Structure–activity relationships of tyrosinase inhibitory combinatorial library of 2,5-disubstituted-1,3,4-oxadiazole analogues

Khan, Mahmud Tareq Hassan; Choudhary, M. Iqbal; Khan, Khalid Mohammed; Rani, Mubeen; Atta-ur-Rahman, _

doi:10.1016/j.bmc.2005.03.012

Cited by 177 publications

(43 citation statements)

References 12 publications

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“…1,3,4-Oxadiazoles forms an important class of heterocyclic compounds with broad spectrum of biological activities. Substituted 1,3,4-oxadiazoles have revealed antibacterial 21 , antimycobacterial 22 , antifungal 23 , anti-inflammatory and analgesic [24][25][26] , anticonvulsant 27 , antihyperglycemic 28 , anticancer 29 , anti-HIV-1 30 , and tyrosinase inhibitory activity 31 . 1,2,4-Oxadiazole derivatives have been reported as potent anti-inflammatory agents with selectivity for COX-2 [32][33][34] .…”

Section: Research Articlementioning

confidence: 99%

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

Akhter

Alam

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

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Section: Research Articlementioning

confidence: 99%

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

Akhter

Alam

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Several 1,3,4-oxadiazole derivatives have been shown to possess insecticidal, hypoglycemic, hypotensive, antiviral [4], as well as antitumor activities [5]. Certain 1,3,4-oxadiazoline-2(3H)-thiones are known to possess antibacterial, antifungal, antimicrobial, and antiviral activities [4], as well as tyrosinase-inhibiting effect [6]. Nucleosides and their analogs possess a wide range of medicinal properties, including antibiotic, antiviral, and antitumor activity [7][8][9][10][11][12][13][14][15][16].…”

mentioning

confidence: 99%

Synthesis of novel 1,3,4-oxadiazole derivatives and their nucleoside analogs with antioxidant and antitumor activities

Fadda

Abdel‐Rahman

El‐Sayed³

et al. 2011

Chem Heterocycl Comp

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A series of new (1,3,4-oxadiazol-2-yl)-1H-benzo[h]quinolin-4-one derivatives were synthesized, including glucose and xylose hydrazones that were obtained by the reaction of hydrazides with monosaccharides. Cyclization of the sugar hydrazones with acetic anhydride afforded substituted oxadiazoline derivatives. The newly synthesized compounds were evaluated for their antioxidant properties and cytotoxicity, and showed moderate to high activities.A significant part of drug discovery efforts in the past few years has been focused on prevention or treatment of cancer. This is not surprising because in most developed countries, and to an increasing extent, cancer is among the three most common causes of death. Among the five-membered nitrogen heterocycles, 1,3,4-oxadiazoles are associated with a broad spectrum of biological activities. The 1,3,4-oxadiazole ring has been found in the structures of fungicidal, bactericidal, analgesic, antipyretic, antiphlogistic, anticompulsive, anti-inflammatory, paralytic, hypnotic, and sedative agents [1-3]. Several 1,3,4-oxadiazole derivatives have been shown to possess insecticidal, hypoglycemic, hypotensive, antiviral [4], as well as antitumor activities [5]. Certain 1,3,4-oxadiazoline-2(3H)-thiones are known to possess antibacterial, antifungal, antimicrobial, and antiviral activities [4], as well as tyrosinase-inhibiting effect [6]. Nucleosides and their analogs possess a wide range of medicinal properties, including antibiotic, antiviral, and antitumor activity [7][8][9][10][11][12][13][14][15][16]. Consequently, and considering the possible enhancement of biological activity resulting from the attachment of carbohydrate moieties to 1,3,4-oxadiazole heterocycles, our attention was turned to the synthesis of new 1,3,4-oxadiazole derivatives and their nucleoside analogs [17,18].

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“…1,3,4-oxadiazole is commonly utilized pharmacophore has been subjected to extensive study in the recent years due to their metabolic profile and ability to engage in hydrogen bonding with receptor site. 1,3,4-Oxadiazoles are an important class of heterocyclic compounds with a wide range of biological activities such as antiviral [10], antimicrobial [11], antineoplastic [12], fungicidal [13], anticancer [14,15], inhibition of tyrosinase [16], They are also useful intermediates in organic synthesis [17] and widely employed as electron transporting and hole-blocking materials.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Biologically Potent Chalcone Bearing 1,3,4-Oxadiazole Linkage

Variya¹,

Panchal²,

Bhabhor³

et al. 2015

ILCPA

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ABSTRACT. In this article, we have described to design and synthesized a series of substituted chalcone based 1,3,4-oxadiazole derivatives. Titled compounds (E)-S-(-5-phenyl-1,3,4-oxadiazol-2-yl) 2-(4-(3-(5-methyl-3oxo-2(p-tolyl)-2,3-dihydro-1H-pyrazol-4-yl)-3-oxoprop-1-en-1-yl)phenoxy) etanethioate (III 1-6 ) were synthesized using of derivatives of S-(-5-phenyl-1,3,4 oxadiazole-2-yl)2-chloroethaethioate (I 1-6 ) were reacted with (E)-4-(3-(4-hydroxyphenyl)acryloyl)-5-methyl-2(ptolyl)-1H-pyrazol-3(2H)-one (II) in presence of K 2 CO 3 in DMF as a solvent. The synthesized compounds were evaluated for their antimicrobial activity. The newly synthesized compounds were characterized by analytical and spectral (IR, 1 H NMR, and LC-MS) Methods.

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Structure–activity relationships of tyrosinase inhibitory combinatorial library of 2,5-disubstituted-1,3,4-oxadiazole analogues

Cited by 177 publications

References 12 publications

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

Synthesis of novel 1,3,4-oxadiazole derivatives and their nucleoside analogs with antioxidant and antitumor activities

Synthesis and Characterization of Biologically Potent Chalcone Bearing 1,3,4-Oxadiazole Linkage

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