Synthesis and antimicrobial activity of new (E)-4-[piperidino (4'-methylpiperidino-, morpholino-) N-alkoxy]stilbenes

Wyrzykiewicz, E.; Wendzonka, Monika; Kędzia, Bogdan

doi:10.1016/j.ejmech.2005.11.010

Cited by 29 publications

(22 citation statements)

References 23 publications

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“…Therefore, it is an urgent need to design and develop new anti-AIDS drugs with improved potency to halt the spread of HIV. Among the non-nucleoside reverse transcriptase inhibitors, diarylpyrimidine (DAPY) derivatives such as dapivirine (67), etravirine (68) and rilpivirine (69) and diaryltriazine (70) [99,100] with superior activity profiles against HIV-1 have attracted considerable attention over the past few years (Fig. 30).…”

Section: Antiviral Activitymentioning

confidence: 99%

Triazine as a promising scaffold for its versatile biological behavior

Singla

Luxami

Paul

2015

European Journal of Medicinal Chemistry

114

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Section: Antiviral Activitymentioning

confidence: 99%

Triazine as a promising scaffold for its versatile biological behavior

Singla

Luxami

Paul

2015

European Journal of Medicinal Chemistry

114

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“…Another important pharmacophore group is the morpholine nucleus incorporated in a wide variety of therapeutically important drugs, one of which is linezolid which belongs to the oxazolidinone class of antibiotics and is used for the treatment of infections caused by gram-positive bacteria (Wyrzykiewicz et al ., 2006; Dixit et al ., 2005; Raparti et al ., 2009; Bektas et al ., 2010, 2012; Bayrak et al ., 2009a, b). In addition, 4-phenylmorpholine derivatives have been reported to possess antimicrobial, anti-inflammatory, and central nervous system activities (Dixit et al ., 2006), Oxazolidinones are a relatively new class of synthetic antibacterial agents, having a new mechanism of action that involves early inhibition of bacterial protein synthesis.…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial and antiurease activities of newly synthesized morpholine derivatives containing an azole nucleus

et al. 2012

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2-[6-(Morpholin-4-yl)pyridin-3-ylamino]acetohydrazide (4) was obtained starting from 6-morpholin-4-ylpyridin-3-amine (2) via the formation of ester (3) and then converted to the corresponding Schiff bases (5, 6) with the reaction with aromatic aldehydes. The carbothioamide (9), obtained from the reaction of hydrazide with phenylisothiocyanate, was converted to the corresponding 1,2,4-triazole (11) and 1,3,4-thiadiazole (12) derivatives by the treatment with NaOH or H2SO4, respectively. The cyclocondenzation of 9 with 4-chlorophenacyl bromide or ethyl bromoacetate produced the corresponding 1,3-thiazole (10) or 1,3-thiazolidine derivatives (13), respectively. Antimicrobial and antiurease activities of newly synthesized compounds were investigated. Some of them were found to be active on M. smegmatis, and they displayed activity toward C. albicans and S. cerevisiae in high concentration. Compound 10 proved to be the most potent showing an enzyme inhibition activity with an IC50 = 2.37 ± 0.19 μM.

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“…Morpholine nucleus is an integral part of linezolid, a clinically used drug for the treatment of infections caused by gram-positive bacteria [16]. A number of morpholine containing chemical compounds have also been reported as antimicrobial agents [17][18][19][20][21][22]. Encouraged by these observations and also in continuation of our search for potent antimicrobial agents [23,24] including antimicrobial agents having coumarin moiety [25,26], we decided to prepare some 2-morpholinomethylamino-4-(7-unsubstituted/substitutedcoumarin-3-yl)-6-chlorosubstitutedphenyl pyrimidines, herein after the title compounds (1a-18a), as antimicrobial agents.…”

Section: Introductionmentioning

confidence: 99%