Therapeutic potential of oxazole scaffold: a patent review (2006–2017)

Kaur, Ramandeep; Palta, Kezia; Kumar, Manoj; Bhargava, Meha; Dahiya, Lalita

doi:10.1080/13543776.2018.1526280

Cited by 39 publications

(30 citation statements)

References 36 publications

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“…Due to its tendency to form Hbonding interaction, it can easily fit into the cavity of varieties of biological receptors and enzymes. [46][47][48][49] It is worth to anchor both quinoline and oxazole cores in a single pharmacophoric unit and to investigate its anticancer potency.…”

Section: Quinoline-oxazole Hybridsmentioning

confidence: 99%

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Panda

Chakroborty

2020

ChemistrySelect

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The emergence of drug resistance and low specificity with side effects are the significant challenges in pharmaceutical sectors for control of cancer nowadays. Notwithstanding, this is an imperative prerequisite to develop novel anticancer agents through mainstream medicinal chemistry approaches. The intriguing quinoline and its derivatives have demonstrated as significant building blocks for the locating of new promising anticancer agents. Consequently, quinoline moiety with the addition of suitable congeners would offer a strategy for the development of potential drug candidates. This present review article summarizes the recent advances (2018‐2020) of quinoline hybrids and their anticancer activity. The mechanism action and plausible structure‐activity relationship have discussed.

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Section: Quinoline-oxazole Hybridsmentioning

confidence: 99%

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Panda

Chakroborty

2020

ChemistrySelect

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“…Oxadiazole moiety is readily able to bind with diverse enzymes and receptors in biological systems through various noncovalent interactions, and thus displays versatile pharmacological profiles including antibacterial activity. [ 106,107 ] Thus, hybridization of indole with oxadiazole may provide valuable therapeutic intervention in bacterial infection.…”

Section: Indole/isatin–azole Hybridsmentioning

confidence: 99%

Indole/isatin‐containing hybrids as potential antibacterial agents

Song

Bian

et al. 2020

Archiv der Pharmazie

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The emergence and worldwide spread of drug-resistant bacteria have already posed a serious threat to human life, creating the urgent need to develop potent and novel antibacterial drug candidates with high efficacy. Indole and isatin (indole-2,3-dione) present a wide structural and mechanistic diversity, so their derivatives possess various pharmacological properties and occupy a salient place in the development of new drugs. Indole/isatin-containing hybrids, which demonstrate a promising activity against a panel of clinically important Gram-positive and Gram-negative bacteria, are privileged scaffolds for the discovery of novel antibacterial candidates. This review, covering articles published between January 2015 and May 2020, focuses on the development and structure-activity relationship (SAR) of indole/isatincontaining hybrids with potential application for fighting bacterial infections, to facilitate further rational design of novel drug candidates.

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“…Oxazole and its derivatives are heterocyclic systems which have gained strong interest in recent times due to their increasing importance in the field of medicinal chemistry [1]. They feature a well-known important doubly unsaturated 5-membered ring heterocyclic motif having one oxygen atom at position 1 and a nitrogen at position 3 separated by a carbon in between [2]. Their widespread useful biological activities including antimicrobial [3], anticancer [4], antitubercular [5], anti-inflammatory [6], antidiabetic [7], antiobesity [8] and anthelminthic [9] effects have attracted increasing attention of chemical and pharmacological communities in their search for new lead compounds [1].…”

Section: Introductionmentioning

confidence: 99%

“…Their widespread useful biological activities including antimicrobial [3], anticancer [4], antitubercular [5], anti-inflammatory [6], antidiabetic [7], antiobesity [8] and anthelminthic [9] effects have attracted increasing attention of chemical and pharmacological communities in their search for new lead compounds [1]. Some of them have shown promising therapeutic potential and have qualified for both preclinical and clinical evaluations [2]. Previous studies reported the isolation of several biologically active substituted oxazole-containing natural products mostly from marine invertebrates and microorganisms [2,10,11].…”

Section: Introductionmentioning

confidence: 99%

“…Some of them have shown promising therapeutic potential and have qualified for both preclinical and clinical evaluations [2]. Previous studies reported the isolation of several biologically active substituted oxazole-containing natural products mostly from marine invertebrates and microorganisms [2,10,11]. For instance, hennoxazole A, isolated from a marine sponge Polyfibrospongia sp., was reported to possess antiviral activity [12,13] while the phthoxazolins isolated from Streptomyces sp.…”

Section: Introductionmentioning

confidence: 99%

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Macrooxazoles A–D, New 2,5-Disubstituted Oxazole-4-Carboxylic Acid Derivatives from the Plant Pathogenic Fungus Phoma macrostoma

et al. 2020

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In our ongoing search for new bioactive fungal metabolites, four previously undescribed oxazole carboxylic acid derivatives (1–4) for which we proposed the trivial names macrooxazoles A–D together with two known tetramic acids (5–6) were isolated from the plant pathogenic fungus Phoma macrostoma. Their structures were elucidated based on high-resolution mass spectrometry (HR-MS) and nuclear magnetic resonance (NMR) spectroscopy. The hitherto unclear structure of macrocidin Z (6) was also confirmed by its first total synthesis. The isolated compounds were evaluated for their antimicrobial activities against a panel of bacteria and fungi. Cytotoxic and anti-biofilm activities of the isolates are also reported herein. The new compound 3 exhibited weak-to-moderate antimicrobial activity as well as the known macrocidins 5 and 6. Only the mixture of compounds 2 and 4 (ratio 1:2) showed weak cytotoxic activity against the tested cancer cell lines with an IC50 of 23 µg/mL. Moreover, the new compounds 2 and 3, as well as the known compounds 5 and 6, interfered with the biofilm formation of Staphylococcus aureus, inhibiting 65%, 75%, 79%, and 76% of biofilm at 250 µg/mL, respectively. Compounds 5 and 6 also exhibited moderate activity against S. aureus preformed biofilm with the highest inhibition percentage of 75% and 73% at 250 µg/mL, respectively.

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Therapeutic potential of oxazole scaffold: a patent review (2006–2017)

Cited by 39 publications

References 36 publications

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Indole/isatin‐containing hybrids as potential antibacterial agents

Macrooxazoles A–D, New 2,5-Disubstituted Oxazole-4-Carboxylic Acid Derivatives from the Plant Pathogenic Fungus Phoma macrostoma

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