618098-48-9Relevant academic research and scientific papers
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis
Abay, Efrem,Barry, Clifton E.,Basarab, Gregory S.,Boshoff, Helena I. M.,Boyle, Grant A.,Chibale, Kelly,Eyermann, Charles J.,Fienberg, Stephen,Ghorpade, Sandeep R.,Khonde, Lutete Peguy,Lawrence, Nina,Lenaerts, Anne J.,Massoudi, Lisa M.,Myers, Timothy G.,Myrick, Alissa,Nchinda, Aloysius T.,Njoroge, Mathew,Reddy, Virsinha,Robertson, Gregory T.,Singh, Vinayak,Sirgel, Frederick A.,Su, Qin,Van Helden, Paul D.,Müller, Rudolf
, p. 12790 - 12807 (2021/09/11)
Phenotypic whole cell high-throughput screening of a μ150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide 1 as a moderately active hit. Structure-activity
Novel pyrazole-clubbed thiophene derivatives via Gewald synthesis as antibacterial and anti-inflammatory agents
Nayak, Soukhyarani G.,Poojary, Boja,Kamat, Vinuta
, (2020/09/09)
The aim of this study was to synthesize newer potent Schiff bases by condensing 2-amino-5-(2,4-dichlorophenyl)thiophene-3-carbonitrile and 1,3-disubstituted-1H-pyrazole-4-carbaldehydes, and to investigate their biological activity. The compounds were synthesized via Gewald synthesis and characterized by spectral data and elemental analyses. They were screened for their in vitro antibacterial and anti-inflammatory activities. The synthesized compounds were also evaluated for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Compounds 8b, 8c, 8f, 8g, 8k, 8n, and 8o showed promising antibacterial activity. The interactions between the substituted pyrazoles and bovine protein showed promising anti-inflammatory activity. The experimental results revealed compound 8a as a promising antitubercular agent. Hemolytic assays confirmed that the compounds are nontoxic, with percentage hemolysis ranging from 3.6 to 20.1, at a concentration of 1 mg/ml. The results suggest that the pyrazole ring and the substitution pattern on the heterocyclic moiety have an effect on the bioactivity.
Synthesis, anti-inflammatory screening, molecular docking, and COX-1,2/-5-LOX inhibition profile of some novel quinoline derivatives
Chaaban, Ibrahim,Rizk, Ola H.,Ibrahim, Tamer M.,Henen, Shery S.,El-Khawass, El-Sayeda M.,Bayad, Aida E.,El-Ashmawy, Ibrahim M.,Nematalla, Hisham A.
, p. 220 - 235 (2018/04/05)
New quinoline compounds comprising pyrazole scaffold through different amide linkages were synthesized. The synthesized compounds were evaluated for their anti-inflammatory activity. Eight compounds (5c, 11b,c, 12c, 14a,b, 20a and 21a) were found to exhib
Antitubercular and antimicrobial activity of nh4vo3 promoted 1,4-dihydropyridine incorporated 1,3,4-Trisubstituted pyrazole
Harikrishna, Nandam,Isloor, Arun M.,Ananda,Parish, Tanya,Jamalis, Joazaizulfazli,Ghabbour, Hazem A.,Fun, Hoong-Kun
, p. 699 - 711 (2017/07/15)
Background: A new series of pyrazole containing 1,4-dihydropyridine derivatives 5a-i and 6a-i were synthesized from substituted acetylated aryls and substituted phenylhydrazine by the multistep reaction. Method: The target compounds 1,4-dihydropyridine de
1,3,4-Trisubstituted pyrazole bearing a 4-(chromen-2-one) thiazole: Synthesis, characterization and its biological studies
Harikrishna,Isloor, Arun M.,Ananda,Obaid, Abdulrahman,Fun, Hoong-Kun
, p. 43648 - 43659 (2015/05/27)
A new series 3-{2-[N′-(1,3-disubstituted-1H-pyrazol-4-yl-methylene)-hydrazino]-thiazol-4-yl}-chromen-2-one (10a-l) was synthesized by a multi-step reaction. All the synthesized compounds were characterized by IR, NMR, and mass spectral studies, followed by elemental analysis. The newly synthesized thiazole compounds were screened for their in vitro antibacterial and antifungal studies against various microorganisms. Antimicrobial studies carried out by the well diffusion method, showed a very good zone of inhibition for both bacteria (at a range of 20-50 mm diameter) and fungi (at a range of 10-30 mm diameter). Minimum Inhibitory Concentration (MIC) required for the 100% inhibition of bacteria and fungi was found to be as low as 15.6 μg ml-1 for a few of the synthesized compounds.
