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Journals Organic and Medicinal Chemistr...

Organic and Medicinal Chemistry Letters

https://read.qxmd.com/read/23968361/design-and-synthesis-of-tetrahydrophthalimide-derivatives-as-inhibitors-of-hiv-1-reverse-transcriptase
#21
JOURNAL ARTICLE
Ashok Penta, Swastika Ganguly, Sankaran Murugesan
BACKGROUND: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are one of the key components in highly active anti-retroviral therapy because of their high specificity and less toxicity. NNRTIs inhibit reverse transcriptase enzyme by binding to the allosteric site, which is 10Å away from the active site. Rapid emergence of resistance is the major problem with all anti-HIV agents. Hence, there is continuous need to develop novel anti-HIV agents active against both drug sensitive and resistance strains...
August 22, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23919542/facile-and-efficient-one-pot-synthesis-of-benzimidazoles-using-lanthanum-chloride
#22
JOURNAL ARTICLE
Yekkirala Venkateswarlu, Sudhagani Ramesh Kumar, Panuganti Leelavathi
BACKGROUND: We report the synthesis of benzimidazoles using lanthanum chloride as an efficient catalyst. One-pot synthesis of 2-substituted benzimidazole derivatives from o-phenylenediamine and a variety of aldehydes were developed under mild reaction conditions. RESULTS: We have examined the effect of different solvents using the same reaction conditions. The yield of the product varied with the nature of the solvents, and better conversion and easy isolation of products were found with acetonitrile...
August 6, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23870758/%C3%AE-keto-esters-from-ketones-and-ethyl-chloroformate-a-rapid-general-efficient-synthesis-of-pyrazolones-and-their-antimicrobial-in-silico-and-in-vitro-cytotoxicity-studies
#23
JOURNAL ARTICLE
Ramasamy Venkat Ragavan, Kalavathi Murugan Kumar, Vijayaparthasarathi Vijayakumar, Sundaramoorthy Sarveswari, Sudha Ramaiah, Anand Anbarasu, Sivashanmugam Karthikeyan, Periyasamy Giridharan, Nalilu Suchetha Kumari
BACKGROUND: Pyrazolones are traditionally synthesized by the reaction of β-keto esters with hydrazine and its derivatives. There are methods to synthesize β-keto esters from esters and aldehydes, but these methods have main limitation in varying the substituents. Often, there are a number of methods such as acylation of enolates in which a chelating effect has been employed to lock the enolate anion using lithium and magnesium salts; however, these methods suffer from inconsistent yields in the case of aliphatic acylation...
July 19, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23870710/antibacterial-activities-and-antioxidant-capacity-of-aloe-vera
#24
JOURNAL ARTICLE
Fatemeh Nejatzadeh-Barandozi
BACKGROUND: The aim of this study was to identify, quantify, and compare the phytochemical contents, antioxidant capacities, and antibacterial activities of Aloe vera lyophilized leaf gel (LGE) and 95% ethanol leaf gel extracts (ELGE) using GC-MS and spectrophotometric methods. RESULTS: Analytically, 95% ethanol is less effective than ethyl acetate/diethyl ether or hexane (in the case of fatty acids) extractions in separating phytochemicals for characterization purposes...
July 19, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23497605/bioactive-flavanoids-from-glycosmis-arborea
#25
JOURNAL ARTICLE
Mohammad Faheem Khan, Nisha Negi, Rajnikant Sharma, Devendra Singh Negi
BACKGROUND: Glycosmis is a genus of evergreen glabrous shrub and distributed all over India. It possesses various medicinal properties and is used in indigenous medicine for cough, rheumatism, anemia, and jaundice. Glycosmis arborea is a rich source of alkaloids, terpenoids, coumarins, as well as flavonoids. RESULTS: The chemical investigation of methanol fraction of the leaves of G. arborea led to the isolation of one new flavone C-glycoside along with three known flavanoids, named as 5,7-dihydroxy-2-[4-hydroxy-3-(methoxy methyl) phenyl]-6-C-β-d-glucopyranosyl flavone (4), 5,7,4'-trihydroxy-3'-methoxy flavone (1), 5,4'-dihydroxy-3'-methoxy-7-O-β-d-glucupyranosyl flavanone (2), and 5,4'-dihydroxy-3'-methoxy-7-O-(α-l-rhamnosyl-(1‴→6‴)-β-d-glucopyranosyl) flavanone (3), respectively...
March 4, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23458122/ultrasound-assisted-synthesis-of-2-4-thiazolidinedione-and-rhodanine-derivatives-catalyzed-by-task-specific-ionic-liquid-tmg-lac
#26
JOURNAL ARTICLE
Suresh, Jagir Singh Sandhu
BACKGROUND: Synthesized arylidene derivatives of rhodanine and 2,4-thiazolidiendione have potent pharmacological activities, and these are also key substrates for the preparation of clinically used antidiabetics. FINDINGS: Some 1,1,3,3-tetramethylguanidine-based task-specific ionic liquids (TSILs) 1a-1e were prepared and employed to the catalyzed solvent-free Knoevenagel condensation of 2,4-thiazolidinedione 3a and rhodanine 3b with a variety of aldehydes. CONCLUSIONS: Best results were obtained with 1,1,3,3-tetramethylguanidine lactate ([TMG][Lac]) 1c...
March 3, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23452433/novel-indole-bearing-combretastatin-analogues-as-tubulin-polymerization-inhibitors
#27
JOURNAL ARTICLE
Sunil Kumar, Samir Mehndiratta, Kunal Nepali, Manish K Gupta, Surrinder Koul, Parduman R Sharma, Ajit K Saxena, Kanaya L Dhar
BACKGROUND: The combretastatins are a class of natural stilbenoids. These molecules generally share three common structural features: a trimethoxy "A"-ring, a "B"-ring containing substituent often at C3' and C4', and an ethene bridge between the two rings, which provides necessary structural rigidity. Members of the combretastatin family possess varying ability to cause vascular disruption in tumors. Combretastatin binds to the colchicine binding site of β-subunit of tubulin. Despite having a similar name, combretastatin is unrelated to statins, a family of cholesterol-lowering drugs...
March 3, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23414667/facile-synthesis-of-symmetrical-bis-benzhydryl-ethers-using-p-toluenesulfonyl-chloride-under-solvent-free-conditions
#28
JOURNAL ARTICLE
Goutam Brahmachari, Bubun Banerjee
BACKGROUND: The benzhydryl ether moiety is widely distributed in nature and constitutes a key structural motif in numerous molecules of significant biological potential and of prospective clinical uses. Solvent-free and cost-effective facile synthesis of symmetrical bis(benzhydryl)ethers is, thus, much desirable. RESULTS: A simple and efficient method for the facile synthesis of symmetrical bis(benzhydryl)ethers directly from the corresponding benzhydrols has been developed using a catalytic amount of p-toluenesulfonyl chloride (5 mol%) at an oil bath temperature of 110°C under solvent-free conditions...
February 18, 2013: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23151464/free-radical-scavenging-properties-of-pyrimidine-derivatives
#29
JOURNAL ARTICLE
Tabassum Bano, Nitin Kumar, Rupesh Dudhe
Free radicals are well known for playing a dual role in our body- deleterious as well as beneficial. It includes a metabolic pathway for its generation. Oxidative stress in our body occurs due to excessive generation of free radicals and reduced level of antioxidants, but at low concentrations, these radicals help to perform normal physiological functions of the body. Scientific evidence suggests that antioxidants reduce the risk for chronic diseases including cancer and heart disease. This review shows current tendency in the pyrimidine synthesis and reveals the pyrimidine core to be a very potent moiety which can be a rich source for the synthesis of new compounds having desirable antioxidant activity...
November 14, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23095284/ft-ir-study-of-the-polysaccharides-isolated-from-the-skin-juice-gel-juice-and-flower-of-aloe-vera-tissues-affected-by-fertilizer-treatment
#30
JOURNAL ARTICLE
Fatemeh Nejatzadeh-Barandozi, Sattar Tahmasebi Enferadi
BACKGROUND: This experiment was conducted to evaluate the effect of different amounts of fertilizers on the polysaccharides of Aloe vera plant. There were four different treatments, viz. T1 = 150% N, T2 = 150% P, T3 = 150% K, and T4 = 150% NPK (50% N + 50% P + 50% K) soil. Crude water-soluble polysaccharides were isolated from the gel juice, skin juice, and flowers of A. vera planted in these soils. RESULTS: Result indicates that skin juice contained 2...
October 24, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/23067874/cannabinoid-receptor-type-2-cb2-selective-n-aryl-oxadiazolyl-propionamides-synthesis-radiolabelling-molecular-modelling-and-biological-evaluation
#31
JOURNAL ARTICLE
Thomas Rühl, Winnie Deuther-Conrad, Steffen Fischer, Robert Günther, Lothar Hennig, Harald Krautscheid, Peter Brust
BACKGROUND: The endocannabinoid system is involved in many physiological and pathological processes. Two receptors (cannabinoid receptor type 1 (CB1) and type 2 (CB2)) are known so far. Many unwanted psychotic side effects of inhibitors of this system can be addressed to the interaction with CB1. While CB1 is one of the most abundant neuroreceptors, CB2 is expressed in the brain only at very low levels. Thus, highly potent and selective compounds for CB2 are desired. N-aryl-((hetero)aromatic)-oxadiazolyl-propionamides represent a promising class of such selective ligands for the human CB2...
October 15, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22937773/chemical-composition-and-antibacterial-activity-of-the-essential-oils-of-ferula-vesceritensis-coss-et-dur-leaves-endemic-in-algeria
#32
JOURNAL ARTICLE
Amar Zellagui, Noueddine Gherraf, Salah Rhouati
UNLABELLED: BACKGROUND: The biological importance of members of genus Ferula promoted us to investigate the leaves of Ferula vesceritensis Coss et Dur. (endemic plant) previously not investigated. This study presents the chemical composition and antibacterial activities of the hydrodistilled oils. RESULTS: Volatile components of the leaves of F. vesceritensis have been studied by gas chromatography-mass spectrometry to afford 23 compounds...
September 3, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22898269/chemical-characterization-antioxidant-and-inhibitory-effects-of-some-marine-sponges-against-carbohydrate-metabolizing-enzymes
#33
JOURNAL ARTICLE
Mohamed Shaaban, Howaida I Abd-Alla, Amal Z Hassan, Hanan F Aly, Mohamed A Ghani
UNLABELLED: BACKGROUND: More than 15,000 marine products have been described up to now; Sponges are champion producers, concerning the diversity of products that have been found. Most bioactive compounds from sponges were classified into anti-inflammatory, antitumor, immuno- or neurosurpressive, antiviral, antimalarial, antibiotic, or antifouling. Evaluation of in vitro inhibitory effects of different extracts from four marine sponges versus some antioxidants indices and carbohydrate hydrolyzing enzymes concerned with diabetes mellitus was studied...
August 16, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22853621/synthesis-and-screening-of-antibacterial-and-antifungal-activity-of-5-chloro-1-3-benzoxazol-2-3-h-one-derivatives
#34
JOURNAL ARTICLE
Priya R Modiya, Chhaganbhai N Patel
UNLABELLED: BACKGROUND: An antibacterial is a substance that either kills bacteria or slows their growth. Antifungal are the agents that use drugs for treatment of fungal infections. 5-Chloro-1,3-benzoxazol-2(3 H)-one (5-Chloro Benzoxazolinone) contains an azole ring structure. Numbers of azole compounds are reported as antibacterial and antifungal agents. Benzoxazolinones naturally occur in plants. They play a role as defense compounds against bacteria, fungi, and insects...
August 1, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22800677/two-new-aliphatic-lactones-from-the-fruits-of-coriandrum-sativum-l
#35
JOURNAL ARTICLE
Kamran J Naquvi, Mohammed Ali, Javed Ahmad
BACKGROUND: The present paper describes the isolation and characterization of two new aliphatic δ-lactones along with three glycerides and n-nonadecanyl cetoleate from the fruits of Coriandrum sativum L. (Apiaceae). The structures of all the isolated phytoconstituents have been established on the basis of spectral data analysis and chemical reactions. RESULTS: Phytochemical investigation of the methanolic extract of C. sativum L. (Apiaceae) fruits resulted in the isolation of two new aliphatic δ-lactones characterized as 2α-n-heptatriacont-(Z)-3-en-1,5-olide (1) (coriander lactone) and 2α-n-tetracont-(Z,Z)-3,26-dien-18α-ol-1,5-olide (2) (hydroxy coriander lactone) together with glyceryl-1,2-dioctadec-9,12-dienoate-3-octadec-9-enoate (3); glyceryl-1,2,3-trioctadecanoate (4); n-nonadecanyl-n-docos-11-enoate (5) and oleiyl glucoside (6)...
July 16, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22794498/discovery-of-indole-tetrafluorophenoxymethylketone-based-potent-novel-small-molecule-inhibitors-of-caspase-3
#36
JOURNAL ARTICLE
Dodheri Syed Samiulla, Andra Naidu, Gummadi Venkateshwar Rao, Murali Ramachandra
UNLABELLED: BACKGROUND: Caspase-3 inhibition has been demonstrated to be therapeutically effective in moderating excessive programmed cell death. Interest in caspase-3 as a therapeutic target has led many to pursue the development of inhibitors. To date, only a few series of non-peptide inhibitors have been described, and these have limitations on their drug-like properties. METHODS: Here, we report the screening of 70 novel small molecules against the caspase-3 enzyme which belongs to four different series (indole fluoromethylketone, indole difluoro and tetrafluorophenoxymethylketone, and oxalamide)...
July 16, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22759342/synthesis-and-evaluation-of-antitumor-activities-of-novel-chiral-1-2-4-triazole-schiff-bases-bearing-%C3%AE-butenolide-moiety
#37
JOURNAL ARTICLE
Xiang Li, Xue-Qiang Li, He-Mei Liu, Xue-Zhang Zhou, Zhi-Hui Shao
BACKGROUND: 1,2,4-Triazole derivatives have received much attention due to their versatile biological properties including antibacterial, antifungal, anticonvulsant, antiinflammatory, anticancer, and antiproliferative properties. 1,2,4-Triazole nucleus has been incorporated into a wide variety of therapeutically interesting molecules to transform them into better drugs. Schiff bases of 1,2,4-triazoles have also been found to possess extensive biological activities. On the other hand, γ-substituted butenolide moiety represents a biological important entity that is present in numerous biologically active natural products...
July 3, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22747771/pharmacophore-generation-and-atom-based-3d-qsar-of-n-iso-propyl-pyrrole-based-derivatives-as-hmg-coa-reductase-inhibitors
#38
JOURNAL ARTICLE
Mahesh Kumar Teli, Rajanikant G K
UNLABELLED: BACKGROUND: Coronary heart disease continues to be the leading cause of mortality and a significant cause of morbidity and account for nearly 30% of all deaths each year worldwide. High levels of cholesterol are an important risk factor for coronary heart disease. The blockage of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity by small molecule inhibitors has been shown to inhibit hypercholesterolemia. Herein, we describe the development of effective and robust pharmacophore model and the structure-activity relationship studies of 43N-iso-propyl pyrrole-based derivatives previously reported for HMG-CoA reductase inhibition...
July 2, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22726766/microwave-assisted-polystyrene-sulfonate-catalyzed-synthesis-of-novel-pyrroles
#39
JOURNAL ARTICLE
Rosario Astrid Vargas Cárdenas, Blanca Olinda Quintanilla Leal, Ashwini Reddy, Debasish Bandyopadhyay, Bimal K Banik
UNLABELLED: BACKGROUND: Pyrroles are widely distributed in nature and important biologically active molecules. The reaction of amines with 2,5-dimethoxytetrahydrofuran is a promising pathway for the synthesis of pharmacologically active pyrroles under microwave irradiation. RESULTS: Microwave-induced polystyrenesulfonate-catalyzed synthesis of pyrroles from amines and 2,5-diemthoxytetrahydrofuran has been accomplished with excellent yield...
June 22, 2012: Organic and Medicinal Chemistry Letters
https://read.qxmd.com/read/22691718/2d-3d-qsar-and-docking-studies-of-1-2-3-thiadiazole-thioacetanilides-analogues-as-potent-hiv-1-non-nucleoside-reverse-transcriptase-inhibitors
#40
JOURNAL ARTICLE
Shailesh V Jain, Manjunath Ghate, Kamlendra S Bhadoriya, Sanjaykumar B Bari, Amar Chaudhari, Jayshri S Borse
UNLABELLED: BACKGROUND: The discovery of clinically relevant inhibitors of HIV-RT for antiviral therapy has proven to be a challenging task. To identify novel and potent HIV-RT inhibitors, the quantitative structure-activity relationship (QSAR) approach became very useful and largely widespread technique forligand-based drug design. METHODS: We perform the two- and three-dimensional (2D and 3D) QSAR studies of a series of 1,2,3-thiadiazole thioacetanilides analogues to elucidate the structural properties required for HIV-RT inhibitory activity...
June 12, 2012: Organic and Medicinal Chemistry Letters
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