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International Journal of Medicinal Chemistry

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https://www.readbyqxmd.com/read/27127651/benzyl-1-2-4-triazoles-as-cb-1-cannabinoid-receptor-ligands-preparation-and-in-vitro-pharmacological-evaluation
#1
Laura Hernandez-Folgado, Juan Decara, Fernando Rodríguez de Fonseca, Pilar Goya, Nadine Jagerovic
In a previous study, we have identified 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles to be a novel class of cannabinoid type 1 receptor (CB1R) antagonists. In order to expand the number of cannabinoid ligands with a central 1,2,4-triazole scaffold, we have synthesized a novel series of 1-benzyl-1H-1,2,4-triazoles, and some of them were evaluated by CB1R radioligand binding assays. Compound 12a showed the most interesting pharmacological properties, possessing a CB1R affinity in the nanomolar range.
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27119022/ct-dna-binding-and-antibacterial-activity-of-octahedral-titanium-iv-heteroleptic-benzoylacetone-and-hydroxamic-acids-complexes
#2
Raj Kaushal, Sheetal Thakur, Kiran Nehra
Five structurally related titanium (IV) heteroleptic complexes, [TiCl2(bzac)(L(1-4))] and [TiCl3(bzac)(HL(5))]; bzac = benzoylacetonate; L(1-5) = benzohydroximate (L(1)), salicylhydroximate (L(2)), acetohydroximate (L(3)), hydroxyurea (L(4)), and N-benzoyl-N-phenyl hydroxylamine (L(5)), were used for the assessment of their antibacterial activities against ten pathogenic bacterial strains. The titanium (IV) complexes (1-5) demonstrated significant level of antibacterial properties as measured using agar well diffusion method...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27057354/in-silico-designing-and-analysis-of-inhibitors-against-target-protein-identified-through-host-pathogen-protein-interactions-in-malaria
#3
Monika Samant, Nidhi Chadha, Anjani K Tiwari, Yasha Hasija
Malaria, a life-threatening blood disease, has been a major concern in the field of healthcare. One of the severe forms of malaria is caused by the parasite Plasmodium falciparum which is initiated through protein interactions of pathogen with the host proteins. It is essential to analyse the protein-protein interactions among the host and pathogen for better understanding of the process and characterizing specific molecular mechanisms involved in pathogen persistence and survival. In this study, a complete protein-protein interaction network of human host and Plasmodium falciparum has been generated by integration of the experimental data and computationally predicting interactions using the interolog method...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27051530/new-conjugates-of-quinoxaline-as-potent-antitubercular-and-antibacterial-agents
#4
Ramalingam Peraman, Rajendran Kuppusamy, Sunil Kumar Killi, Y Padmanabha Reddy
Considering quinoxaline as a privileged structure for the design of potent intercalating agents, some new sugar conjugates of quinoxaline were synthesized and characterized by IR, (1)HNMR, (13)C NMR, and mass spectral data. In vitro testing for antitubercular and antimicrobial activities was performed against Mycobacterium tuberculosis H 37 Rv and some pathogenic bacteria. Results revealed that conjugate containing ribose moiety demonstrated the most promising activity against Mycobacteria and bacteria with minimum inhibitory concentrations (MIC) of 0...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27022484/synthesis-in-vivo-anti-inflammatory-activity-and-molecular-docking-studies-of-new-isatin-derivatives
#5
Ravi Jarapula, Kiran Gangarapu, Sarangapani Manda, Sriram Rekulapally
A novel synthesis of 2-hydroxy-N'-(2-oxoindolin-3-ylidene) benzohydrazide derivatives was synthesized by the condensation of 2-hydroxybenzohydrazide with substituted isatins. The synthesized compounds were characterized by FT-IR, (1)H-NMR, and mass spectral data. Further, the compounds were screened for in vivo anti-inflammatory activity by carrageenan induced paw edema method. The tested compounds have shown mild-to-moderate anti-inflammatory activity. The compounds VIIc and VIId exhibited 65% and 63% of paw edema reduction, respectively...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26998358/design-and-microwave-assisted-synthesis-of-coumarin-derivatives-as-pde-inhibitors
#6
Mahadev N Kumbar, Ravindra R Kamble, Atulkumar A Kamble, Sujith Raj Salian, Sandhya Kumari, Ramya Nair, Guruprasad Kalthur, Satish Kumar Adiga, D Jagadeesh Prasad
Coumarins appended to benzimidazole through pyrazole are designed and synthesized using microwave irradiation. These compounds were analyzed for phosphodiesterase (PDE) inhibition indirectly by motility pattern in human spermatozoa. Some of the synthesized compounds, namely, 5d, 5e, 5f, 5g, 5h, and 5k, have exhibited potent inhibitory activity on PDE.
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26998357/changes-in-the-physicochemical-properties-of-piperine-%C3%AE-cyclodextrin-due-to-the-formation-of-inclusion-complexes
#7
Toshinari Ezawa, Yutaka Inoue, Sujimon Tunvichien, Rina Suzuki, Ikuo Kanamoto
Piperine (PP) is a pungent component in black pepper that possesses useful biological activities; however it is practically insoluble in water. The aim of the current study was to prepare a coground mixture (GM) of PP and β-cyclodextrin (βCD) (molar ratio of PP/βCD = 1/1) and subsequently evaluate the solubility of PP and physicochemical properties of the GM. DSC thermal behavior of the GM showed the absence of melting peak of piperine. PXRD profile of the GM exhibited halo pattern and no characteristic peaks due to PP and βCD were observed...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26989511/biological-impact-of-pd-ii-complexes-synthesis-spectral-characterization-in-vitro-anticancer-ct-dna-binding-and-antioxidant-activities
#8
Nitin Kumar Sharma, Rakesh Kumar Ameta, Man Singh
A new series of Pd (II) complexes of methyl substituted benzylamine ligands (BLs) has been synthesized and characterized via spectroscopic techniques such as UV/Vis. FTIR, LCMS, (1)H, and (13)C NMR. The UV/Vis study in DMSO, DMSO + water, and DMSO + PBS buffer (pH = 7.2) confirmed their molecular sustainability in liquids. Their in vitro anticancer activity against breast cancer cell lines such as MCF-7 and MDA-MB-231 makes them interesting for in vivo analysis. Their stronger DNA binding activity (DBA) compared with free ligand suggested them as a good DNA binder...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26981281/syntheses-and-antibiotic-evaluation-of-2-2r-4r-4-carboxy-2-hydroxypyrrolidin-1-yl-carbonyl-benzene-1-5-dicarboxylic-acids-and-2-carbamoylbenzene-1-5-dicarboxylic-acid-analogues
#9
Abdulrazaq Tukur, Isaac Asusheyi Bello, Neil Anthony Koorbanally, James Dama Habila
Our search for new antibiotics led to the syntheses and biological evaluation of new classes of dicarboxylic acid analogues. The syntheses involve nucleophilic addition of different substituted benzylamine, aniline, alkylamine, and 4-hydroxyl-L-proline with carbamoylbenzoic acid. The results of the antimicrobial activity as indicated by the zone of inhibition (ZOI) showed that Z 10 is the most active against Pseudomonas aeruginosa (32 mm) and least active against Candida stellatoidea (27 mm) and Vancomycin Resistant Enterococci (VRE) (27 mm), while Z 7 shows the least zone of inhibition (22 mm) against Methicillin Resistant Staphylococcus aureus (MRSA)...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26981280/synthesis-and-evaluation-of-mannitol-based-inhibitors-for-lipopolysaccharide-biosynthesis
#10
Richard E Johnsson
Antibiotic resistance is a serious threat against humankind and the need for new therapeutics is crucial. Without working antibiotics, diseases that we thought were extinct will come back. In this paper two new mannitol bisphosphate analogs, 1,6-dideoxy-1,6-diphosphoramidate mannitol and 1,6-dideoxy-1,6-dimethansulfonamide mannitol, have been synthesized and evaluated as potential inhibitors of the enzyme GmhB in the biosynthesis of lipopolysaccharides. 1,6-Dideoxy-1,6-diphosphoramidate mannitol showed promising result in computational docking experiments, but neither phosphate analog showed activity in the Kirby-Bauer antibiotic susceptibility test...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26942008/a-review-on-platensimycin-a-selective-fabf-inhibitor
#11
REVIEW
Manik Das, Partha Sakha Ghosh, Kuntal Manna
Emerging resistance to existing antibiotics is an inevitable matter of concern in the treatment of bacterial infection. Naturally occurring unique class of natural antibiotic, platensimycin, a secondary metabolite from Streptomyces platensis, is an excellent breakthrough in recent antibiotic research with unique structural pattern and significant antibacterial activity. β-Ketoacyl-(acyl-carrier-protein (ACP)) synthase (FabF) whose Gram-positive bacteria need to biosynthesize cell membranes is the target of inhibition of platensimycin...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26904285/antibacterial-properties-of-alkaloid-extracts-from-callistemon-citrinus-and-vernonia-adoensis-against-staphylococcus-aureus-and-pseudomonas-aeruginosa
#12
Donald Mabhiza, Tariro Chitemerere, Stanley Mukanganyama
The development of new antibiotics from new chemical entities is becoming more and more expensive, time-consuming, and compounded by emerging strains that are drug resistant. Alkaloids are plant secondary metabolites which have been shown to have potent pharmacological activities. The effect of alkaloids from Callistemon citrinus and Vernonia adoensis leaves on bacterial growth and efflux pump activity was evaluated on Staphylococcus aureus and Pseudomonas aeruginosa. At a concentration of 1.67 mg/mL, the alkaloids inhibited bacterial growth with comparable effects to ampicillin, a standard antibiotic...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26881075/synthesis-and-anti-inflammatory-activity-of-some-o-propargylated-n-acetylpyrazole-derived-from-1-3-diarylpropenones
#13
Ashwani Kumar Dhingra, Bhawna Chopra, Rameshwar Dass, Sanjeev K Mittal
In search of novel effective potent therapeutic agents delivered by oral route for inflammation treatment, some novel O-propargylated-N-acetylpyrazole analogs (5a-j) were prepared by treating N-acetylpyrazole (4a-j) derived from 1,3-diarylpropenones (3a-j) with propargyl bromide. Claisen-Schmidt condensation of a series of substituted aryl ketones 1 and benzaldehydes 2 in glacial acetic acid afforded 1,3-diarylpropenones which on further treatment with hydrazine hydrate in acetic acid under reflux conditions afforded 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles (4a-j)...
2016: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26798517/p-sulfonic-acid-calix-4-arene-as-an-efficient-catalyst-for-one-pot-synthesis-of-pharmaceutically-significant-coumarin-derivatives-under-solvent-free-condition
#14
Hamed Tashakkorian, Moslem Mansour Lakouraj, Mona Rouhi
One-pot and efficient protocol for preparation of some potent pharmaceutically valuable coumarin derivatives under solvent-free condition via direct coupling using biologically nontoxic organocatalyst, calix[4]arene tetrasulfonic acid (CSA), was introduced. Calix[4]arene sulfonic acid has been incorporated lately as a magnificent and recyclable organocatalyst for the synthesis of some organic compounds. Nontoxicity, solvent-free conditions, good-to-excellent yields for pharmaceutically significant structures, and especially ease of catalyst recovery make this procedure valuable and environmentally benign...
2015: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26682068/a-review-of-the-updated-pharmacophore-for-the-alpha-5-gaba-a-benzodiazepine-receptor-model
#15
REVIEW
Terry Clayton, Michael M Poe, Sundari Rallapalli, Poonam Biawat, Miroslav M Savić, James K Rowlett, George Gallos, Charles W Emala, Catherine C Kaczorowski, Douglas C Stafford, Leggy A Arnold, James M Cook
An updated model of the GABA(A) benzodiazepine receptor pharmacophore of the α5-BzR/GABA(A) subtype has been constructed prompted by the synthesis of subtype selective ligands in light of the recent developments in both ligand synthesis, behavioral studies, and molecular modeling studies of the binding site itself. A number of BzR/GABA(A) α5 subtype selective compounds were synthesized, notably α5-subtype selective inverse agonist PWZ-029 (1) which is active in enhancing cognition in both rodents and primates...
2015: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/25834744/synthesis-and-biological-activity-of-arylspiroborate-salts-derived-from-caffeic-acid-phenethyl-ester
#16
Martin J G Hébert, Andrew J Flewelling, Trevor N Clark, Natalie A Levesque, Jacques Jean-François, Marc E Surette, Christopher A Gray, Christopher M Vogels, Mohamed Touaibia, Stephen A Westcott
Two novel boron compounds containing caffeic acid phenethyl ester (CAPE) derivatives have been prepared and characterized fully. These new compounds and CAPE have been investigated for potential antioxidant and antimicrobial properties and their ability to inhibit 5-lipoxygenase and whether chelation to boron improves their biological activity. Sodium salt 4 was generally more active than ammonium salt 5 in the biological assays and surpassed the radical scavenging ability of CAPE. Compounds 4 and 5 were more active than CAPE and Zileuton in human polymorphonuclear leukocytes...
2015: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/25802757/facile-synthesis-characterization-and-in-vitro-antimicrobial-screening-of-a-new-series-of-2-4-6-trisubstituted-s-triazine-based-compounds
#17
Ravi Bhushan Singh, Nirupam Das, Md Kamaruz Zaman
A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, (1)HNMR, (13)CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 μgmL(-1) against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 μgmL(-1)) and S...
2015: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/25734015/design-and-synthesis-of-pyrazole-3-one-derivatives-as-hypoglycaemic-agents
#18
Prasanna A Datar, Sonali R Jadhav
Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the docking score, the designed compounds were selectively prioritized for synthesis. The synthesized compounds were subjected to in vivo hypoglycemic activity using alloxan induced diabetic rats and metformin as a standard...
2015: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/25734014/design-and-synthesis-of-novel-hybrid-molecules-against-malaria
#19
Melanie Lödige, Luisa Hiersch
The effective treatment of malaria can be very complex: Plasmodium parasites develop in multiple stages within a complex life cycle between mosquitoes as vectors and vertebrates as hosts. For the full and effective elimination of parasites, an effective drug should be active against the earliest stages of the Plasmodium infection: liver stages (reduce the progress of the infection), blood stages (cure the clinical symptoms), and gametocytes (inhibit the transmission cycle). Towards this goal, here we report the design, the synthetic methodology, and the characterization of novel hybrid agents with combined activity against Plasmodium liver stages and blood stages and gametocytes...
2015: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/25685554/design-and-synthesis-of-novel-antileishmanial-compounds
#20
Melanie Loedige
According to the WHO, infectious diseases, and in particular neglected tropical diseases in poor developing countries, still play a significant role in a vast number of deaths reported worldwide. Among them, leishmaniasis occurs as a complex and clinically diverse illness caused by protozoan Leishmania species which are transmitted through the bite of sandflies. They develop through a complex life cycle, from promastigotes in sandflies to amastigotes in humans. The severity of disease is determined by the type of infecting Leishmania species and also depends strongly on whether the parasite infection leads to a systemic involvement or not...
2015: International Journal of Medicinal Chemistry
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