Synthesis of novel antimicrobial 7-But-2-ynyl-1-(substituted-benzyl)-3-methyl-8-morpholin-4-yl-1H -purine-2,6-diones

In this study, we synthesized 7-But-2-ynyl-3-methyl-8-morpholin-4-yl-3,4,5,7-tetrahydro-purine-2,6-diones from 8-Bromo-7-but-2-ynyl-3-methyl-3,4,5,7-tetrahydro-purine-2,6-dione and morpholine using lithium hydroxide and DMSO as a medium. We further coupled 7-But-2-ynyl-3-methyl-8-morpholin-4-yl-3,4,5,7-tetrahydro-purine-2,6-dione with different halo compounds to obtain various derivatives. These synthesized compounds were then tested for their antimicrobial activities against S. aureus, B. subtilis, S. typhi, and E. coli

Synthesis of 3-methyl-4H-benzo[b][1,4]thiazine-2-carboxylates Using CAN as a Catalyst and Its Conversion Into Guanidines

Background: 1,4-benzothiazine carboxylates show wide application in the field of medicinal chemistry. Therefore, we have designed convenient and efficient method for the synthesis of 1,4-benzothiazine carboxylates. Objective: Synthesis of 1,4-benzothiazine carboxylates and its guanidines by simple and facile method using efficient catalyst. Methods: Derivatives of 1,4-benzothiazine carboxylates were synthesized by cyclocondensing β- keto esters with 2-aminobenzenethiols using CAN as a catalyst at room temperature. 1,4-benzothiazine carboxylate, condensed with guanidine hydrochloride in the presence of sodium methoxide in DMF to obtained new 3-substituted-l-4H-benzo[b][1,4]thiazine-2-carboxyguanidines (88-91%). Results: All the products were obtained with good to excellent yields within 40 min. Here, CAN oxidizes aminothiophenol into disulfide and then nucleophilic attack of enolic form of β-ketoesters on the disulphide and 1, 4-benzothiazine acetates, were obtained with good yields. Conclusion: We have designed convenient and efficient method for the synthesis of 1,4-benzothiazine carboxylates. Most remarkable features of this cyclocondensation such as use of efficient catalyst and non-volatile solvent under mild reaction condition to obtain excellent yield. </jats:sec

Synthesis and Anti-Tubercular Screening of 8-Benzyloxy-5-[2-(Substituted-Phenyl)-Thiazol-4-yl]-1<i>H</i>-Quinolin-2-One Derivatives

Novel 8-Benzyloxy-5-[2-(substituted-phenyl)-thiazol-4-yl]-1H-quinolin-2-one derivatives are synthesized by the cyclocondensation of substituted thiobenzamide and in-situ generated 8-benzyloxy-5-(2-bromo-acetyl)-1H-quinolin-2-one in the ethanol using simple one-pot multicomponent protocol under catalyst-free reaction conditions. All the products were screened for anti-tuberculosis (TB) activity against Mycobacterium tuberculosis H37Rv stains using L. J. medium conventional method and Compound 4h show good and Compound 4a, 4c, 4e, 4g, 4i, and 4j are also showing significant activity against M. tuberculosis.</p