Amidino benzimidazole inhibitors of bacterial two-component systems

Synthesis and in vitro Study of Novel Thiophenyl Benzoimidazolyl Benzamides, Acrylamides and Propionamides as Antimicrobial Agents

“…2-[(4-Benzoyl-5-ethylthiophen-2-yl)carbamoyl]-acrylic acid (4) and propionic acid (6) were prepared similarly following the same reaction conditions as described for compound 2.…”

Synthesis and Potent In vitro Activity of Novel 1H‐Benzimidazoles as Anti‐MRSA Agents

“…These acids were converted into acyl chlorides with SOCl 2 , and reaction between the corresponding acyl chlorides and 3-amino-propionitrile fumarate salt resulted in the required benzamides 8-10. The CN group of these benzamides was converted into aliphatic amidine by using well-known Pinner method, [11][12][13][14][15][16][17][18]. Nucleophilic displacement of the chloro group of 2,4,5-trichloronitrobenzene with 1-naphtylmethylamine in DMF gave 19 (Scheme 2).…”

“…Some novel amidinobenzimidazoles (V) have been identified as inhibitors of bacterial KinA ⁄ SpoOF two-component system that includes a histidine protein kinase and a response regulator (RR). Histidine protein kinase and RR enable bacteria to adapt to the environmental changes and survival within the host (16). These amidino inhibitors display good in vitro antibacterial activity, in particular, against Gram-positive bacteria (i.e., S. aureus, MRSA, VRE).…”

“…These results prompted us to investigate a series of new benzimidazoles substituted with aliphatic amidines (11)(12)(13)(14)(15)(16)(17)(18), benzamides (26-30), and benzamidines (32-33), with multiple chloro substituents at different positions to evaluate their antistaphylococcal and antifungal activities.…”

Synthesis and Biological Evaluation of Some New Class of Chromenoimidazole Derivatives as Probable Anti Cancer Agents

“…15 Presence of amidino moiety on benzimidazole nucleus possess antimicrobial and anti protozoal activity. 16 Aryl or alkyl carboxamide benzimidazole derivatives possess potent antihypertensive activity by inhibiting angiotensine II. 17 Nitro benzimidazoles were reported to possess antitumor activity.…”