- Novel [1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives embedded with benzimidazole moiety as potent antioxidants
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Fourteen novel [1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives bearing benzimidazole moiety (7a-n) have been synthesized using the one-pot nitro reductive cyclization method. All the synthesized compounds were confirmed by 1H nuclear magne
- Sathyanarayana, Reshma,Poojary, Boja,Chandrashekarappa, Revanasiddappa B.,Kumar, Hemanth,Merugumolu, Vijay K.
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- Hydroxy-benzimidazoles as blue-green emitters: Synthesis, structural and DFT studies
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The new benzimidazole ligands (3a-e) were synthesized using ethyl 4-(butylamino)-3-nitrobenzoate and substituted salicylaldehyde in the presence of sodium dithionite reagent which undergoes “one-pot’’ nitro reductive cyclization. Here benzimidazole moiety acts as an electron-acceptor (A) whereas substituted 2-hydroxyphenyl moiety acts as an electron-donor (D) unit. The molecular structures were characterised by FTIR, 1H NMR, 13C NMR, single crystal XRD and MS analysis. Optoelectronic properties were determined by UV–vis, solution and solid photoluminescence, quantum yield and lifetime. The solvent-dependent absorption and emission were studied using both polar protic and polar aprotic solvents. All the derivatives exhibited ESIPT, especially compound ethyl 1-butyl-2-(3,5-dichloro-2-hydroxyphenyl)-1H-benzo[d]imidazole-5-carboxylate (3e) displayed dual emission in both polar protic and polar aprotic solvents. The compound stability and electrochemical property were determined by thermal gravimetric analysis (TGA) and cyclic voltammetry (CV) respectively. The compounds emit intense blue-green fluorescence with high to moderate quantum yield. Also, these derivatives exhibited a high Stokes shift. The computational studies like Density-Functional Theory (DFT) and Molecular Electrostatic Potential (MEP) were conducted to provide important insights into the structure-property relationships. The crystal packing is stabilized through intermolecular hydrogen bonds (C—H…O) and intermolecular interactions (π… π). The findings of results help in developing novel ligands in the field of organic optoelectronics.
- Kumar, Vasantha,Poojary, Boja,Pujar, G. H.,Sathyanarayana, Reshma,Shankar, Madan Kumar,Yallappa, Sangappa
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- Benzo[d]imidazol-5-yl)-5-(substituted)-1,3,4-Oxadiazoles: Synthesis, anticancer, antimicrobial and in silico studies
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Background: Cancer is a fatal disease for mankind; continuous research is still going on for the invention of potent anticancer drugs. In this view, 1, 3, 4-Oxadiazoles are privileged molecules which attracted medicinal chemists towards their anticancer p
- Kumar, Naveen,Sreenivasa, Swamy,Kalal, Bhuvanesh Sukhlal,Kumar, Vasantha,Holla, Bantwal Shivarama,Pai, Vinitha Ramanath,Mohan, Nadigar Revansiddappa,Govindaiah, Shivaraj
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- In vitro, in vivo and in silico-driven identification of novel benzimidazole derivatives as anticancer and anti-inflammatory agents
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The synthesis of novel benzimidazole derivatives with varied carbon chain length was achieved via “one-pot” nitro reductive cyclization (6a–o). In each case, compounds were determined by the elemental analyses, FT-IR, mass, 1H and 13
- Chandrashekarappa, Revanasiddappa B.,Merugumolu, Vijay K.,Poojary, Boja,Rangappa, Shobith,Sathyanarayana, Reshma,Srinivasa, Sudhanva M.
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- The Suzuki–Miyaura Cross-Coupling as the Key Step in the Synthesis of 2-Aminobiphenyls and 2,2'-Diaminobiphenyls: Application in the Synthesis of Schiff Base Complexes of Zn
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2-Nitrophenylboronic acids serve as interesting starting materials for the construction of biphenyl- and terphenyl-based amines if subjected to the Suzuki–Miyaura reaction. Unfortunately, these boronic acids suffer from low reactivity in Suzuki reactions, alongside their low stability in the presence of Pd. Herein, a general method for the construction of 2-nitro-substituted bi- and terphenyls is presented, with special emphasis on the synthesis of 2-amino-2'-nitrobi- and terphenyls. Comparisons are made with other boronic acids that have some of the aforementioned issues. Finally, the application of the obtained 2-amino-2'-nitrobi- and terphenyls as starting materials for the synthesis of bi- and terphenyl based di- and triamines is encountered for, with emphasis on the use of these amines as precursors for Schiff base ligands. In addition, the synthesis of some Zn complexes of these ligands is presented.
- Hylland, Knut Tormodss?nn,?ien-?degaard, Sigurd,Tilset, Mats
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supporting information
p. 4208 - 4226
(2020/07/06)
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- Microwave-assisted synthesis of benzimidazole derivatives through nitro reductive cyclization and their biological study
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A simple, effective, and eco-friendly synthesis of new benzimidazole-bearing aromatic/heteroaromatic compounds (4 a-o) using sodium dithionite as an effective reductive cyclizing reagent in dimethyl sulfoxide under microwave method is described. The newly
- Manju,Kalluraya, Balakrishna,Asma,Kumar, Madan S
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p. 415 - 422
(2018/09/25)
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- Novel benzimidazole-oxadiazole hybrid molecules as promising antimicrobial agents
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In the present study, we describe the design and expeditious synthesis of novel 2-aryl-5-(3-aryl-[1,2,4]-oxadiazol-5-yl)-1-methyl-1H-benzo[d]imidazole hybrid molecules as promising antimicrobial agents. The core moiety 2-aryl-ethyl-1H-benzo[d]imidazole-5-
- Shruthi,Poojary, Boja,Kumar, Vasantha,Hussain, Mumtaz Mohammed,Rai, Vaishali M.,Pai, Vinitha R.,Bhat, Mahima,Revannasiddappa
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p. 8303 - 8316
(2016/02/09)
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- Novel arylalkylamine compounds exhibits potent selective antiparasitic activity against Leishmania major
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Leishmania major (L. major) is a protozoan parasite causal agent of Leishmaniasis. It is estimated that 12 million people are currently infected and around 2 million infections occur each year. Current treatments suffer of high toxicity for the patient, low efficacy toward the parasite, high cost, and are losing effectiveness due to parasite resistance. Discovering novel small molecule with high specificity/selectivity and drug-like properties for anti-leishmanial activity remains a significant challenge. The purpose of this study is to communicate the design and synthesis strategies of novel chemical compounds based of the arylalkylamine scaffold with selective toxicity towards L. major and less toxicity to human cells in vitro. Here, we have developed a structure activity relationship (SAR) study of arylalkylamine AA1 in order to study their anti-parasitic effect in L. major. Overall, 27 arylalkylamine compounds derived from AA1 were synthesized and purified by silica gel column chromatography. The purity of each analog was confirmed by spectroscopic methods (1H, 13C NMR and LC/MS). Among these analogs, the compound AA9 showed the best toxic activity on L. major (LD50 = 3.34 μM), which represents a 9 fold higher lethality as compared with its parental AA1 (Fer-1) compound (LD50 = 28.75 μM). In addition, AA9 showed no significant toxicity at 80 μM on U20S Human Osteoblasts, Raw 264.7 Macrophages or intraperitoneal macrophages. In summary, our combined SAR study and biological evaluation data of AA1-AA27 compounds allow the identification of novel arylalkylamine compound AA9 that exhibits potent cytotoxicity against L. major promastigote with minimum toxic effect on human cells.
- Iniguez, Eva A.,Perez, Andrea,Maldonado, Rosa A.,Skouta, Rachid
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supporting information
p. 5315 - 5320
(2015/11/09)
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- BENZOTHIAZIN-3-ONE COMPOUND AND INTERMEDIATE THEREFOR
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A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): (wherein n is 3 or 4; R represents ethyl or hydrogen; and R 1 represents hologeno, alkoxy, haloalkyl, or haloalkoxy) or a pharmaceutically acceptable salt thereof. It is useful as a therapeutic or preventive agent for arthrosis deformans, chondrodegenerative discases such as chronic articular rheumatism, cancers, gingivitis, etc. Also provided are an intermediate for the compound and a process for producing the compound.
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Page/Page column 47
(2008/06/13)
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- INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USES THEREOF
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The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 70-71
(2010/02/14)
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- Synthesis and potent antimicrobial activity of some novel methyl or ethyl 1H-benzimidazole-5-carboxylates derivatives carrying amide or amidine groups
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A series of benzimidazole-5-carboxylic acid alkyl ester derivatives carrying amide or amidine substituted methyl or phenyl groups at the position C-2 were synthesised and evaluated for antibacterial and antifungal activities against S. aureus, methicillin
- Oezden, Seckin,Atabey, Dilek,Yildiz, Sulhiye,Goeker, Hakan
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p. 1587 - 1597
(2007/10/03)
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- BICYCLIC IMIDAZOL DERIVATIVES AGAINST FLAVIVIRIDAE
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Disclosed are compounds, compositions and methods for treatingFlaviviridae family virus infections.
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Page/Page column 87; 126
(2008/06/13)
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- Bivalent inhibitors of Glutathione-S-Transferases
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Bivalent inhibitors having affinity for one or more dimeric GST isozymes are provided. The bivalent inhibitors comprise two ligand domains connected by a molecular linker, wherein the ligand domains have affinity for one or more monomers in the one or mor
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Page/Page column 19
(2010/02/10)
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- ANABASEINE DERIVATIVES USEFUL IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
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The compounds of the present invention are of formula (I): wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.
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Page/Page column 78; 79
(2008/06/13)
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- INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF
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The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page 105;106
(2008/06/13)
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- Novel antiprotozoal products: imidazole and benzimidazole N-oxide derivatives and related compounds.
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The syntheses and biological evaluation of the first anti-protozoa imidazole N-oxide and benzimidazole N-oxide and their derivatives are reported. They were tested in vitro against two different protozoa, Trypanosoma cruzi and Trichomonas vaginalis. Deriv
- Aguirre, Gabriela,Boiani, Mariana,Cerecetto, Hugo,Gerpe, Alejandra,Gonzalez, Mercedes,Sainz, Yolanda Fernandez,Denicola, Ana,De Ocariz, Carmen Ochoa,Nogal, Juan Jose,Montero, David,Escario, Jose Antonio
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p. 259 - 270
(2007/10/03)
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- Fused-ring compounds and use thereof as drugs
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The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. Th
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- Viral polymerase inhibitors
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An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein R1 is selected from: H, haloalkyl, (C1-6)alkyl, (C2-6)alkenyl, (C3-7)cycloalkyl, (C2-6)alkynyl, (C5-7)cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C6-10)bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR5, wherein R5 is H, halogen, haloalkyl, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; X is N or CR5; D is N or CR5; each of Y1 and Y2 is independently O or S; Z is O, N, or NRz wherein Rz is H, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; R3 and R4 are each independently H, (C1-6)alkyl, first (C3-7)cycloalkyl or 6- or 10-membered aryl, Het (C1-6)alkyl-6- or 10-membered aryl, (C1-6)alkyl-Het; or each R3 and R4 are independently covalently bonded together to form second (C3-7)cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R3 or R4 are independently covalently bonded thereto to form a nitrogen-containing heterocycle; R7 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; or R7 is covalently bonded to either of R3 or R4 to form a heterocycle; A is (C1-6) alkyl-CONHR8 wherein R8 is-6- or 10-membered aryl, or Het; or A is a 6- or 10-membered aryl, or Het said aryl or Het being optionally substituted; or a salt or a derivative thereof; such compounds being potent inhibitors of HCV NS5B polymerase.
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- Novel benzimidazole derivatives and pharmaceutical compositions comprising these compounds
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The present invention relates to novel benzimidazole derivatives, pharmaceutical composition containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
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- Ceric(IV) ammonium nitrate mediated transesterification and esterification
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The transesterification of carboxylic esters and the esterification of carboxylic acids are effected under mild conditions in the presence of ceric(IV) ammonium nitrate (CAN).
- Stefane, Bogdan,Kocevar, Marijan,Polanc, Slovenko
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p. 1703 - 1707
(2007/10/03)
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- Benzimidazole derivative, hair growth promoter and external composition for skin using the same
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A benzimidazole derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30expressed by R1and the other is —(CH2)n—NR2R3; R
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- Synthesis of some novel tetrahydronaphthalene benzimidazole derivatives
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Retinoids, synthetic and natural analogues of all-trans-retinoic acid (RA), exert their biological effects with responsive elements of DNA to promote on cell differentiation and proliferation and behave as potent adipogenic hormones. Herein, we describe the synthesis of a number of novel tetrahydrotetramethylnaphthalene benzimidazole derivatives as retinoids. Analogs were prepared as depicted in Scheme 1 and 2. As is evident from both shemes, a variety of tetrahydrotetramethylnaphthalene benzimidazole derivatives have been synthesized by using an appropiate NaHSO3 addiction product.
- Ates-Alagoz, Zeynep,Buyukbingol, Erdem
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p. 455 - 460
(2007/10/03)
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