52211-81-1Relevant articles and documents
Novel pyranopyrazole derivatives comprising a benzoxazole core as antimicrobial inhibitors: Design, synthesis, microbial resistance and machine aided results
Garcia, Jarem Raul,Kumari, Avula Krishna,Reddy, Guda Mallikarjuna,Reddy, Vemulapati Hanuman
, (2020)
From a medical point of view lot of existing antibiotics became unusable because microbial gained strong antibiotic resistance. The combination of two compounds in one core may lead to kill such type of pathogens. Herein, we developed pyranopyrazole derivatives comprising benzoxazole moiety by green approach strategy and studied their antimicrobial performance on four bacteria and two fungi. As a result, most of the compounds delivered reliable toxicity to kill the pathogens. In those, 6a exhibited considerable activity against the microbial pathogens. Moreover, compounds 6d, 6l, and 6n showed prominent antibacterial activity. In addition, molecular docking studies of docked compounds revealed the strong bonding interaction with DNA-Gyrase and were docked into the intercalation location of DNA of the DNA-gyrase complex. The molecule bounded to the DNA stabilized by the H bonds, hydrophobic interactions, and π-π interaction. In addition, the linked 5-chlorobenazoxazole structure stabilized by the DT-8 and DG2009 of the F chain with pi-pi interactions. From the computer-aided results, it was observed that compound 6a demonstrated maximum docking score ?10.0 kcal/mole towards DNA-gyrase. Overall, this investigation suggested that these biologically active compounds can be utilized as leads for preclinical studies with the goal of developing newer antimicrobial drugs.
Synthesis, in-vitro and in-silico studies of triazinoindole bearing bis-Schiff base as β-glucuronidase inhibitors
Ahmad, Shakeel,Aziz, Aamir,Khan, Fahad,Rahim, Fazal,Sarfraz, Maliha,Taha, Muhammad,Ullah, Hayat,Wadood, Abdul
, (2021/07/16)
Triazinoindole bearing bis-Schiff base analogs (1–20) were synthesized by triazinoindole-thione ring formation, triazinoindole-thiol-phenylethanone, followed by triazinoindole bis-Schiff base formation. Synthesized analogs showed β-glucuronidase potential with IC50 value ranging between 2.60 ± 0.10 to 55.40 ± 1.60 μM as compared to standard D-saccharic acid 1,4-lactone (IC50 = 48.10 ± 1.2 μM). Analog 20 was the most potent one with IC50 value 2.60 ± 0.10 μM. Analogs 17, 4 showed IC50 values 5.20 ± 0.20 and 5.70 ± 0.20 μM respectively and withstand 2nd and 3rd ranked scaffolds among the synthesized analogs. All other sixteen analogs showed many-fold better potency with IC50 values ranging from 7.9 ± 0.2 to 48.1 ± 1.2 μM. The structure-activity relationship was established and confirmed of binding interactions through molecular docking studies.
Facile synthesis of (E)-β-(trifluoromethyl)styrenes from halothane (HCFC-123B1)
Hirotaki, Kensuke,Kawazoe, Genyu,Hanamoto, Takeshi
, p. 169 - 173 (2015/03/04)
A practical and convenient synthesis of (E)-β-(trifluoromethyl)styrenes has been achieved by the reaction of commercially available halothane (HCFC-123B1) and hydrazones prepared in advance in situ, in the presence of 1,2-ethylenediamine and a catalytic amount of CuCl2·2H2O at room temperature. The products showed acceptable to high yields and high to excellent stereoselectivity. This handy synthetic method provided easy access to a variety of (E)-β-(trifluoromethyl)styrenes.
The Huang-Minlon modification of Wolff-Kishner reduction in rapid and simple way using microwave technology
Chattopadhyay, Sarmishtha,Banerjee, Sajal Kumar,Mitra, Alok Kumar
, p. 906 - 907 (2007/10/03)
A high yielding, simple and fast method for the reduction of various aldehydes and ketones to the respective hydrocarbons following Huang-Minlon modification tender microwave irradiation is described.
RETROVIRAL PROTEASE INHIBITING COMPOUNDS
-
, (2008/06/13)
A retroviral protease inhibiting compound of the formula: STR1 is disclosed wherein R 1, R 2, R 5, R 6, Y m and Y' n are herein defined.