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doi:10.13040/ijpsr.0975-8232.4(9).3296-03

Cited by 5 publications

(4 citation statements)

References 16 publications

(30 reference statements)

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“…On the basis of the lack of in vivo data on this scaffold and to study the effect of stereochemistry as well as substituents at C1 and C3 position of THβC’s and to investigate this scaffold in combination therapy for malaria, we synthesized a set of eight THβC derivatives including both cis- and trans-isomers by reaction between methyl ester derivative of l -tryptophan and aldehydes containing medicinally important heterocyclic rings such as benzo[1,3]dioxole ( 8a and 9a ), pyridine ( 8b and 9b ) and thiophene ( 8c and 9c ) rings. The selected heterocycles are privileged structures and found in several drugs such as tadalafil, niacin, clopidogrel, and many more. , Additional aliphatic hydrocarbon chain-substituted THβC’s ( 8d and 9d ) were also synthesized to confirm the exact requirement of C1 aromatic substitution for the desired antimalarial activity (Scheme ).…”

Section: Results and Discussionmentioning

confidence: 99%

Synthesis and Evaluation of Antiplasmodial Efficacy of β-Carboline Derivatives against Murine Malaria

et al. 2018

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The difficulty of developing an efficient malaria vaccine along with increasing spread of multidrug resistant strain of Plasmodium falciparum to the available antimalarial drugs poses the need to discover safe and efficacious antimalarial drugs to control malaria. An alternative strategy is to synthesize compounds possessing structures similar to the active natural products or marketed drugs. Several biologically active natural products and drugs contain β-carboline moiety. In the present study, few selected β-carboline derivatives have been synthesized and tested for their in vitro and in vivo antiplasmodial activity against the rodent malaria parasite Plasmodium berghei (NK-65). The designed analogs exhibited considerable in vitro antimalarial activity. Two compounds (1R,3S)-methyl 1-(benzo[d][1,3]dioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate (9a) and (1R,3S)-methyl 1-(pyridin-3-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate (9b) were further selected for in vivo studies. Both the lead compounds (9a and 9b) were observed to be safe for oral administration. The therapeutic effective dose (ED50) for 9a and 9b were determined and in the animal model, 9a (at 50 mg/kg dose) exhibited better activity in terms of parasite clearance and enhancement of host survival. Biochemical investigations also point toward the safety of the compound to the hepatic and renal functions of the rodent host. Further studies are underway to explore its activity alone as well as in combination therapy with artesunate against the human malaria parasite P. falciparum.

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Section: Results and Discussionmentioning

confidence: 99%

Synthesis and Evaluation of Antiplasmodial Efficacy of β-Carboline Derivatives against Murine Malaria

et al. 2018

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“…Numerous reports have documented diverse biological activities attributed to the benzodioxole ring system, encompassing anticancer, anticonvulsant, antidepressant, antiinflammatory, antihypertensive, anti-oxidant, antiprotozoal, antivitiligo, and immunomodulatory effects (Figure 30). 100 Mansour and group 101 recently communicated the synthesis of benzodioxole-linked thiazolyl-pyrazolines 102a−102b through the ring closure reaction of 4,5-dihydro-1H-pyrazoles 101 and phenacyl bromide 7. The reaction was conducted under reflux conditions on a water bath for 3 h, resulting in Scheme 39 Scheme 40 favorable yields.…”

Section: Morpholine-linked Hybridsmentioning

confidence: 99%

Section: Thiazolyl-pyrazoline Hybridsmentioning

confidence: 99%

Development in the Synthesis of Bioactive Thiazole-Based Heterocyclic Hybrids Utilizing Phenacyl Bromide

Kumari,

Dhillon,

Rani

et al. 2024

ACS Omega

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Heterocyclic hybrid frameworks represent a burgeoning domain within the realms of drug discovery and medicinal chemistry, attracting considerable attention in recent years. Thiazole pharmacophore fragments, inherent in natural products such as peptide alkaloids, metabolites, and cyclopeptides, have demonstrated a broad spectrum of pharmacological potentials. Given their profound biological significance, a plethora of thiazole-based hybrids have been synthesized through the conjugation of thiazole moieties with bioactive pyrazole and pyrazoline fragments. This review systematically presents a compendium of robust methodologies for the synthesis of thiazole-linked hybrids, employing the (3 + 2) heterocyclization reaction, specifically the Hantzsch-thiazole synthesis, utilizing phenacyl bromide as the substrate. The strategic approach of molecular hybridization has markedly enhanced drug efficacy, mitigated resistance to multiple drugs, and minimized toxicity concerns. The resultant thiazole-linked hybrids exhibit a myriad of medicinal properties viz. anticancer, antibacterial, anticonvulsant, antifungal, antiviral, and antioxidant activities. This compilation of methodologies and insights serves as a valuable resource for medicinal chemists and researchers engaged in the design of novel thiazole-linked hybrids endowed with therapeutic attribute.

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“…A recent research has shown that some benzodioxole compounds act as negative modulators for AMPA receptors. In addition to increasing the rate of desensitization and prolonging the deactivation process, many additional derivatives have shown potential as anti-Alzheimer and antiepileptic agents. − The capacity of these substances to modulate AMPA receptors and exhibit neuroprotective effects indicates a possible avenue for their neuroprotective capacities. Furthermore, these chemicals have also shown effectiveness in reducing inflammation, anticancer, and antiviral activities, underscoring their diverse pharmacological significance.…”

Section: Introductionmentioning

confidence: 99%

Evaluating the Neuroprotective Potential of Novel Benzodioxole Derivatives in Parkinson’s Disease via AMPA Receptor Modulation

Hawash,

Qneibi,

Natsheh

et al. 2024

ACS Chem. Neurosci.

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Parkinson’s disease (PD) is a significant health issue because it gradually damages the nervous system. α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors play a significant role in the development of PD. The current investigation employed hybrid benzodioxole-propanamide (BDZ-P) compounds to get information on AMPA receptors, analyze their biochemical and biophysical properties, and assess their neuroprotective effects. Examining the biophysical characteristics of all the subunits of the AMPA receptor offers insights into the impact of BDZ-P on the desensitization and deactivation rate. It demonstrates a partial improvement in the locomotor capacities in a mouse model of Parkinson’s disease. In addition, the in vivo experiment assessed the locomotor activity by utilizing the open-field test. Our findings demonstrated that BDZ-P7 stands out with its remarkable potency, inhibiting the GluA2 subunit nearly 8-fold with an IC50 of 3.03 μM, GluA1/2 by 7.5-fold with an IC50 of 3.14 μM, GluA2/3 by nearly 7-fold with an IC50 of 3.19 μM, and GluA1 by 6.5-fold with an IC50 of 3.2 μM, significantly impacting the desensitization and deactivation rate of the AMPA receptor. BDZ-P7 showed an in vivo impact of partially reinstating locomotor abilities in a mouse model of PD. The results above suggest that the BDZ-P7 compounds show great promise as top contenders for the development of novel neuroprotective therapies.

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Cited by 5 publications

References 16 publications

Synthesis and Evaluation of Antiplasmodial Efficacy of β-Carboline Derivatives against Murine Malaria

Synthesis and Evaluation of Antiplasmodial Efficacy of β-Carboline Derivatives against Murine Malaria

Development in the Synthesis of Bioactive Thiazole-Based Heterocyclic Hybrids Utilizing Phenacyl Bromide

Evaluating the Neuroprotective Potential of Novel Benzodioxole Derivatives in Parkinson’s Disease via AMPA Receptor Modulation

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