- Synthesis, in-vitroreverse transcriptase inhibitory activity and docking study of some new imidazol-5-one analogs
-
Non-nucleoside reverse transcriptase inhibitors have a definitive role and most commonly used in treatment of HIV-1 infection. A new series of 4-ethylidene/substituted-benzylidene-1-(4-hydroxy/chloro-6-methylpyrimidin-2-yl) -2-ethyl/phenyl-1H-imidazol-5(4H)-one were designed, synthesized, and evaluated for HIV-1 reverse transcriptase (RT) inhibitory activity. The results of in-vitro HIV-1 RT assay showed that some of the new compounds, such as 4c, 4d, 4e, 5a, and 5e effectively inhibit HIV-1 RT activity. 1-(4-Chloro-6- methylpyrimidin-2-yl)-4-(furan-2-ylmethylene)-2-methyl-1H-imidazol-5(4H)-one (5e) exerted most potent in-vitro HIV-1 RT inhibitory activity, among the group of compounds. Molecular docking studies were carried out to explore the binding affinity of imidazole-5-one analogs in active site of HIV-1 RT enzyme. Springer Science+Business Media 2014.
- Mokale, Santosh N.,Lokwani, Deepak K.,Shinde, Devanand B.
-
p. 3752 - 3764
(2014/08/05)
-
- Microwave-assisted synthesis and antimicrobial screening of new imidazole derivatives bearing 4-thiazolidinone nucleus
-
A new series of compounds 2-((1-(4-(4-arylidene-2-methyl-5-oxo-4,5-dihydro- 1H-imidazol-1-yl)phenyl)ethylidene)hydrazono)thiazolidin-4-ones (4a-o) have been synthesized under conventional and microwave irradiation method. All compounds were characterized by IR, 1H NMR, 13C NMR and mass spectra. Newly synthesized compounds were screened for their antibacterial and antifungal activities on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogenes, Candida albicans, Aspergillus niger and Aspergillus clavatus by bioassays, namely serial broth dilution. The synthesized compounds showed potent antimicrobial activity against tested microorganisms. Compounds 4h, 4j, 4m and 4n were the most potent amongst tested compounds.
- Desai,Joshi,Rajpara,Vaghani,Satodiya
-
p. 1893 - 1908
(2013/07/26)
-
- Synthesis, biological activity and docking study of imidazol-5-one as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
-
A novel series of substituted imidazol-5-ones were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) inhibition activity using reverse transcriptase assay kit (Roche, Colorimetric). It has been observed from in vitro screening that newly synthesized compounds possess RT inhibitory activity. Docking study was performed to study the binding orientation and affinity of synthesized compounds for RT enzyme.
- Mokale, Santosh N.,Lokwani, Deepak,Shinde, Devanand B.
-
experimental part
p. 3119 - 3127
(2012/06/29)
-
- Synthesis of substituted quinazolone derivatives as potential anti-HIV agents (part III)
-
Several 1-[2-phenyl-4(4H)-oxo-3-quinazolinyl]-2-methyl-4-arylidine -5-oxo-imidazolines (Va-1), 2-phenyl-3-(aroyl amino)-4(4H)-oxo quinazolines (Vla-I) and N1-2-methyl-4(4H)-oxo-3-quinazolinyl-N2-aryl-thioureas (Vlla-k), have been synthesised and tested for anti-HIV activity. The structures of these compounds have been established on the basis of elemental analysis and spectral data.
- Desai,Bhatt,Shah,Undavia,Trivedi,Narayanan
-
p. 361 - 366
(2007/10/03)
-
- Synthesis of some new 2-methyl-4-(substituted benzylidene) 1-phenyl-1,2,4 triazolo [3,4,-b] 1,3,4 thiadiazole as potential AChE inhibitory agents
-
4-(1-aminophenyl) -1,2,4 - triazolo [3,4,-b] 1,3,4-thiadiozole (2) was prepared by treatment of 4-(1-aminophenyl)-5-mercapto-4-amino-1,2,4-S-triazole with carbondisulfide and KOH in methanol. This on further reaction with different 2-methyl-4-(substituted
- Sen,Shanker
-
p. 465 - 467
(2007/10/03)
-