140134-65-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of (E)-5-styryl-1,2,4-oxadiazoles as anti-tubercular agents
Atmaram Upare, Abhay,Gadekar, Pradip K.,Sivaramakrishnan,Naik, Nishigandha,Khedkar, Vijay M.,Sarkar, Dhiman,Choudhari, Amit,Mohana Roopan
supporting information, p. 507 - 512 (2019/02/19)
Cinnamic acid and its derivatives are known for anti-tubercular activity. The present study reports the synthesis of cinnamic acid derivatives via bioisosteric replacement of terminal carboxylic acid with “oxadiazole”. A series of cinnamic acid derivatives (styryl oxadiazoles) were designed and synthesized in good yields by reaction of substituted cinnamic acids (2, 15a-15s) with amidoximes. The synthesized styryl oxadiazoles were evaluated in vitro for anti-tubercular activity against Mycobacterium tuberculosis (Mtb) H37Ra strain. The structure-activity relationship (SAR) study has identified several compounds with mixed anti-tubercular profiles. The compound 32 displayed potent anti-tubercular activity (IC50 = 0.045 μg/mL). Molecular docking studies on mycobacterial enoyl-ACP reductase enzyme corroborated well with the experimental findings providing a platform for structure based hit-to-lead development.
One-pot synthesis of trans-4-alkylthio- And 4-arylthio-cinnamic acids from trans-4-chlorosulfonylcinnamic acid in an aqueous medium
Zhang, Wensheng,Kuang, Chunxiang,Yang, Qing
experimental part, p. 546 - 548 (2009/04/06)
A one-pot syntheses of trans-4-alkylthio- and 4-arylthio-cinnamic acids were achieved in high yields by reduction of trans-4-chlorosulfonylcinnamic acid with stannous chloride dihydrate followed by alkylation and arylation of the resulting trans-4-thiocinnamic acid with various kinds of alkyl and activated aryl halides in an aqueous medium.
Novel oxidized thioether derivatives
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Page/Page column 21, (2010/02/13)
The present invention provides the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them
Synthetic routes to ninhydrins. Preparation of ninhydrin, 5-methoxyninhydrin, and 5-(methylthio)ninhydrin
Heffner,Joullie
, p. 2231 - 2256 (2007/10/02)
Two syntheses of 5-methoxyninhydrin (2,2-dihydroxy-5-methoxy-1,3-indanedione) are described. One method employs a novel and efficient two step route, which begins with commercially available 6-methoxy-1-indanone. The application of this strategy for the preparation of a new ninhydrin derivative, 5-(methylthio)ninhydrin, and ninhydrin is also presented.
Central cholinergic agents. II. Synthesis and acetylcholinesterase inhibitory activities of N-[ω-[N-alkyl-N-(phenylmethyl)amino]alkyl]-3-arylpropenamides
Ishihara,Kato,Goto
, p. 3236 - 3243 (2007/10/02)
A series of N-[ω-[N-alkyl-N-(phenylmethyl)amino]alkyl]-3-arylpropenamides was prepared and tested for its inhibitory activities on acetylcholinesterase. Some in the series were found to be potent inhibitors. The structure-activity relationships were discussed in detail.
