19551-59-8Relevant academic research and scientific papers
Novel Synthesis of Thioguanine and Sulfanylpurine Analogues: Reaction of Heterocyclic Ketene Dithioacetals with Nucleophiles
Elgemeie, Galal H.,Elghandour, Ahmed H.,Elzanate, Ali M.,Ahmed, Sayed A.
, p. 162 - 163 (1998)
A novel synthesis of thioguanine and sulfanylpurine analogues via the reaction of heterocyclic ketone dithioacetals with nucleophiles is reported and the synthetic potential of the method is demonstrated.
Structure-activity relationships of pyrazole-4-carbodithioates as antibacterials against methicillin–resistant Staphylococcus aureus
Majed, Hiwa,Johnston, Tatiana,Kelso, Celine,Monachino, Enrico,Jergic, Slobodan,Dixon, Nicholas E.,Mylonakis, Eleftherios,Kelso, Michael J.
supporting information, p. 3526 - 3528 (2018/10/15)
Methicillin-resistant Staphylococcus aureus (MRSA) is a major cause of serious hospital-acquired infections and is responsible for significant morbidity and mortality in residential care facilities. New agents against MRSA are needed to combat rising resistance to current antibiotics. We recently reported 5-hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbodithioate (HMPC) as a new bacteriostatic agent against MRSA that appears to act via a novel mechanism. Here, twenty nine analogs of HMPC were synthesized, their anti-MRSA structure-activity relationships evaluated and selectivity versus human HKC-8 cells determined. Minimum inhibitory concentrations (MIC) ranged from 0.5 to 64 μg/mL and up to 16-fold selectivity was achieved. The 4-carbodithioate function was found to be essential for activity but non-specific reactivity was ruled out as a contributor to antibacterial action. The study supports further work aimed at elucidating the molecular targets of this interesting new class of anti-MRSA agents.
Synthesis, biological evaluation and molecular modeling study of pyrazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents
Tewari, Ashish Kumar,Singh, Ved Prakash,Yadav, Pratima,Gupta, Garima,Singh, Amit,Goel, Raj Kumar,Shinde, Pravin,Mohan, C. Gopi
, p. 8 - 15 (2014/06/23)
A novel series of pyrazole derivatives were synthesized and evaluated in vivo for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Among all compounds, 5a, and 5b showed comparable anti-inflammatory activity to Nimesulide, the
Synthesis, spectral, crystal and theoretical studies of some novel 4-heterocyclic substituted pyrazolones
Narayanan, Kuppusamy,Shanmugam, Mani,Vasuki, Gnanasambandam,Kabilan, Senthamaraikannan
, p. 70 - 78 (2013/11/19)
Reactions of pyrazolone ketene dithioacetals with various binucleophiles afforded 4-heterocyclic substituted pyrazolone compounds as ketene N,N-, N,O-acetals in the absence of any acid/base catalyst in good yields. The products 3a-i formed by the direct d
Synthesis of pyrazole-based 1,5-diaryl compounds as potent anti-inflammatory agents
Shrivastava, Priyanka,Singh, Praveen,Tewari, Ashish Kumar
, p. 2465 - 2475 (2012/11/06)
Series of 1,5-diaryl pyrazole ester derivatives have been synthesized and found to contain potent inhibitory activity against cyclooxygenase-2 (COX-2) enzyme. The article describes synthesis of the target pyrazole analogs and biological assay using Carrag
Novel anti-inflammatory agents based on pyrazole based dimeric compounds; design, synthesis, docking and in vivo activity
Tewari, Ashish Kumar,Srivastava, Priyanka,Singh, Ved Prakash,Singh, Amit,Goel, Raj Kumar,Mohan, Chethampadi Gopi
scheme or table, p. 634 - 638 (2010/08/19)
Series of pyrazole ester prodrugs analogues have been synthesized and found to contain highly potent inhibitors of the cyclooxygenase-2 (COX-2) enzyme. The paper describes synthesis of the target pyrazole analogues. The structure of the synthesized mutual
Applications of dithioacetals in ester synthesis
Tewari, Ashish Kumar,Srivastava, Priyanka
experimental part, p. 2837 - 2842 (2009/12/03)
The α-oxoketene dithioacetals are simple synthetic intermediates widely utilized and implicated for the synthesis of a variety of heterocyclic compounds other than alicyclic and aromatic compounds. They act as 1,3-electrophilic three-carbon synthons. The
Synthesis of heteroarylidene derivatives of 2-aryl-2,4-dihydro-5-methyl-3H-pyrazol-3-one and barbituric acid as possible nonsteroidal contraceptives
Ram, Vishnu,Verma, Monika
, p. 1119 - 1123 (2007/10/02)
Several 2,3-dihydro-1H-benzimidazol-2-ylidene, 2,3-dihydrobenzoxazol-2-ylidene, 5,6-dihydro-7H-1,2,4-triazolo-1,2,4-triazol-6-ylidene derivatives of 2-aryl-2,4-dihydro-5-methyl-3H-pyrazol-3-one (3a-h, 4, 5a,b) and barbituric acid (8, 9a-d) have bee
