Diffractaic acid and its ethers as anti-respiratory syncytial virus agents
AbstractA major secondary metabolite of lichens, diffractaic acid, was found here to exert a significant antiviral action on respiratory syncytial virus strain A2 with a EC50 of 4.8  µM while showing low toxicity to a tested cell line (CC50 of 221.9  µM). We developed methods for the synthesis of derivatives at the hydroxyl group of diffractaic acid and obtained three series of new derivatives: those of diffractaic acid and of its methyl and benzyl esters. We noted that the most promising compounds are derivatives of benzyldiffractate, which typically were found to have same or lower cytotoxicity as compared to eithe...
Source: Medicinal Chemistry Research - March 11, 2024 Category: Chemistry Source Type: research

Motor and non-motor symptoms, drugs, and their mode of action in Parkinson ’s disease (PD): a review
AbstractParkinson ’s disease is second most common neurodegenerative disorder neurological illness that primarily affects patients in their later years of life. Specific neurons in the brain begin to malfunction resulting in a loss of a substance called dopamine which is characterized by the accumulation of α-synu clein aggregates within cells, forming structures known as Lewy bodies and Lewy neurites. It is affecting more than 1% of people worldwide (aged 65 and above) and is expected to increase in prevalence by 2030. Muscle rigidity, tremor, and unresponsiveness of motion are some of the motor signs of thi s conditio...
Source: Medicinal Chemistry Research - March 7, 2024 Category: Chemistry Source Type: research

Synthesis, urease inhibitory and anticancer evaluation of glucosamine-sulfonylurea conjugates
AbstractUrease catalyses the hydrolysis of urea to ammonia and carbon dioxide. This enzyme is important in the virulence of several human pathogens and urease activity in soil can cleave urea fertilisers prematurely, leading to waste of agricultural nitrogen. A series of arylsulfonylurea-glucosamine hybrid compounds were synthesised. Reaction of arylsulfonamides with phenyl chloroformate and 4-dimethylaminopyridine gave either phenyl N-(2,4-arylsulfonyl)carbamate 4-dimethylaminopyridinium salts or N-(4-arylsulfonyl)-4-dimethylaminopyridinium-1-carboxamide inner salts, depending on the substitution on the arylsulfonamide. B...
Source: Medicinal Chemistry Research - March 7, 2024 Category: Chemistry Source Type: research

Motor and non-motor symptoms, drugs, and their mode of action in Parkinson ’s disease (PD): a review
AbstractParkinson ’s disease is second most common neurodegenerative disorder neurological illness that primarily affects patients in their later years of life. Specific neurons in the brain begin to malfunction resulting in a loss of a substance called dopamine which is characterized by the accumulation of α-synu clein aggregates within cells, forming structures known as Lewy bodies and Lewy neurites. It is affecting more than 1% of people worldwide (aged 65 and above) and is expected to increase in prevalence by 2030. Muscle rigidity, tremor, and unresponsiveness of motion are some of the motor signs of thi s conditio...
Source: Medicinal Chemistry Research - March 7, 2024 Category: Chemistry Source Type: research

Synthesis, urease inhibitory and anticancer evaluation of glucosamine-sulfonylurea conjugates
AbstractUrease catalyses the hydrolysis of urea to ammonia and carbon dioxide. This enzyme is important in the virulence of several human pathogens and urease activity in soil can cleave urea fertilisers prematurely, leading to waste of agricultural nitrogen. A series of arylsulfonylurea-glucosamine hybrid compounds were synthesised. Reaction of arylsulfonamides with phenyl chloroformate and 4-dimethylaminopyridine gave either phenyl N-(2,4-arylsulfonyl)carbamate 4-dimethylaminopyridinium salts or N-(4-arylsulfonyl)-4-dimethylaminopyridinium-1-carboxamide inner salts, depending on the substitution on the arylsulfonamide. B...
Source: Medicinal Chemistry Research - March 7, 2024 Category: Chemistry Source Type: research

Evaluation of ortho-substituted Bis-Functionalized Triazoles as Tyrosinase Inhibitors: Modulating Dopamine Synthesis and Behavior in Zebrafish
AbstractFacile and green chemistry pathways are utilized through microwave-assisted organic synthesis (MAOS) to generate biologically activeortho-substituted bis-functionalized triazole derivatives (C1-C7) in one step. MAOS expedited the process by improving reaction times (from 24  hours to 15–20 minutes) and provided the triazoles with good to excellent yields. Zebrafish based physiological and morphological analyses were carried out and most synthesized triazole compounds showed a significantly increased heart rate and growth in Zebrafish. The maximum tolerable dose ( MTD) of these compounds were identified to be ...
Source: Medicinal Chemistry Research - March 6, 2024 Category: Chemistry Source Type: research

Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction
AbstractIsatin (indol-2,3-dione), a secondary metabolite of tryptophan, has been used as the core structure to design several compounds that have been tested and identified as potent inhibitors of apoptosis, potential antitumor agents, anticonvulsants, and antiviral agents. In this work, several analogs of isatin hybrids have been synthesized and characterized, and their activities were established as inhibitors of both Aurora A kinase and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike/host angiotensin-converting enzyme II (ACE2) interactions. Amongst the synthesized isatin hybrids, compounds6a,6f,6g, a...
Source: Medicinal Chemistry Research - March 5, 2024 Category: Chemistry Source Type: research

Bioassay-guided fractionations of Cannabis sativa extract and HPLC-assisted purifications of anti-proliferative active fractions lead to the isolation of 16 known and one new phytomolecule and their in-silico analysis
AbstractThe comprehensive anti-cancer activities of cannabinoid acids and non-cannabinoids are not fully explored. Herein we report simple extraction, faster bioassay-guided fractionation, and HPLC-assisted purification of bioactive secondary metabolite and their identification. Anti-proliferative activity of six cannabinoid acids and eleven non-cannabinoids from the leaves ofCannabis sativa was evaluated. HPLC- assisted purification from the bioactive fractions leads to isolate one new compound Methoxy Canniprene (methoxy isoprenyl bibenzyl), including all six CBDA ’s eleven non-cannabinoids in a single step, and NMR, H...
Source: Medicinal Chemistry Research - March 5, 2024 Category: Chemistry Source Type: research

Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction
AbstractIsatin (indol-2,3-dione), a secondary metabolite of tryptophan, has been used as the core structure to design several compounds that have been tested and identified as potent inhibitors of apoptosis, potential antitumor agents, anticonvulsants, and antiviral agents. In this work, several analogs of isatin hybrids have been synthesized and characterized, and their activities were established as inhibitors of both Aurora A kinase and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike/host angiotensin-converting enzyme II (ACE2) interactions. Amongst the synthesized isatin hybrids, compounds6a,6f,6g, a...
Source: Medicinal Chemistry Research - March 5, 2024 Category: Chemistry Source Type: research

Bioassay-guided fractionations of Cannabis sativa extract and HPLC-assisted purifications of anti-proliferative active fractions lead to the isolation of 16 known and one new phytomolecule and their in-silico analysis
AbstractThe comprehensive anti-cancer activities of cannabinoid acids and non-cannabinoids are not fully explored. Herein we report simple extraction, faster bioassay-guided fractionation, and HPLC-assisted purification of bioactive secondary metabolite and their identification. Anti-proliferative activity of six cannabinoid acids and eleven non-cannabinoids from the leaves ofCannabis sativa was evaluated. HPLC- assisted purification from the bioactive fractions leads to isolate one new compound Methoxy Canniprene (methoxy isoprenyl bibenzyl), including all six CBDA ’s eleven non-cannabinoids in a single step, and NMR, H...
Source: Medicinal Chemistry Research - March 5, 2024 Category: Chemistry Source Type: research

Synthesis and pharmacological activities of Schiff bases with some transition metal complexes: a review
AbstractSchiff bases transition metal complexes have received significant attentions in the scientific community for their versatile applications. The incorporation of metals to Schiff base ligands attracts much attention, since the metals and Schiff base ligands coordinated via bonding. Thus, chelation effects will enhance and improve the biological activities of the derivatives of title compound. Most of these derivatives displayed broad range bioactivities including antibacterial, antifungal, antituberclosis, antimalarial, antioxidant, antidiabetic, anti-inflammatory and anticancer activities. Up to date, continuous eff...
Source: Medicinal Chemistry Research - March 1, 2024 Category: Chemistry Source Type: research

Selectivity of N(2)-substituted oxotriazinoindole aldose reductase inhibitors is determined by the interaction pattern with Pro301-Arg312 loop of aldehyde reductase
AbstractNovel oxotriazinoindoles (OTIs) were recently reported as highly efficient and selective aldose reductase inhibitors. Here, a series of novelN(2)-substituted oxotriazinoindoles was developed with the aim to investigate molecular interactions within the aldose reductase (ALR2) inhibitor binding site. About twice increased inhibition efficacy of the most efficient derivative14 (N(2)-CH2CH2COOH) compared to the unsubstituted leadOTI was obtained, yet at the expense of selectivity relative to anti-target aldehyde reductase (ALR1). To explain the major drop in selectivity, observed also in otherN(2)-substituted derivati...
Source: Medicinal Chemistry Research - March 1, 2024 Category: Chemistry Source Type: research

Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications
AbstractThe 2021 statistics from the International Diabetes Federation reveals that approximately 537 million adults between the ages of 20 and 79 are currently coping with diabetes, highlighting the pressing demand for innovative treatments. To expedite this process, it is crucial to learn from previous failures in drug development. One established method for enhancing the biological, pharmacokinetic or the physicochemical properties of potent drug candidates is through the use of prodrugs. Prodrugs have demonstrated their effectiveness in surmounting challenges related to a drug ’s efficacy during the phases of drug re...
Source: Medicinal Chemistry Research - March 1, 2024 Category: Chemistry Source Type: research