 homologues are not liquid crystals, the C7 homologue is enantiotropic nematic, the C8 to C16 homologues are smectogenic in addition to nematogenic (C8 & C10 monotropic smectic). The texture of nematic phases are threaded or Schlieren and that of the smectic phase are fan-shaped smectic-A or smectic-C type. Transition temperatures and the textures of mesophases were determined by an optical polarizing microscope equipped with a heating stage. Transition curves Cr-I/M, Sm-N/N-Sm, and N-I showing phase behaviors of series in a phase diagram behave in normal manner. Thermal stability for smectic and nematic are 115.66°C and 126.83°C and their mesophase lengths minimum to maximum are 6.3 to 12.9°C and 6.9°C to 17.4°C, respectively. Analytical and spectral data confirms the molecular structures of homologues. LC properties of present novel series are compared with structurally similar other reported series.
Thieny/furanyl-hydroxyphenylpropenones as inhibitors of LPS-induced ROS and NO production in RAW 264.7 macrophages, and their structure-activity relationship study
Kadayat, Tara Man,Kim, Mi Jin,Nam, Tae-Gyu,Park, Pil-Hoon,Lee, Eung-Seok
, p. 2481 - 2486 (2014/09/17)
Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, and evaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages. Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production in RAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moiety plays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3- thienyl moiety on molecule.
Synthesis, pharmacological, and biological screening of novel derivatives of benzodiazepines
Bhat, K. Ishwar,Chauhan, Manoj Kumar Singh,Kumar, Abhishek,Kumar, Pankaj
, p. 1189 - 1192 (2014/08/05)
A series of novel 4-(substituted phenyl)-2-(thiophen-2-yl)-2,3-dihydro-1H- benzo[b][1,4]diazepine have been synthesized from 3-(substituted phenyl)-1-(thiophen-2-yl)prop-2-en-1-one. 3-(Substituted phenyl)-1-(thiophen-2- yl)prop-2-en-1-one was prepared by
Synthesis and QSAR analysis of chalcone derivatives as nitric oxide inhibitory agent
Lam, Kok Wai,Lajis, Nordin H.,Uddin, Reaz,Ul-Haq, Zaheer,Liew, Choi Yi,Tham, Chau Ling,Israf, Daud A.,Syahida, Ahmad,Rahman, Mohd. Basyaruddin Abdul
, p. 1953 - 1966,14 (2020/07/30)
In this study, thirty-eight chalcone analogs were synthesized and evaluated for nitric oxide (NO) inhibition activity on RAW 264.7 cells. Among these compounds, chalcones bearing furanyl group showed remarkable anti-inflammatory activity. Both compounds 2d and 2j were identified as the most potent NO inhibitor on IFN-γ/LPS-activated RAW 264.7 cells. In order to examine the structure-activity relationship, a 3D QSAR analysis was carried out by comparative molecular field analysis (CoMFA) method on the selected chalcones. Partial least square analysis produced a statistically coherent model with good predictive value, r2 = 0.989 and a good cross validated value, q 2 = 0.583.
Synthesis of some 1-[(N,N-disubstituted thiocarbamoylthio)acetyl]-3-(2- thienyl)-5-aryl-2-pyrazoline derivatives and investigation of their antibacterial and antifungal activities
Turan-Zitouni, Gulhan,Oezdemir, Ahmet,Gueven, Kiymet
, p. 96 - 104 (2007/10/03)
Fourteen new 1-[(N,N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)- 5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N,N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised compounds were confirmed by elemental analyses, UV, IR, 1H-NMR and FAB+-MS spectral data. Their antibacterial activities against Proteus vulgaris (NRRL B-123), Escherichia coli (NRRL B-3704), Aeromonas hydrophila (Ankara University, Faculty of Veterinary Sciences), Salmonella typhimurium (NRRL B-4420), Streptococcus feacalis (NRRL B-14617), Micrococcus luteus (NRLL B-4375) were investigated and in this investigation, a significant level of activity was illustrated. Antifungal activities of the compounds against Candida albicans and Candida globrata (isolates obtained from Osmangazi Uni. Fac. of Medicine) were found to be inactive. Compounds 7c-n were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system and BACTEC 12B medium. The preliminary results indicated that all of the tested compounds were inactive against the test organism.
