Department of Chemistry
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Item Synthesis of 1,5-benzothia/oxazepines as potent neuroleptic agents(NISCAIR, 2003-05) Bajaj, KiranSome new 2-(4'-oxo-2'-substitutedaryl-thiazolidinyl)iminomethyl-1 ,5-benzothialoxazepin-4(5H)-ones 5a-d/5a'-d' and 2-(4'-oxo-3'-chloro-2'-substitutedaryl-azetidinyl)-imino-methyl-l ,5-benzothialoxazepin-4(5H)-ones 6a-dl6a' -d' have been synthesized starting from 2-aminobenzenethioVphenol and evaluated for their neuroleptic activity. The structures of the synthesized compounds are confirmed by IR, 1H NMR and mass spectrometery and also by chemical methods.Item Synthesis of Newer Indolyl/ Phenothiazinyl Substituted 2-Oxo/ Thiobarbituric Acid Derivatives as Potent Anticonvulsant Agents(Thieme, 2003) Bajaj, Kiran2-Amino-5-(heteroarylmethylene)-1,3,4-oxadiazoles/thiadiazoles 7−10 were synthesized by cyclisation of 1-(heteroarylacetyl)semicarbazides/thiosemicarbazides 3−6. 5-(2’-Heteroarylmethylene-5’-aminomethylene-1’, 3’, 4’-oxadiazol-2’-yl/ thiadiazol-2’-yl)-2-oxo/thiobarbituric acids 11−18 were synthesized by condensation of compounds 7−10 at the 5th position of 2-oxo/thiobarbituric acids. The newly synthesized compounds showed anticonvulsant activity ranging from 50–90 % (seizures protection). Compound 18 (5-(2’-phenothiazinylmethylene-5’-aminomethylene-1’,3’,4’-thiadiazol-2’-yl)-2-thiobarbituric acid) showed maximum activity being more potent than the reference drug phenytoin sodium (CAS 630-93-3)Item Synthesis of some new benzothia/oxazepinyl indoles as an antipsychotic agents(NISCAIR, 2003-07) Bajaj, KiranSome new 3-(2'-substitutedaryl -2',3'-dihydro-1 ',5'-benzothia/oxazepin-4'-yl)indoles 3a-h, 3-(2'-substitutedary 1-3'substitutedarylaminomethylene-2' ,3'-dihydro-1',5'-benzothia/oxazepin-4'-yl)indoles 4a-p and 3-(2'-substitutedary 1-3'substitutedarylazo- 2',3'- dihydro-1',5'- benzothia/oxazepin-4'-yl)indoles 5a-p have been synthesized and evaluated for antipsychotic activity. 3-[2'-( 4"-N,N-dimethylphenyl)-3' -arylaminomethylene-2',3'-dihydro-1 ,5-benzothiazepin-4'-yl] indole 4i showes most promising antipsychotic activity. The structures of all the compounds were determined by IR,1H NMR and mass spectrometry.Item Synthesis and anti-inflammatory, analgesic, ulcerogenic and cyclooxygenase activities of novel quinazolinyl-2-pyrazolines(NISCAIR, 2002-03-13) Bajaj, KiranItem Synthesis of some newer derivatives of 2-amino benzoic acid as potent anti-inflammatory and analgesic agents.(PMC, 2003-11-01) Bajaj, KiranDiazotization of N-benzylidene anthranilic acids 1a-1n at pH 9 yielded N-[alpha-(phenylazo) benzylidene] anthranilic acids 2a-2n and at pH 3 yielded N-benzylidene-5-(phenylazo) anthranilic acids 3a-3n. When compounds 3a-3n were treated with thioglycolic/thiolactic acid in the presence of anhydrous ZnCl(2), 2-(4-oxo-2-phenylthiazolidin-3-yl)-5-(phenylazo) benzoic acids 4a-4n were afforded. The newly synthesized compounds were screened for their anti-inflammatory and analgesic activities and were compared with standard drugs, aspirin and phenylbutazone. Out of the compounds studied, the most active compound 4n showed more potent activity than the standard drugs at all doses tested.Item Synthesis and psychotropic evaluation of some new N-substitutedbenzothia/oxazepinylphenothiazines(NISCAIR, 2004-01) Bajaj, KiranA number of N-[2-substitutedaryl-3-substitutedarylaminomethylene-2, 3-dihydro- 1, 5-benzothia/oxazepin-4-yl] phenothiazines 4a-p and 4a'-p' have been synthesized from N-[2-substitutedaryl-2, 3-dihydro-1, 5-benzothia/ oxazepin-4-yl]phenothiazines by Mannich reaction, on the 3rd position of benzothia/oxazepine ring. The structure of these compounds have been confirmed by IR, 1H NMR and Mass analysis. The newly synthesized compounds have been evaluated for their psychotropic activities and acute toxicity studies. Compound 4i is found to be most potent compound of this series.Item Synthesis of acridinyl-thiazolino derivatives and their evaluation for anti-inflammatory, analgesic and kinase inhibition activities(Elsiever, 2005-07-01) Bajaj, KiranVariety of N-(4-phenyl-3-(2′,3′,4′(un)substituted phenyl)thiazol-2(3H)-ylidene)-2,4(un)substituted acridin-9-amine (4a–o) and 1-[(2,4-(un)substituted acridin-9-yl)-3-(4-phenyl-3-(2′,3′,4′(un)substituted phenyl)thiazol-2(3H)-ylidene)]isothiourea (5a–h) derivatives have been synthesized by condensation of 4-phenyl-3-(2′,3′,4′(un)substituted phenyl)thiazol-2(3H)-imine (3a–g) with 9-chloro-2,4-(un)substituted acridine (1a–c) and 9-isothiocyanato-2,4-(un)substituted acridine (2a–d), respectively. All these compounds were characterized by correct 1H NMR, FT-IR, MS and elemental analyses. These compounds were screened for anti-inflammatory, analgesic and kinase (CDK1, CDK5 and GSK3) inhibition activities. Some compounds exhibited good anti-inflammatory (25–32%) and potent analgesic (50–75%) activities, at 50 mg/kg p.o. A compound, 4o (R1 = H, R2 = OCH3, R3 = CH3, R4 = CH3, R5 = H) exhibited moderate CDK1 (IC50 = 8.5 μM) inhibition activity.Item Synthesis And CNS Depressant Of Newer Spirobarbiturates(IJPS, 2005) Bajaj, KiranIn an effort to search for more active CNS depressants, a series of spirobarbiturates incorporated with thiazolidinones and azetidinones were synthesized and evaluated for their sedative, hypnotic and anticonvulsant activities. Starting bis compounds (1a-d) were prepared from the reaction of acetone and substituted aldehydes. These bis compounds on Michael addition with barbituric acid give rises to triones (2a-d), which on condensation with NH2NH2.H2O afforded (3a-d) which on reaction with different aromatic aldehydes afforded and Schiff bases (4a-n). These on cyclocondensation with thiolactic acid and chloroacetyl chloride furnished the final products (5a-n) and (6a-n), respectively. Result of toxicity studies and central nervous system depressant activities of these compounds are reported. The structures of the products have been delineated by chemical reaction, elemental analysis and spectral studies.Item Quinine bis-conjugates with quinoloneantibiotics and peptides: synthesis and antimalarial bioassay(RSC, 2012) Bajaj, KiranBenzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC50 values ranging from 12 to 207 nM, similar to quinine itself.Item Microwave Assisted Synthesis of Five Membered Azaheterocyclic Systems(Bentham Science, 2012) Sakhuja, Rajeev; Bajaj, KiranThe present review provides a comprehensive summary of microwave-assisted preparation of five-membered azaheterocyclic systems, such as pyrrole, pyrazole, imidazole, triazole, thiazole, isothiazole, oxazole, isoxazole, oxadiazole, thiadiazole and tetrazole.