Synthesis and Oral Hypoglycemic Activity of 3-[5'-Methyl-2'-aryl-3'-(thiazol-2ʺ-yl amino) thiazolidin-4'-one]coumarin Derivatives

Number of heterocyclic compounds has been exploited to develop pharmaceutically important molecules, out of which biheterocyclic coumarins are clinically used potential drug candidates showing oral hypoglycemic and antidiabetic activities. A new series of 3-[5'-methyl-2'-aryl-3'-(thiazol-2ʺ-yl amino)thiazolidin-4'-one]coumarin derivatives were designed and synthesized. The title compounds were synthesized from starting material 3- acetyl coumarin. All the synthesized compounds were characterized and screened for hypoglycemic activity. Some of the compounds exhibited promising activity

Benzimidazole-Urea derivatives as anti-cancer agents: In-silico study, synthesis and in-vitro evaluation

A new series of urea derivatives containing benzimidazole group as potential anticancer agents have been designed and synthesized. The structures of the synthesized compounds were characterized and confirmed by spectroscopic techniques such as 1H NMR, and Mass spectrometry. A new series of urea derivatives containing benzimidazole group were design with an intention to search new antiproliferative lead compound. Drug like properties and bioactivity score for drug targets of designed compounds were calculated by molinspiration tool and obtained result found to obey Lipinski’s rule that indicates the compound are orally active molecules. Osiris property explorer was used for the prediction of drug relevant properties and toxicity of synthetic compounds. Pre ADMET server was also used to estimate ADME properties of synthetic compounds, results showed good to notable anticancer activity. So that, these new benzimidazole-urea compounds could serve as potential template to become leads in near future for the discovery and development of new effect orally drugs molecules

Synthesis and Oral Hypoglycemic Activity of 3-[5'-Methyl-2'-aryl-3'- (thiazol-2''-yl amino)thiazolidin-4'-one]coumarin Derivatives. E-Journal of Chemistry

Abstract: Number of heterocyclic compounds has been exploited to develop pharmaceutically important molecules, out of which biheterocyclic coumarins are clinically used potential drug candidates showing oral hypoglycemic and antidiabetic activities. A new series of 3-[5'-methyl-2'-aryl-3'-(thiazol-2''-yl amino)thiazolidin-4'-one]coumarin derivatives were designed and synthesized. The title compounds were synthesized from starting material 3-acetyl coumarin. All the synthesized compounds were characterized and screened for hypoglycemic activity. Some of the compounds exhibited promising activity

<!--[if gte mso 9]><xml> <w:WordDocument> <w:View>Normal</w:View> <w:Zoom>0</w:Zoom> <w:PunctuationKerning/> <w:ValidateAgainstSchemas/> <w:SaveIfXMLInvalid>false</w:SaveIfXMLInvalid> <w:IgnoreMixedContent>false</w:IgnoreMixedContent> <w:AlwaysShowPlaceholderText>false</w:AlwaysShowPlaceholderText> <w:Compatibility> <w:BreakWrappedTables/> <w:SnapToGridInCell/> <w:WrapTextWithPunct/> <w:UseAsianBreakRules/> <w:DontGrowAutofit/> </w:Compatibility> <w:BrowserLevel>MicrosoftInternetExplorer4</w:BrowserLevel> </w:WordDocument> </xml><![endif]--><span style="font-size:12.0pt;font-family: "Times New Roman";mso-fareast-font-family:"Times New Roman";mso-ansi-language: EN-GB;mso-fareast-language:EN-US;mso-bidi-language:AR-SA" lang="EN-GB">QSAR analysis on inhibitors of human dihydroorotate dehydrogenase <br> (<i style="mso-bidi-font-style:normal">h</i>DHODH): The aryl carboxylic acid amide derivatives</span><!--[if gte mso 9]><xml> <w:LatentStyles DefLockedState="false" LatentStyleCount="156"> </w:LatentStyles> </xml><![endif]--><!--[if gte mso 10]> <style> /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-parent:""; mso-padding-alt:0cm 5.4pt 0cm 5.4pt; mso-para-margin:0cm; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:10.0pt; font-family:"Times New Roman"; mso-ansi-language:#0400; mso-fareast-language:#0400; mso-bidi-language:#0400;} </style> <![endif]-->

1749-1760Structural and physicochemical requirements of aryl carboxylic acid amide derivatives for the inhibition of human dihydroorotate dehydrogenase (hDHODH) are explored in this QSAR study. The calculated molecular descriptors (electronic and thermodynamic) have been used to derive QSAR models between hDHODH inhibitory activity and structural properties. The best model for prediction of hDHODH inhibitory activity is obtained by applying sequential multiple linear regression (SMLR) analysis.  Regression coefficient of all the descriptors is significant at more than 99% and statistically significant model with r2 > 0.87 is obtained. Selected QSAR model emphasized the importance of logP, torsion energy (Et), 1,4-dihedral van der Waals interaction (1,4-VDWE) and <span style="mso-bidi-font-weight: bold">electronic descriptor like lowest unoccupied molecular orbital (LUMO) on hDHODH inhibitory activity. Results of QSAR analysis show that logP and LUMO are the principle descriptors for inhibition of hDHODH. QSAR model has also been tested successfully for internal (q2 > 0.753) and external (r2 pred > 0.621) validation criteria. It is believed that the results of this study will be helpful in the design of more potent and selective <i style="mso-bidi-font-style: normal">hDHODH inhibitors. </span

Synthesis and anti-inflammatory activity of 4-(5'-acetyl-6'-hydroxy -3'-methyl-benzofuran-2'-yl) coumarin and 6-acetyl-3, 7-dimethyl-2-(coumarin-4'-yl) furo [3,2-<i style="">g</i>] chromen-5-one

1674-1678Various 4-bromomethylcoumarins 1 have been reacted with diacetyl resorcinol 2 to afford corresponding ethers 3, which undergo intermolecular aldol condensation followed by dehydration to form 4-(5'-acetyl-6'-hydroxy-3'-methylbenzofuran-2'-yl) coumarin 4. Further compound 4 on reaction with sodium acetate and acetic anhydride afford 6-acetyl-3, 7-dimethyl-2-(coumarin 4'-yl) furo [3,2-g] chromen-5-one 5. Their structures have been confirmed by IR, NMR and mass spectral data. Of these compounds, 4e, 4f and 5e show good anti-inflammatory and analgesic activity

Dual fluorescence and biological evaluation of paracetamol ethers from 4-bromomethylcoumarins

2416-2422Paracetamol 1 has been reacted with 4-bromomethylcoumarins 2 to obtain the corresponding ethers 3 which have been hydrolyzed to the amino ethers 4. Structure of 4 has been confirmed by the chemoselective reaction of 2 with p-aminophenol, which has also been found to yield the thermodynamically controlled products 5 at elevated temperatures. Compounds 3 have been found to exhibit dual fluorescence. IR,1H NMR and mass spectral data have confirmed structures of all the compounds. Biological evaluation has shown that compounds 3e and 3g show good anti-inflammatory and analgesic properties

Design, synthesis and antimicrobial activities of some novel 1,3,4-thiadiazole, 1,2,4-triazole-5-thione and 1,3-thiazolan-4-one derivatives of benzimidazole

A series of novel 1,3,4-thiadiazole; 1,2,4-triazole-5-thione and 1,3-thiazolan-4-one derivatives of benzimidazole were synthesized by nucleophilic substitution reaction of 2-substituted-1[H] benzimidazole. Compounds (1H-benzo[d]imidazol-2-yl)methanamine 3, 2-(isothiocyanatomethyl)-1H-benzo[d]imidazole 4, 4-(1H-benzo[d]imidazol-2-yl)benzenamine 6 and 4-(1H-benzo[d]imidazol-2-yl)benzenamine 7 are synthesized for the synthesis of targeted compounds. Structures of all the targeted synthesized compounds were evaluated by spectral and elemental methods of analysis. All the synthesized compounds were evaluated for antibacterial and antifungal activities. Some of the synthesized compounds showed good antibacterial and antifungal activities with 2.0 and 2.5 μg/mL MIC (minimum inhibitory concentration), respectively

A brief review of Cherylline synthesis

1301-13201,2,3,4-Tetrahydroisoquinolines are an important class of synthetic and natural compounds, which display a broad range of medicinal activities. The 1,2,3,4-tetrahydroisoquinoline system has attracted attention not only because of its biological activities, but also due to its presence as a basic framework in many naturally occurring products and drugs. Their skeletons are unique among the Amaryllidaceae alkaloids and they have long been alluring targets for synthetic chemists as witnessed by a number of articles dealing with biogenesis, isolation, characterization and synthesis. The alkaloid cherylline is an optically active naturally occurring, 4-phenyl-1,2,3,4-tetrahydroisoquinoline alkaloid, isolated from Crinum powelli, Amaryllidaceae plant. There are many ways for cherylline synthesis. In this short review is described the different methods for synthesis of the alkaloid cherylline

UPTAKE AND SUBCELLULAR DISTRIBUTION OF LIPOSOMES IN RAT LIVER IN NORMAL CONDITIONS AND IN CHRONIC HEPATIC INSUFFICIENCY

Liposomal absorption and subcellular distribution in the rat liver in normal conditions and in chronic hepatic insufficiency (CHI) due to venous congestion were compared. The rats were intravenously administered with empty liposomes (EL) and α-tocopherol containing liposomes (TL). Both liposomal types contained 3Н-lecithin as a radioactive label. Liposomal absorption and distribution were assessed by the tritium activity in the liver sample and its subcellular fractions. It was found that either type of liposomes is absorbed both by the normal and diseased liver. Intact rats showed around 70% of the label in the liver 1h after EL or TL administration. CHI rats had around 75% and 60% of the label within 1h after TL and EL administration, respectively, which demonstrated the preserved ability of the affected liver to absorb liposomes. During the first 6 hours the slow-down of the liposomal label activity was slower in CHI rats. Liposomal membrane modification by incorporating α-tocopherol had an impact both on liposomal absorption and cellular distribution. In particular, both groups showed higher affinity of TL to mitochondria as compared to EL. Thus, the results suggest that liposomal compositions can be used for targeted delivery of biologically active substances both in normal and diseased liver and can be the basis for the development of highly effective pharmaceuticals for intracellular therapy