74169-00-9Relevant academic research and scientific papers
Construction of Chiral-Fused Tricyclic γ-Lactams via a trans-Perhydroindolic Acid-Catalyzed Asymmetric Domino Reaction
An, Qianjin,Shen, Jiefeng,Liu, Delong,Liu, Yangang,Zhang, Wanbin
supporting information, p. 2925 - 2928 (2017/06/07)
An asymmetric domino reaction was developed utilizing readily available cyclic α-dehydroamino ketones and aldehydes, which when subjected a 2-iodoxybenzoic acid (IBX)-mediated oxidation gives pyrrolidinone-containing tricyclic derivatives. trans-Perhydroi
Synthesis, in-vitroreverse transcriptase inhibitory activity and docking study of some new imidazol-5-one analogs
Mokale, Santosh N.,Lokwani, Deepak K.,Shinde, Devanand B.
, p. 3752 - 3764 (2014/08/05)
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.
Asymmetric synthesis of unnatural amino acids and tamsulosin chiral intermediate
Arava, Veera Reddy,Amasa, Srinivasulu Reddy,Goud Bhatthula, Bharat Kumar,Kompella, Laxmi Srinivas,Matta, Venkata Prasad,Subha
supporting information, p. 2892 - 2897 (2013/09/02)
An efficient and enantioselective hydrogenation of N-acetylamino phenyl acrylic acids was successfully developed by using ruthenium catalyst. This methodology is important in the field of pharmaceuticals and provides a new process for the preparation of unnatural amino acids and tamsulosin chiral intermediate.
Synthesis, biological activity and docking study of imidazol-5-one as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
Mokale, Santosh N.,Lokwani, Deepak,Shinde, Devanand B.
experimental part, p. 3119 - 3127 (2012/06/29)
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.
Synthesis and antimicrobial studies of thiazolotriazinones
Karthikeyan, Mari Sithambaram
scheme or table, p. 5039 - 5043 (2010/11/19)
A series of 6-substitutedphenyl thiazolo-1,2,4-triazinones (8) were obtained by the initial reaction of 6-substituted arylmethyl-3-mercapto-1,2,4- triazin-5-ones (5) with substituted phenacyl bromides (6) and further followed by PPA cyclization. The struc
Synthesis and antimicrobial evaluation of halogen-containing arylidene thiazolo triazinediones
Karthikeyan, Mari Sithambaram,Mahalinga, Manjathuru,Karegoundar, Prakash,Poojary, Boja,Holla, Bantwal Shivarama
scheme or table, p. 3231 - 3240 (2010/05/02)
A series of 7-substituted arylidene-1,3-thiazolo[2,3-c]-1,2,4-triazine-4,6- diones were synthesized in an one-pot multicomponent reaction of 6-arylmethyl-3-mercapto-1,2,4-triazin-5-ones with substituted benzaldehydes and monochloroacetic acid in the presence of acetic anhydride, acetic acid, and sodium acetate. The structures of the new compounds were supported by IR, 1H NMR, MS, and analytical data. All the new compounds were tested for their antibacterial and antifungal activity. Arylidene thiazolo triazinediones with 1,3-benzodioxolo substituent at seventh and p-chlorophenyl or 2,4-dichlorophenyl substituents at third displayed good antibacterial and antifungal activity. And also compound bearing 2,3,5-trimethoxyphenyl substituent at seventh and 2,4-dichlorophenyl substituent at third displayed good activity.
A novel three-component synthesis of triazinothiazolones
Holla, Bantval Shivarama,Malini, Kani Veetil,Sarojini, Balladka Kunhanna,Poojary, Boja
, p. 333 - 340 (2007/10/03)
A series of 4-arylidene-2-methyloxazol-5-ones 1 were condensed with thiosemi-carbazide to yield 6-arylmethyl-3-mercapto-1,2,4-triazin-5-ones 2. The resulting mercapto triazinones 2 were condensed with monochloroacetic acid and 5-aryl-furan-2-carboxaldehydes 3 in a one-pot three-component reaction in the presence of acetic anhydride, acetic acid, and sodium acetate to yield 4-substituted-5-oxo-7-(5-aryl-2-furfurylidene)-1,2,4-triazino[3,4-b] -thiazol-6-ones 4. Some of the newly synthesized compounds were tested for their antibacterial activity against Gram (+)ve and Gram (-)ve bacteria. The results of such studies are discussed in this paper. Copyright Taylor & Francis, Inc.
