{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,26]],"date-time":"2025-10-26T14:59:31Z","timestamp":1761490771887},"reference-count":26,"publisher":"Bentham Science Publishers Ltd.","issue":"2","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["CNSAMC"],"published-print":{"date-parts":[[2019,8,6]]},"abstract":"<jats:sec><jats:title>Background:<\/jats:title><jats:p>Approach for green chemistry for chemical synthesis is found to be very efficient as it makes the reaction more easily, less tedious, maximize desired products and minimize by-products.<\/jats:p><\/jats:sec><jats:sec><jats:title>Materials &amp; Methods:<\/jats:title><jats:p>Utilizing this approach 1, 5-benzodiazepines and its derivatives have been synthesized and evaluated for skeletal muscle and antianxiety activity. 1, 5-benzodiazepine derivatives have attracted great attention due to its diversity of pharmacological activities and its application in heterocyclic synthesis and medicines. The target compounds were synthesized by first reacting o-phenylenediamine with acetophenone to yield 1, 5-benzodiazepines. In the next step the NH of 1, 5-benzodiazepines were chloroacetylated and then the chloro group was substituted with different anilines. The structures were confirmed on the basis of their TLC, IR, 1H NMR and CHN elemental studies. The physicochemical parameters were determined for BBB penetration through online software.<\/jats:p><\/jats:sec><jats:sec><jats:title>Results:<\/jats:title><jats:p>The Log P values of the compounds tested showed that compounds have the potential to be CNS active. The compounds were evaluated for the skeletal muscle relaxant activity and antianxiety activity. It was investigated that 1, 5-benzodiazepines derivatives possess significant differences between control group and treated group.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion:<\/jats:title><jats:p>Among these derivatives, the compound bearing chloro group possesses the highest skeletal muscle relaxant and antianxiety activity.<\/jats:p><\/jats:sec>","DOI":"10.2174\/1871524919666190227234238","type":"journal-article","created":{"date-parts":[[2019,3,4]],"date-time":"2019-03-04T12:03:15Z","timestamp":1551700995000},"page":"146-151","update-policy":"http:\/\/dx.doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Glacial Acetic Acid Catalyzed Synthesis, Physicochemical and Biological Evaluation of Benzodiazepines as Potent CNS Agents"],"prefix":"10.2174","volume":"19","author":[{"given":"Vipin","family":"Kumar","sequence":"first","affiliation":[{"name":"Faculty of Pharmacy, IFTM University, Moradabad-244001, India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shweta","family":"Verma","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, IFTM University, Moradabad-244001, India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sushil","family":"Kumar","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, IFTM University, Moradabad-244001, India"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"965","reference":[{"key":"ref=1","author":"de Baun J.R.","unstructured":"de Baun J.R.; Pallos F.M.; Baker D.R.; \u201c5-furoyl-2,2,4-trimethyl- 1,4-dihydro-1H-1,5-benzodiazepine as an anti-inflamma-tory agent,\u201d 1976, US Patent 3,978,227. Available from: scholar_lookup?title=5-furoyl-2%2c2%2c4-trimethyl-1%2c4-dihyd ro-1H-1%2c5-benzodiazepine+as+an+anti-inflammatory+agent"},{"key":"ref=2","first-page":"5498d","volume":"86","author":"de Baun J.R.","year":"1977","unstructured":"de Baun J.R.; Pallos F.M.; Baker D.R.; 5-furoyl-2,2,4-trimethyl-1,4-dihydro-1H-1,5-benzodiazepine as an anti-inflamma-tory agent. Chem Abstr 1977,86,5498d","journal-title":"Chem Abstr"},{"key":"ref=3","doi-asserted-by":"crossref","DOI":"10.1007\/978-3-642-68426-5","author":"Schultz H.","year":"1982","unstructured":"Schultz H.; Benzodiazepines 1982","journal-title":"Benzodiazepines"},{"key":"ref=4","author":"Smiley R.K.","year":"1979","unstructured":"Smiley R.K.; Comprehensive Organic Chemistry 1979","journal-title":"Comprehensive Organic Chemistry"},{"key":"ref=5","author":"Landquist J.K.","year":"1984","unstructured":"Landquist J.K.; Comprehensive Heterocyclic Chemistry 1984","journal-title":"Comprehensive Heterocyclic Chemistry"},{"key":"ref=6","author":"Randall L.O.","year":"1973","unstructured":"Randall L.O.; Kappel B.; Benzodiazepines 1973","journal-title":"Benzodiazepines"},{"key":"ref=7","author":"Haris R.C.","unstructured":"Haris R.C.; Straley J.M.; Lifting apparatus. 1968, US Patent 1,537,757, Available from: lookup?title=Lifting+apparatus"},{"key":"ref=8","doi-asserted-by":"crossref","first-page":"3561","DOI":"10.1080\/00397919908085990","volume":"29","author":"El-Sayed A.M.","year":"1999","unstructured":"El-Sayed A.M.; Abdel-Ghany H.; El-Saghier A.M.M.; A novel synthesis of pyrano(2,3-c)-, 1,3-oxazino(2,3 b)-,1,2,4- triazolo(3,4-b)-, oxazolo(2,3-b)-, furano(3,2-c)-, and 3-substituted- (1,5)benzo-diazepin-2-ones. Synth Commun 1999,29(20),3561-3572","journal-title":"Synth Commun"},{"key":"ref=9","doi-asserted-by":"crossref","first-page":"84","DOI":"10.1002\/cjoc.19990170112","volume":"17","author":"Xu J.X.","year":"1999","unstructured":"Xu J.X.; Wu H.T.; Jin S.; Cycloaddition of benzoheteroazepine II reactions and conformations of cycloadducts on 1, 5-benzothia-zepines and 1,5-benzodiazepines with nitrile imine and nitrile oxides. Chin J Chem 1999,17(1),84-91","journal-title":"Chin J Chem"},{"key":"ref=10","doi-asserted-by":"crossref","first-page":"404","DOI":"10.1002\/cjoc.19990170414","volume":"17","author":"Zhang X.Y.","year":"1999","unstructured":"Zhang X.Y.; Xu J.X.; Jin S.; Cycloaddition of benzoheteroazepine reaction of 2,3-dihydro-lh-l,5-benzodiazepines with dichlorocarbene and stereo-structures of products. Chin J Chem 1999,17(4),404-410","journal-title":"Chin J Chem"},{"key":"ref=11","first-page":"375","volume":"9","author":"Kim K.","year":"1998","unstructured":"Kim K.; Volkman S.K.; Ellman J.A.; Synthesis of 3-substituted 1,4-benzodiazepin-2-ones. J Braz Chem Soc 1998,9(4),375-379","journal-title":"J Braz Chem Soc"},{"key":"ref=12","doi-asserted-by":"crossref","first-page":"2902","DOI":"10.1002\/cber.19590921138","volume":"92","author":"Reid W.","year":"1959","unstructured":"Reid W.; Torinus E.; \u00dcber heterocyclische Siebenringsysteme, X. Synthesen kondensierter 5-, 7-und 8-gliedriger Heterocyclen mit 2 Stickstoffatomen. Chem Ber 1959,92(11),2902-2916","journal-title":"Chem Ber"},{"key":"ref=13","first-page":"2657","volume":"1","author":"Herbert J.A.L.","year":"1974","unstructured":"Herbert J.A.L.; Suschitzky H.; Syntheses of heterocyclic compounds substituted 2,3-dihydro-1h-1,5-benzodiazepines. J Chem Soc 1974,1,2657-2661","journal-title":"J Chem Soc"},{"key":"ref=14","doi-asserted-by":"crossref","first-page":"135","DOI":"10.3987\/R-1986-01-0135","volume":"24","author":"Morales H.R.","year":"1986","unstructured":"Morales H.R.; Bulbarela A.; Contreras R.; New synthesis of dihydro-and tetrahydro-1,5-benzodiazepines by reductive condensation of o-phenylenediamine and ketones in the presence of sodium borohydride. Heterocycles 1986,24(1),135-139","journal-title":"Heterocycles"},{"key":"ref=15","doi-asserted-by":"crossref","first-page":"1941","DOI":"10.1080\/00397919908086183","volume":"29","author":"Jung D.I.","year":"1999","unstructured":"Jung D.I.; Choi T.W.; Kim Y.Y.; In-Shik K.; You-Mi P.; Yong-Gyun L.; Doo-Hee J.; Synthesis Of 1,5-benzodiazepine derivatives. 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Tetrahedron Lett 2001,42(18),3193-3195","journal-title":"Tetrahedron Lett"},{"key":"ref=18","doi-asserted-by":"crossref","first-page":"5302","DOI":"10.1016\/j.tetlet.2008.06.082","volume":"49","author":"Pan X.Q.","year":"2008","unstructured":"Pan X.Q.; Zou J.P.; Huang Z.H.; Zhang W.; Ga(otf)3-promoted condensation reactions for 1,5-benzodiazepines and 1,5-benzothiazepines. Tetrahedron Lett 2008,49(36),5302-5308","journal-title":"Tetrahedron Lett"},{"key":"ref=19","doi-asserted-by":"crossref","first-page":"519","DOI":"10.1039\/b601993e","volume":"8","author":"Kumar R.","year":"2006","unstructured":"Kumar R.; Chaudhary P.; Nimesh S.; Verma A.K.; Chandra R.; An efficient synthesis of 1,5-benzadiazepine derivatives catalyzed by silver nitrate. Green Chem 2006,8(6),519-521","journal-title":"Green Chem"},{"key":"ref=20","doi-asserted-by":"crossref","first-page":"3833","DOI":"10.1081\/SCC-200034752","volume":"34","author":"Sivamurugan V.","year":"2004","unstructured":"Sivamurugan V.; Deepa K.; Palanichamy M.; Murugesan V.; [(l)proline]zn catalysed synthesis of 1,5-benzodiazepine derivatives under solvent-free condition. Synth Commun 2004,34(21),3833-3846","journal-title":"Synth Commun"},{"key":"ref=21","first-page":"1755","volume":"vol. 43, no.9","author":"Minothora P.","unstructured":"Minothora P.; Julia S.S.; Constantinos A.T.; An efficient method for the synthesis of 1,5-benzodiazepine derivatives under microwave irradiation without solvent. Tetrahedron Letters 2002,vol. 43, no.9,1755-1758","journal-title":"Tetrahedron Letters"},{"key":"ref=22","doi-asserted-by":"crossref","first-page":"1337","DOI":"10.1055\/s-2005-868516","volume":"8","author":"Chen W.Y.","year":"2005","unstructured":"Chen W.Y.; Lu J.; Molecular iodine catalyzed one-pot synthesis of 1, 5-benzodiazepine derivatives under solvent-free conditions. Synlett 2005,8,1337-1339","journal-title":"Synlett"},{"key":"ref=23","doi-asserted-by":"crossref","first-page":"1835","DOI":"10.1016\/S0040-4039(03)00096-0","volume":"44","author":"Jarikote D.V.","year":"2003","unstructured":"Jarikote D.V.; Siddiqui S.A.; Rajagopal R.; Thomas D.; Lahoti R.J.; Srinivasan K.V.; Room temperature ionic liquid promoted synthesis of 1,5-benzodiazepine derivatives under ambient conditions. Tetrahedron Lett 2003,44(9),1835-1838","journal-title":"Tetrahedron Lett"},{"key":"ref=24","doi-asserted-by":"crossref","first-page":"71","DOI":"10.1016\/j.molcata.2004.09.003","volume":"225","author":"Reddy B.M.","year":"2005","unstructured":"Reddy B.M.; Sreekamth P.M.; Reddy V.R.; Modified zirconia solid acid catalysts for organic synthesis and transformations. J Mol Catal A 2005,225,71-78","journal-title":"J Mol Catal A"},{"key":"ref=25","doi-asserted-by":"crossref","first-page":"1443","DOI":"10.3987\/COM-01-9253","volume":"55","author":"Kaboudin B.","year":"2001","unstructured":"Kaboudin B.; Navaee K.; Alumina\/phosphorus pentoxide (app) as an efficient reagent for the synthesis of 1,5-benzodiazepines under microwave irradiation. Heterocycles 2001,55(8),1443-1446","journal-title":"Heterocycles"},{"key":"ref=26","doi-asserted-by":"crossref","first-page":"901","DOI":"10.1055\/s-2004-816013","volume":"6","author":"Yadav J.S.","year":"2004","unstructured":"Yadav J.S.; Reddy B.V.S.; Praveenkumar S.; Nagaiah K.; Lingaiah N.; Saiprasad P.S.; Ag3pw12o40: A novel and recyclable heteropoly acid for the synthesis of 1,5-benzodiazepines under solvent-free conditions. 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