Antimicrobials. 3. Benzothiazolylphenylalkylamines

Palmer, P. J.; Trigg, Richard; Warrington, J. V.

doi:10.1021/jm00294a026

Cited by 4 publications

(3 citation statements)

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“…Synthesis and characterization of the following starting materials and intermediate bromoacetylphenyl derivatives, trans -2-methylamino-cyclohexanol, 2-(4-acetylphenyl)thiophene ( 23 ), , 2-(4-bromoacetylphenyl)thiophene ( 24 ), 2-bromo-5-(4-bromoacetylphenyl)thiophene ( 25 ), 2-(acetylphenyl)benzothiazole ( 26 ), 2-(4-bromoacetylphenyl)benzothiazole ( 27 ), 4-(2′-fluorophenyl)acetophenone ( 28 ), 4-(4′-fluorophenyl)acetophenone ( 29 ), 4-(4′-chlorophenyl)acetophenone ( 30 ), 4-(2′-fluorophenyl)-bromoacetophenone ( 31 ), 4-(4′-fluorophenyl)bromoacetophenone ( 32 ), 4-(4′-chlorophenyl)-bromoacetophenone ( 33 ), and 4-(4′-bromophenyl)-bromoacetophenone ( 34 ) are reported in Supporting Information.…”

Section: Methodsmentioning

confidence: 99%

Lipid-Lowering (Hetero)Aromatic Tetrahydro-1,4-Oxazine Derivatives with Antioxidant and Squalene Synthase Inhibitory Activity

et al. 2008

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A number of newly synthesized 2-[4-(hetero)aromatic]phenyl-2-hydroxy-tetrahydro-1,4-oxazine derivatives were found to inhibit lipid peroxidation (IC50 of the most potent was 20 microM) as well as rat squalene synthase (IC50 for most between 1-10 microM). Antidyslipidemic action was demonstrated in vivo: the most active compound decreased triglycerides, total cholesterol, and LDL-cholesterol of hyperlipidemic rats by 64, 67, and 82%, respectively, at 56 micromol/kg (ip). Most of the novel compounds are more active than the structurally related and reference biphenyl-morpholine, pointing to useful structural approaches for the design of antiatherosclerotic agents.

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Section: Methodsmentioning

confidence: 99%

Lipid-Lowering (Hetero)Aromatic Tetrahydro-1,4-Oxazine Derivatives with Antioxidant and Squalene Synthase Inhibitory Activity

et al. 2008

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“…Moreover, the BT moiety is also found in many functional molecules, such as ratiometric fluorescent pH indicators and ligands for catalytic reactions [18,19]. Since 1991, BT has been a moiety known to play an important role in chemistry, biochemistry, and medicinal chemistry, with a wide array of interesting biological activities and therapeutic functions, such as antimicrobial [20][21][22][23], anticancer [24][25][26][27][28][29], anthelmintic [30], antidiabetic [31,32], antituberculotic [33,34], antitumor [35][36][37][38][39][40][41], antitrypanosomal [42], antiviral [43][44][45], antibacterial [46][47][48][49], antioxidant [50], antiglutamate and antiparkinsonism [51,52], analgesic [53], anti-inflammatory [54,55], antifungal [56,57], antileishmanial [58], anticonvulsant [59], neuroprotective [60], muscle relaxant [61], vasodilator…”

Section: Introductionmentioning

confidence: 99%

Benzothiazoles from Condensation of o-Aminothiophenoles with Carboxylic Acids and Their Derivatives: A Review

et al. 2021

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Nowadays, organic chemists are interested in the field of heterocyclic chemistry due to its use in the synthesis of a great variety of biologically active compounds. Heterocyclic compounds are widely found in nature and are essential for life. Among these, some natural nitrogen containing heterocyclic compounds have been used as chemotherapeutic agents. Their attachment to sugar molecules either as thioglycosides or as nucleosides analogues plays an important role in vital biological processes as well as in synthetic organic chemistry. Molecules containing benzothiazole (BT) nuclei are of this interesting class of compounds because some of them have been found to have a wide variety of biological activities. In this sense, we selected this topic to review and to then summarize the procedures related to the condensation reactions of o-aminothiophenoles (ATPs) as well as their disulfides with carboxylic acids, esters, orthoesters, acyl chlorides, amides, and nitriles. The condensation reactions with carbon dioxide (CO2) are included. Conventional methods with the use of acid and metal catalysts as well as recent green techniques, such as microwave irradiation, the use of ionic liquids, and ultrasound (US) chemistry, which have proven to have many advantages, were found in the review.

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“…1). 6 The benzothiazole moiety plays an important role in chemistry and is also present in a variety of biologically active applications such as anti-microbial, [7][8][9][10] anti-cancer, [11][12][13][14][15][16] anthelmintic, 17 anti-diabetic, 18,19 anti-tuberculotic, 13,20,21 antitumor, [22][23][24][25][26][27][28] anti-trypanosomal, 29 anti-viral, [30][31][32] antibacterial, [33][34][35][36] anti-oxidant, 37 anti-glutamate and anti-parkinsonism, 38,39 analgesic, 40 anti-inammatory, [41][42][43] antifungal, 44,45 antileishmanial, 46 anticonvulsant, 47 neuroprotective, 48 muscle relaxant activities, 49 vasodilator, 50 orexin receptor,…”

Section: Introductionmentioning

confidence: 99%