Synthesis of potential antitubercular and antimicrobial s-triazine-based scaffolds via Suzuki cross-coupling reaction

Synthesis, characterization and in vitro biological evaluation of some new 1,3,5-triazine-chalcone hybrid molecules as Mycobacterium tuberculosis H37Rv inhibitors

“…The chief intermediate in the present study 1-(4-(4,6-dichloro-1,3,5-triazin-2-ylamino) phenyl)ethanone (3) was prepared by reaction between cyanuric chloride i.e. 2,4,6-trichloro-1,3,5-triazine (1) and 4-aminoacetophenone (2) [10]. Further, successive base catalyzed Claisen-Schmidt condensation of the compound 3 with appropriate substituted aromatic/heteroaromatic aldehydes in the presence of 100% potassium hydroxide solution in ethanol afforded a series of 1-(4-(4,6-dichloro-1,3, 5-triazin-2-ylamino)phenyl)-3-(substituted)-2-propen-1-ones (4a-ii) in good yield.…”

“…In recent past, 2,4,6-trisubstituted-1,3,5-triazine scaffolds were discovered as a potent inhibitors of Mycobacterium tuberculosis (Mtb) H37Rv [10]. Currently 1,3,5-triazine derivatives have been found to possess wide range of biological activities, such as adenosine receptor antagonist [11], antiamoebic [12], anticancer [13], antileishmanial [14], antimalarial [15], antimicrobial [16], antiviral [17], antitubercular [18], carbonic anhydrase inhibitor [19], cathepsin B inhibitor [20], cholesteryl ester transfer protein inhibitor [21], corticotropin-releasing factor ligand [22], CRF1 PET imaging agent [23], cytosolic phospholipase A2α inhibitor [24], dipeptidyl peptidase IV inhibitor [25], bacterial enzyme DNA helicase inhibitor [26], dual PI3/mTOR inhibitor [27], glucocerebrosidase inhibitor [28], α-glucosidase inhibitor [29], growth factor inhibitor [30], human gonadotropin-releasing hormone receptor antagonist [31], 5-HT7 receptor antagonist [32], inosine monophosphate dehydrogenase inhibitor [33], mTOR kinase inhibitor [34],…”

2-Aminobenzothiazole derivatives: Search for new antifungal agents

“…In this perspective, for example, we recently determined the X-ray crystallographic structure of Enterococcus faecalis thymidylate synthase, which should be a potential target for antibacterial therapy [1]. Many heterocyclic nuclei, such as 1,3,4-thiadiazole, benzimidazole, 1,3,5-triazine, and benzothiazole have been recently reviewed as antimicrobial agents [2,3]. Our attention was focused to the benzothiazole nucleus [4].…”

Synthesis and Study of 1,2,4-Triazine and Thiadiazoles Based Derivatives of S-Triazine as Antimicrobial Agents

“…For example, these compounds possess potent antiprotozoal [4] antimalarial [5,6] antiviral [7][8][9] anticancer [10,11] antimicrobial [12][13][14] anti-tuberculosis [15,16]. Recently, significant therapeutic potential for central nervous system (CNS) disorders.…”