Synthesis and Biological Activity of novel 3-(1-chloropiperidin-4-yl)-6-fluoro benzisoxazole
نویسندگان
چکیده
A synthèsis of novel 3-(1-chloropiperidin-4-yl)-6-fluoro benzisoxazole was carried out under mild réaction conditions using 1.2 équivalents of calcium hypochlorite. Interestingly, the developed method does not involve any additives like acids or bases and provides 96% of isolated yields at room temperature. This novel molécule, 3-(1-chloropiperidin-4-yl)-6-fluorobenzisoxazole 2 was stable at ambient conditions and stereo chemistry was established the single crystal XRD technique. Compound 2 was exhibited potent antioxidant activity (107 μg/mL), and also shown their inhibition on diabetes causing enzymes such as alpha amylase (270 μg/mL) and alpha glucosidase (37 μg/mL).
منابع مشابه
Novel Linezolid like Analogues: Synthesis, Characterization and Biological Evaluation
The synthesis of 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4H)-one was achieved in two steps, In first step, pyrazine-2-carboxamide dissolved in EtOH, 10% KOH solution with ClCH2COOH produced compound 2-(pyrazine-2-carboxamido) acetic acid (II) and in second step, compound (II) in (CH3CO)2O with aromatic aldehyde, and catalyst potassium ace...
متن کاملSynthesis and in-vitro antibacterial activity of some novel N-nicotinoyl-1-ethyl-6-fluoro-1,4-dihydro-7-piperazin-1-yl-4-oxoquinoline-3-carboxylates.
A series of N-nicotinoyl-1-ethyl-6-fluoro-1,4-dihydro-7-piperazin-1-yl-4-oxoquinoline-3-carboxylates has been synthesized and evaluated for antibacterial activity. Norfloxacin was reacted with thionyl chloride, to yield norfloxacin acid chloride which was used immediately in next step by reacting with respective alcohols to furnish the corresponding esters i.e. 1-ethyl-6-fluoro-1,4-dihydro-7-pi...
متن کاملA rational approach for synthesis, characterization and antihypertensive activity evaluation of 1-(4-{5-amino-6-fluoro-1-[2'-(2H-tetrazole-5-yl)- biphenyl-4-ylmethyl]-1H-benzoimidazol-2-yl}-phenyl)-3-chloro-4- (substituted -phenyl)-azetidin-2-ones
A new series of 1-(4-{5-Amino-6-fluoro-1-[2'-(2H-tetrazole-5-yl)-biphenyl-4-ylmethyl]-1Hbenzoimidazol-2-yl}-phenyl)-3-chloro-4-(Substituted -phenyl)-azetidin-2-one derivatives MCS 06[1-15] has been synthesized and subjected to evaluate their antihypertensive activity. All the synthesized compounds of the series elicit remarkable activity in comparison to standard drug (Losartan). Structures of ...
متن کاملSynthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity
In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...
متن کاملSynthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity
In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...
متن کامل