65950-49-4Relevant academic research and scientific papers
Synthesis and antimicrobial activities of 2-azetidinyl- 4-quinazolinone derivatives of diclofenac analogue
Patel, Navin B.,Patel, Jaymin C.
, p. 511 - 521 (2011)
A new class of 2-azetidinyl-4-quinazolinones 6a-k was synthesized by multi-step process, starting from 2-[2-(2,6-dichlorophenyl)amino]phenyl acetic acid 1. Acid 1 was easily converted to acid chloride 2, which on cyclization reaction with 5-bromo anthrani
A general strategy to add diversity to ruthenium arene complexes with bioactive organic compounds: Via a coordinated (4-hydroxyphenyl)diphenylphosphine ligand
Biancalana, Lorenzo,Batchelor, Lucinda K.,De Palo, Alice,Zacchini, Stefano,Pampaloni, Guido,Dyson, Paul J.,Marchetti, Fabio
supporting information, p. 12001 - 12004 (2017/09/25)
Esterification of (4-hydroxyphenyl)diphenylphosphine, coordinated to the [Ru(η6-p-cymene)Cl2] fragment, allows a series of bioactive carboxylic acids to be introduced directly into the organometallic molecule. Evaluation of the compounds on human ovarian cancer cells reveals synergistic enhancements in their antiproliferative activity relative to their bioactive organic and organometallic precursors.
Novel penicillin analogues as potential antimicrobial agents; Design, synthesis and docking studies
Ashraf, Zaman,Bais, Abdul,Manir, Md. Maniruzzaman,Niazi, Umar
, (2015/10/12)
A number of penicillin derivatives (4a-h) were synthesized by the condensation of 6-amino penicillinic acid (6-APA) with non-steroidal anti-inflammatory drugs as antimicrobial agents. In silico docking study of these analogues was performed against Penicillin Binding Protein (PDBID 1CEF) using AutoDock Tools 1.5.6 in order to investigate the antimicrobial data on structural basis. Penicillin binding proteins function as either transpeptidases or carboxypeptidases and in few cases demonstrate transglycosylase activity in bacteria. The excellent antibacterial potential was depicted by compounds 4c and 4e against Escherichia coli, Staphylococcus epidermidus and Staphylococcus aureus compared to the standard amoxicillin. The most potent penicillin derivative 4e exhibited same activity as standard amoxicillin against S. aureus. In the enzyme inhibitory assay the compound 4e inhibited E. coli MurC with an IC50 value of 12.5 μM. The docking scores of these compounds 4c and 4e also verified their greater antibacterial potential. The results verified the importance of side chain functionalities along with the presence of central penam nucleus. The binding affinities calculated from docking results expressed in the form of binding energies ranges from -7.8 to -9.2kcal/mol. The carboxylic group of penam nucleus in all these compounds is responsible for strong binding with receptor protein with the bond length ranges from 3.4 to 4.4 ?. The results of present work ratify that derivatives 4c and 4e may serve as a structural template for the design and development of potent antimicrobial agents.
Design, synthesis and docking studies of some novel isocoumarin analogues as antimicrobial agents
Ashraf, Zaman,Saeed, Aamer,Nadeem, Humaira
, p. 53842 - 53853 (2015/02/19)
A number of novel isocoumarin analogues have been synthesized by the condensation of homophthalic acid anhydride with different non-steroidal anti-inflammatory drugs (NSAIDs). To investigate the antimicrobial data on a structural basis, in silico docking studies of the synthesized compounds (4a-4g) into the crystal structure of UDP-N-acetylmuramate-l-alanine ligase using an Autodock PyRx virtual screening program were performed in order to predict the affinity and orientation of the synthesized compounds at the activities. UDP-N-acetylmuramate-l-alanine ligase is essential for d-glutamate metabolism and peptidoglycan biosynthesis in bacteria. R2 values showed good agreement with predicted binding affinities obtained by molecular docking studies. The results indicate that the basic nucleic portion of the (4c), (4g), (4f) and (4a) binds into the specificity pocket. In this pocket, the isocoumarin nucleus of these compounds interacts with the amino acid residue of the target. Moreover, it is verified by in vitro antimicrobial screening, in which all of the compounds were active against tested bacterial strains. Among these compounds (4c), (4g), (4f) and (4a) showed good bacterial zone inhibition. This journal is
Polyfunctional action of biologically active compounds in antitumor chemotherapy of cyclophosphamide
Bogatyrenko,Konovalova,Sipyagin,Bogatyrenko,Kuropteva,Baider,Sashenkova,Fedorov
, p. 1187 - 1191 (2015/04/13)
Combinations of the known cytostatic cyclophosphamide (cyclophosphan) with hydroxamic acids (asparagylhydroxamic and salicylhydroxamic), nitric oxide donor (sodium nitrate), and an original hybrid non-steroidal anti-inflammatory compound, viz., diclofenac
Synthesis, anti-inflammatory and ulcerogenicity studies of some substituted pyrimido[1,6-a]azepine derivatives
El-Sayed, Nehad A.,Awadallah, Fadi M.,Ibrahim, Nashwa A.,El-Saadi, Mohammed T.
experimental part, p. 3147 - 3154 (2010/08/20)
New series of pyrimido[1,6-a]azepines were prepared through reaction of the key amino compound 4 with various reagents to give a variety of 3-N-substituted amino derivatives 5-13. The synthesized compounds included the Mannich bases 5a-c, the formimidic acid ester 6, the phenylformamidines 7a-c, the benzylidine amino derivatives 8a-c, the acetic acid derivatives 9, 10a-c and 11, the carbamoylformates 12a,b and the amides 13a,b. All compounds were screened for their anti-inflammatory activity using the carrageenan-induced paw oedema in rats using diclofenac sodium as reference drug. In addition, ulcer indices for the most active compounds were calculated. Compounds 3, 4, 8a,c, 11 and 12a, b showed activity similar to or higher than diclofenac sodium with no or minimal gastric ulceration. The most active compound with no ulcerogenic effect is the amino derivative 4 (IC 50=6.61 mmol/kg).
Synthesis, characterization and in vitro antimicrobial studies of new 2, 3-disubstituted quinazolin-4(3H) ones of 2-[2-(2, 6-dichlorophenyl)amino] phenyl acetic acid
Patel, Navin B.,Shaikh, Asif R.
experimental part, p. 929 - 936 (2010/10/18)
2-[2-(2, 6-Dichlorophenyl)amino]phenylmethyl-3-{4-[(substituted phenyl)amino]-l, 3-oxazol-2-yl}-]-6-bromoquinazo- lin-4(3H)ones 5a-o have been synthesized from the lead molecule 2-[(2, 6-dichlorophenyl)amino]phenyl acetic acid 1, via carboxamide 4. Compound 4 on cyclization with substituted phenyl acetamide a-o gave desired compounds 5a-o. The title compounds have been characterized by elemental analysis, IR, 1H NMR and 13C NMR spectral data. All the compounds have been screened for antibacterial and antifungal activity.
Synthesis and microbial studies of (4-oxo-thiazolidinyl) sulfonamides bearing quinazolin-4(3H)ones
Patel, Navin B.,Patel, Virendra N.,Patel, Hemant R.,Shaikh, Faiyaz M.,Patel, Jaymin C.
scheme or table, p. 267 - 275 (2011/07/30)
2-[(2,6-Dichlorophenyl)amino]phenylacetic acid (A) on reaction with thionyl chloride gave corresponding acid chloride (B). A series of (4-oxo- thiazolidinyl)sulfonamides of quinazolin-4(3H)ones (4a-l) were prepared from Schiff bases (3a-l) of 2-[2-(2,6-di
Synthesis and biological activity of some new 1,3-thiazolyl-6- bromoquinazolin-4(3H)ones
Patel,Patel
scheme or table, p. 1231 - 1236 (2010/08/05)
The title compound 1,3-thiazolyl-6-bromoquinazolin-4(3H)ones 5 i-xv have been synthesized from the molecule 2-[(2,6-dichlorophenyl) amino]phenyl acetic acid 1 through multi-step reaction sequence. The structures of new compounds have been confi
