Synthesis and structure–activity relationships of new antimicrobial active multisubstituted benzazole derivatives

Synthesis and In vitro Antimicrobial Activity of Novel 2-(4-(Substituted-carboxamido)benzyl / phenyl)benzothiazoles

“…Among the tested compounds, 2-(phenoxymethyl)benzothiazole was found the most active derivative at a MIC value of 3.12 µg/ml against the tested S. aureus. 8 Moreover, the same compound was found very potent as an eukaryotic topoisomerase II inhibitor exhibiting a better inhibitor activity than reference drug [18][19][20] etoposide.…”

“…Hence, the development of novel, potent, and unique antibacterial agents is the preeminent way to overcome bacterial resistance and develop effective therapies. 5 The compounds possess benzothiazole nucleus in their structure are involved in research aimed at evaluating new chemotherapeutically active agents: such as antimicrobial [6][7][8][9] a topical carbonic anhydrase inhibitor, 10 a cyclooxygenase inhibitor, 11 antitubercular, 12,13 antinematode, 14 a dual inhibitor of thromboxane A 2 synthetase and 5-lipoxygenase 15 , a selective and reversible inhibitor of monoamine oxidase type A (MAO-A), 16 antiallergic, 17 multi-drug resistance cancer cell activities with inhibiting activity on eukaryotic topoisomerase II enzyme in cell-free system [18][19][20] and antitumor agents. [21][22][23] Currently, a new series of benzothiazoles have been synthesized as antitumor agents and showed potent inhibitory activity against human breast cancer cell lines in vitro and in vivo.…”

“…21 Among them, lysyl-amide of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (Formula 1) had been selected for phase 1 clinical evaluation. 22 In the last years, we reported the synthesis of several 2-substitutedbenzothiazole derivatives as the anti- microbial agents 7,8 as seen in Formula 2. According to these studies the compounds were found to have inhibitory effect with MIC value of 3.12-50 µg/ml against some of Gram-positive, Gram-negative bacteria and Candida albicans as yeast.…”

The efficient o-benzenedisulfonimide catalysed synthesis of benzothiazoles, benzoxazoles and benzimidazoles

“…1 In particular, they are a common heterocyclic scaffold in biologically active and medicinally significant compounds 2a and are found in a large variety of natural products. 2b Moreover, these groups of heterocyclic compounds exhibit a wide range of pharmacological properties, which include antiviral, 3 antimicrobial, 4 antitumor, 5 antibiotic, 6 antifungal, 7 anticonvulsant, 8 anti-inflammatory activity 9 and many others. 10,11 Their use in the field of advanced materials is also worthy of note.…”

Silica Supported Fluoroboric Acid: An Efficient and Reusable Heterogeneous Catalyst for Facile Synthesis of 2-Aliphatic Benzothiazoles, Benzoxazoles, Benzimidazoles and Imidazo[4,5-b]pyridines

“…1,2 These heterocycles have achieved significance in pharmacology as antibacterial, 3 antiviral, 4 antifungal, 5 anticancer, 6 anticonvulsant 7 and immunosuppressant agents. 8 Quite a plethora of methods have been developed for the preparation of these heterocycles including the condensation of carboxylic acids, 9 acid chlorides, 10,11 orthoesters, [12][13][14] esters, 15 and aldehydes [16][17][18][19][20][21] with o-aminophenols, o-aminothiophenols and o-phenylenediamines, dehydration of o-acylaminophenols, 22 the reaction of o-quinones with amines 23 and Beckmann rearrangement of o-acylphenoloximes.…”