The utility of oxazole as intermediates for the synthesis of new chemical entities in medicinal chemistry have been increased in the past few years. Oxazole is an important heterocyclic nucleus ...having a wide spectrum of biological activities which drew the attention of researchers round the globe to synthesize various oxazole derivatives and screen them for their various biological activities. The present review article aims to review the work reported on therapeutic potentials of oxazole scaffolds which are valuable for medical applications during new millennium.
Cancer is one of the most serious medical problem and second leading cause of death in the world, characterized by a deregulation of the cell cycle which mainly results in a progressive loss of ...cellular differentiation and uncontrolled cellular growth. The benzimidazole is a heterocyclic moiety found in extensive number of natural and biological active molecules. Benzimidazole derivatives might be considered as auxiliary isosters of nucleotides having attached heterocyclic cores in their structures, cooperate effortlessly with biopolymers and have potential action for chemotherapeutic applications. Benzimidazole and its derivatives displayed a wide range of biological activity because of its structural similarity with the naturally occurring nucleotides. Benzimidazole has established huge alertness in current time and is extremely significant heterocyclic pharmacophore in recent drug innovation and medicinal chemistry. The present review summarizes the chemistry of various substituted benzimidazole derivatives with their antiproliferative significance towards the various cancer cell lines such as HCT116, MCF7, HeLa, HepG2, A549 and A431.
The detection of pathogens in food substances is of crucial concern for public health and for the safety of the natural environment. Nanomaterials, with their high sensitivity and selectivity have an ...edge over conventional organic dyes in fluorescent-based detection methods. Advances in microfluidic technology in biosensors have taken place to meet the user criteria of sensitive, inexpensive, user-friendly, and quick detection. In this review, we have summarized the use of fluorescence-based nanomaterials and the latest research approaches towards integrated biosensors, including microsystems containing fluorescence-based detection, various model systems with nano materials, DNA probes, and antibodies. Paper-based lateral-flow test strips and microchips as well as the most-used trapping components are also reviewed, and the possibility of their performance in portable devices evaluated. We also present a current market-available portable system which was developed for food screening and highlight the future direction for the development of fluorescence-based systems for on-site detection and stratification of common foodborne pathogens.
Background
Triazole is an important heterocyclic moiety that occupies a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms ...i.e. 1,2,4-triazole and 1,2,3-triazole and is used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, anti-
urease
, anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic and antimigraine agents.
Methods
The structures of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (
B. subtilis
), Gram-negative (
P. aeruginosa
and
E. coli
) bacterial and fungal (
C. albicans
and
A. niger
) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-
urease
screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU as standards.
Results, discussion and conclusion
The biological screening results reveal that the compounds
T
5
(MIC
BS
,
EC
= 24.7 µM, MIC
PA
,
CA
= 12.3 µM) and
T
17
(MIC
AN
= 27.1 µM) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MIC
Cipro
= 18.1 µM, MIC
Amo
= 17.1 µM) and fluconazole (MIC
Flu
= 20.4 µM), respectively. The antioxidant evaluation showed that compounds
T
2
(IC
50
= 34.83 µg/ml) and
T
3
(IC
50
= 34.38 µg/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC
50
= 35.44 µg/ml). Compounds
T
3
(IC
50
= 54.01 µg/ml) was the most potent
urease
inhibitor amongst the synthesized compounds and compared to standard thiourea (IC
50
= 54.25 µg/ml). The most potent anticancer activity was shown by compounds
T
2
(IC
50
= 3.84 μM) and
T
7
(IC
50
= 3.25 μM) against HCT116 cell lines as compared to standard 5-FU (IC
50
= 25.36 μM).
Background
A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities.
Results and discussion
The synthesized benzoxazole ...compounds were confirmed by IR,
1
H/
13
C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium:
Bacillus subtilis
, four Gram-negative bacteria:
Escherichia coli
,
Pseudomonas aeruginosa
,
Klebsiella pneumoniae
,
Salmonella typhi
and two fungal strains:
Candida albicans
and
Aspergillus niger
using tube dilution technique and minimum inhibitory concentration (MIC) was noted in µM and compared to ofloxacin and fluconazole. Human colorectal carcinoma (HCT116) cancer cell line was used for the determination of in vitro anticancer activity (IC
50
value) by Sulforhodamine B assay using 5-fluorouracil as standard drug.
Conclusion
The performed study indicated that the compounds
1
,
10
,
13
,
16
,
19
,
20
and
24
had highest antimicrobial activity with MIC values comparable to ofloxacin and fluconazole and compounds
4
,
6
,
25
and
26
had best anticancer activity in comparison to 5-fluorouracil.
Bioreceptor functionalized metallic nano-colloids have been identified as effective nanobioprobes to realize the detection of an analyte based on a common phenomenon of salt-induced aggregation. In ...marked contrast to this, we describe a nano-sandwich assay integrating the novel match-pair of aptamer and peptide functionalized gold nanoparticles. The site-directed biomolecular interaction of high affinity aptamer and peptide bioreceptors directed towards distinct sites of cardiac biomarker troponin I; this was found to form a nano-sandwich assay in a peculiar manner. The gold nanoconjugates interact with specific and distant regions of troponin I to result in collision of probes upon target identification. In the presence of TnI, both nanobioprobes bind at their respective sites forming a nano-sandwich pair providing a visual color change from red to blue. Thus, the presence of target TnI itself causes instant agglomeration in just a single-step without addition of any external aggregator. The assay imparts 100% specificity and 90% sensitivity in a dynamic concentration range of 0.1–500 ng/mL troponin I with detection limit as low as 0.084 ng/mL. The applicability of the assay has been validated in clinical samples of acute myocardial infarction patients thus establishing a promising point-of-care detection of TnI.
Graphical abstract
Nyctanthes arbour-tristis belongs to the Oleaceae family and is known as Harsingar. Harsingar is an important Indian medicinal plant; traditionally, harsingar is used to treat skin diseases including ...piles and scalp itching infections, and used as a laxative, diaphoretic, and in chronic fever. N. arbour-tristis microscopic and powder microscopy revealed the presence of stomates, gland cells, vein islet, and trichome. Carbohydrates, amino acids, steroids, coumarin glycoside, flavonoids, alkaloids, and tannins were discovered in preliminary phytochemical analysis. All of the studies were carried out in accordance with WHO guidelines. Quantitative analysis of N. arbour-tristis was done through total phenolic content, total flavonoid content, and total tannin content. Leaves of N. arbortristis were screened for antimicrobial potential against S. typhi, S. aureus, B. subtilis, E. coli by using the MIC method, and chloramphenicol was taken as standard. Among all extract, N. arbour-tristis chloroform extract shows maximum antimicrobial potential.
Alzheimer’s disease (AD) is a multifarious and developing neurodegenerative disorder. The treatment of AD is still a challenge and availability of drug therapy on the basis of symptoms is not up to ...the mark. In the context of existence, which is getting worse for the human brain, it is necessary to take care of all critical measures. The disease is caused due to multidirectional pathology of the body, which demands the multi-target-directed ligand (MTDL) approach. This gives hope for new drugs for AD, summarized here in with the pyrimidine based natural product inspired molecule as a lead. The review is sufficient in providing a list of chemical ingredients of the plant to cure AD and screen them against various potential targets of AD. The synthesis of a highly functionalized scaffold in one step in a single pot without isolating the intermediate is a challenging task. In few examples, we have highlighted the importance of this kind of reaction, generally known as multi-component reaction. Multi-component is a widely accepted technique by the drug discovery people due to its high atom economy. It reduces multi-step process to a one-step process, therefore the compounds library can be made in minimum time and cost. This review has highlighted the importance of multicomponent reactions by giving the example of active scaffolds of pyrimidine/fused pyrimidines. This would bring importance to the fast as well as smart synthesis of bio-relevant molecules.
Honokiol is a neolignan biphenol found in aerial parts of the Magnolia plant species. The Magnolia plant species traditionally belong to China and have been used for centuries to treat many ...pathological conditions. Honokiol mitigates the severity of several pathological conditions and has the potential to work as an anti-inflammatory, anti-angiogenic, anticancer, antioxidant, and neurotherapeutic agent. It has a long history of being employed in the healthcare practices of Southeast Asia, but in recent years, a greater scope of research has been conducted on it. Plenty of experimental evidence suggests it could be beneficial as a neuroprotective bioactive molecule. Honokiol has several pharmacological effects, leading to its exploration as a potential therapy for neurological diseases (NDs), including Alzheimer's disease (AD), Parkinson's disease (PD), cerebral ischemia, anxiety, depression, spinal cord injury, and so on. So, based on the previous experimentation reports, our goal is to discuss the neuroprotective properties of honokiol. Besides, honokiol derivatives have been highlighted recently as possible therapeutic options for NDs. So, this review focuses on honokiol's neurotherapeutic actions and toxicological profile to determine their safety and potential use in neurotherapeutics. Keywords: Honokiol, Chinese Herb, Magnolia species, Neurological diseases, Alzheimer's disease, Parkinson's disease, Ischemia, Anxiety, Depression
Background
In view of wide range of biological activities of oxazole, a new series of oxazole analogues was synthesized and its chemical structures were confirmed by spectral data (Proton/Carbon-NMR, ...IR, MS etc.). The synthesized oxazole derivatives were screened for their antimicrobial and antiproliferative activities.
Results and discussion
The antimicrobial activity was performed against selected fungal and bacterial strains using tube dilution method. The antiproliferative potential was evaluated against human colorectal carcinoma (HCT116) and oestrogen- positive human breast carcinoma (MCF7) cancer cell lines using Sulforhodamine B assay and, results were compared to standard drugs, 5-fluorouracil and tamoxifen, respectively.
Conclusion
The performed antimicrobial activity indicated that compounds
3
,
5
,
6
,
8
and
14
showed promising activity against selected microbial species. Antiproliferative screening found compound
14
to be the most potent compound against HCT116 (IC
50
= 71.8 µM), whereas Compound
6
was the most potent against MCF7 (IC
50
= 74.1 µM). Further, the molecular docking study has been carried to find out the interaction between active oxazole compounds with CDK8 (HCT116) and ER-α (MCF7) proteins indicated that compound
14
and
6
showed good dock score with better potency within the ATP binding pocket and may be used as a lead for rational drug designing of the anticancer molecule.
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