pathogenic infections and inflammation are very common ailments humans suffer. upsurge of resistant pathogens has impeded the antimicrobial drug development process in recent years and the search of new antimicrobial agents is clearly evident from the literature. in line with these developments the synthesis of n-substituted aryl-2-({4-[(substituted aryl carbamoyl) methyl]-5-(pyridin-4-yl)-4h-1...

A novel family of chiral ortho-substituted BINAPO ligands (o-BINAPO) were synthesized from BINOL, and their Ru complexes were highly efficient catalysts for asymmetric hydrogenation of beta-aryl-substituted beta-(acylamino)acrylates and beta-aryl-substituted beta-keto esters. The Ru-bisphosphinite catalysts can tolerate an E/Z mixture of beta-aryl-substituted beta-(acylamino)acrylates. These hi...

Irradiation of substituted 2-benzylidenecyclopentanone O-alkyl and O-acetyloximes in methanol provides a convenient synthesis of alkyl, alkoxy, hydroxy, acetoxy, amino, dimethylamino and benzo substituted annulated quinolines. para-Substituents yield 6-substituted-2,3-dihydro-1H-cyclopenta[b]quinolines with 8-substituted products being obtained from ortho-substituted starting materials. Reactio...

Hammett constants (σ) can be important factor to understanding substitution and position effects on benzoic acid. This report describes a computational study of ∆G◦ and σ for six substituted benzoic acid (X= F,Cl ,OH ,NH2 ,CN,NO2 )and phenylacetic acid substituted (X=OH ,NH2 ) at para and meta positions ingas and aqueousphases by DFT method and comparesit to available experimental and theoretic...

Reaction of 2-hydrazinocarbonyl-3-chloro-5-phenoxy-benzo[b] thiophene with different substituted phenyl isothiocyanate gave N-substituted arylthiosemi-carbazide derivatives (1a-h). 1,3,4-Thiadiazole derivatives (2a-h) were prepared by the cyclization of arylthiosemicarbazides (1a-h) with concentrated sulphuric acid. All the compounds were screened for their antitubercular activity against Mycob...

A series of 5-substituted-4-amino-1,2,4-triazole-3-thioesters was synthesized by converting variously substituted organic acids successively into the corresponding esters, hydrazides, 5-substituted-1,3,4-oxadiazole-2-thiols, 5-substituted-1,2,4-triazole-2-thiols and 5-substituted-1,3,4-oxadiazole-2-thioesters. Finally the target compounds were obtained by refluxing 5-substituted-1,3,4-oxadiazol...

H. Piperidine Analogues of Phenyltropanes 967 III. Cocaine Analogues 969 A. Stereoisomers of Cocaine 970 B. Phenyl Ring Substituted Cocaines 970 C. 2â-Substituted Cocaines 973 1. 2â-Substituted Cocaines 973 2. 2â-Substituted 4′-Iodococaines 977 D. N-Modified Cocaines 978 E. 3â-Carbamoyl Analogues of Cocaine 981 F. 3â-Alkylphenyltropanes 982 G. 6/7-Substituted Cocaine and Pseudococaine 982 H. 6-...

A series of N-substituted-2,4-thiazolidinedione derivatives (TZDs) were prepared via N-alkylation of 2,4-TZD at position 3 using substituted benzyl halides. Synthesized N-substituted-2,4-TZD was then substituted at position 5 with substituted aromatic aldehyde according to Knoevenagel condensation method. Structures of the compounds were elucidated using various spectral techniques viz. IR, 1HN...

starting from readily available 2-substituted-4-methylthiazole-5-carboxylic acid hydrazide (1), the title compounds were prepared. the reaction of compound 1 (r=ch3) with formic acid yielded 1-(formyl)-2-(2,4-dimethylthiazole-5-carboxyl) hydrazine (2). refluxing the latter with phosphorous pentasulfide in xylene afforded compound 3, the reaction of compound 2 with phosphorous pentoxide afforded...

A new series of 2-(ortho & para substituted phenoxy)1-(3-(3-chloro-4-methoxyphenyl)-5-(substituted phenyl)-4,5dihydropyrazol-1-yl)ethanone were synthesized. Ortho and para substituted phenol was refluxed with ethylchloroacetate in dry acetone in presence of anhydrous potassium carbonate to yield ethyl (ortho & para substituted phenoxy) acetate (1). The substituted ester on reaction with hydrazi...