956262-41-2Relevant academic research and scientific papers
New library of pyrazole–imidazo[1,2-α]pyridine molecular conjugates: Synthesis, antibacterial activity and molecular docking studies
Ebenezer, Oluwakemi,Awolade, Paul,Koorbanally, Neil,Singh, Parvesh
, p. 162 - 173 (2019/11/03)
A library of novel pyrazole–imidazo[1,2-α]pyridine scaffolds was designed and synthesized through a one-pot three-component tandem reaction. The structures of synthesized conjugates were confirmed by spectroscopic techniques (NMR, IR and HRMS). In vitro antibacterial evaluation of the twelve synthesized molecules (7a, 8a–k) against methicillin-resistant Staphylococcus aureus and normal strains of Escherichia coli, Salmonella typhimurium, Klebsiella pneumonia and Pseudomonas aeruginosa established 8b, 8d, 8e, 8h and 8i as potent antibacterial agents with superior minimum bactericidal concentration, compared with standard drug ciprofloxacin. Molecular docking studies of all active compounds into the binding site of glucosamine-6-phosphate synthase were further performed in order to have a comprehensive understanding of putative binding modes within the active sites of the receptor.
Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors
Sun, Liangpeng,Wang, Peipei,Xu, Lili,Gao, Lixin,Li, Jia,Piao, Huri
, p. 1187 - 1193 (2019/03/26)
Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 ± 0.09 μM) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Molecular docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Antitubercular Activity and Synergistic Study of Novel Pyrazole Derivatives
Jadhav, Sunil B.,Fatema, Samreen,Sanap, Gajanan,Farooqui, Mazahar
, p. 1634 - 1644 (2018/07/24)
A series of 20 novel pyrazole derivatives were designed and prepared, characterized by 1H-NMR, mass spectra (ES-MS), 13C-NMR, and elemental analysis. The synthesized compounds were then evaluated for their growth inhibitory activity
Thiazolo[3,2-a] Pyrimidones as a Novel Anti-TB Agents
Jadhav, Sunil B.,Fatema, Samreen,Bhagat, Sunil S.,Farooqui, Mazahar
, p. 2893 - 2900 (2018/10/24)
A series of novel thiazolo pyrimidine derivatives were designed, synthesized, and assessed for their in vitro anti-mycobacterial activities. All hybrids displayed considerable antitubercular activities against primary Mycobacterium smegmatis mc2 155 screening and successive Mycobacterium tuberculosis H37Rv. In particular, the hybrid entities 13 and 14 (minimum inhibitory concentration: 47 and 39?μg/mL) were found to be equipotent candidates with first-line antitubercular agent rifampicin, which could act as a lead for further optimization.
Synthesis of novel pyrazolyl tetrazoles as selective COX-2 inhibitors
Swetha, Kolli Sri,Parameshwar, Ravula,Reddy, B. Madhava,Babu, V. Harinadha
, p. 4886 - 4892 (2013/09/23)
A series of novel pyrazolyl tetrazoles were synthesized by introducing tetrazole moiety at the fourth position of 1,3-substituted pyrazole nucleus. Synthesis was carried out by cyclization of different pyrazolonitriles using sodium azide in the presence of triethylammonium chloride as phase transfer catalyst. The structures of the synthesized compounds were confirmed on the basis of physical and spectral data. Among the synthesized compounds, 4b and 4e displayed significant anti-inflammatory activity with no observable ulcerogenic effect when compared with diclofenac sodium. Furthermore, compounds 4b and 4e were found to have COX-2 selectivity with a ratio of 0.44 and 0.48, respectively.
Synthesis of novel 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties as potential antibacterial agents
Xu, Li-Li,Zheng, Chang-Ji,Sun, Liang-Peng,Miao, Jing,Piao, Hu-Ri
, p. 174 - 178 (2012/03/26)
In the present study, a series of 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties were synthesized and their antimicrobial activities were tested against various Gram-positive and Gram-negative bacteria. 1,3-diaryl-4-formylpyrazoles were synthesized as key intermediates following a Vilsmeier-Haack strategy. Several compounds with an MIC of 2 μg/mL, exhibited stronger antibacterial activity against the methicillin-resistant Staphylococcus aureus (MRSA) than the controls. None of the compounds showed any activity against Gram-negative bacteria.
Efficient and rapid synthesis of highly functionalized novel symmetric 1,4-dihydropyridines using glacial acetic acid as solvent
Thakrar, Shailesh,Bavishi, Abhay,Bhavsar, Dhairya,Parekh, Shrey,Vala, Hardev,Radadiya, Ashish,Parmar, Manisha,Savant, Mahesh,Shah, Anamik
, p. 3269 - 3278 (2012/09/08)
A new series of 1,4-dihydropyridines bearing a pyrazole moiety in the 4-position were synthesized by a variation of the classical Hantzsch synthesis. The reaction of 1,3-diphenyl-1H-pyrazole-4-carbaldehyde 4a-n with 3-amino crotononitrile in the presence of glacial acetic acid afforded novel 3,5-dicyano-2,6-dimethyl 1,4-dihydropyridines 5a-n. The procedure has short reaction time (15-20 min), easy workup, and good yield of product. The structures of all synthesized compounds were well characterized by mass, infrared, 1H and 13C NMR, and elemental analysis.
Novel, mild, and highly efficient method for the synthesis of 2-arylbenzothiazoles by the oxidation of 2-arylbenzothiazolines with silicon lewis acids
Sonika,Meenakshi,Malhotra, Rajesh
, p. 136 - 146 (2011/03/19)
Oxidation of structurally diverse 2-arylbenzothiazolines to give the corresponding 2-arylbenzothiazoles has been carried out in benzene using dimethyldichlorosilane and trimethylchlorosilane. Short reaction times, mild reaction conditions, easy and quick isolation of the products, and excellent yields are the main advantages of this procedure. Copyright
