Synthesis and Biological Evaluation of Novel N' (4-aryloxybenzylidene)- 1H-Benzimidazole-2 Carbohydrazide Derivatives as Anti-Tubercular Agents

Abstract

A series of structurally novel, (E)-N'-(4-aryloxybenzylidene)-1H-benzimidazole-2-carbohydrazide derivatives were synthesized by molecular hybridization technique. All these compounds were evaluated against Mycobacterium tuberculosis H37Rv strains using Resazurin Microtiter assay (REMA) method. These compounds showed good antituberculosis activity with minimum inhibitory concentration (MIC) value of the range of 1.5-25 µg/mL.

Rationalization of Benzazole-2-carboxylate versus Benzazine-3-one/Benzazine-2,3-dione Selectivity Switch during Cyclocondensation of 2-Aminothiophenols/Phenols/Anilines with 1,2-Biselectrophiles in Aqueous Medium

“…On the other hand, the mixture of 1d and 5 in water at 60 °C was found to be homogeneous in the absence of SDOSS, justifying the independence of the presence of any surfactant for the reaction of 1d with 5 to form 6d . The reaction of 1d with 5 in EtOH under reflux has been claimed to form 3d that was used for subsequent reaction without any further characterization (e.g., IR, NMR, MS) . However, on the other hand, the treatment of 1d with 5 in EtOH under reflux afforded 6d (IR, NMR, MS) in 89% yield (Table , entry 32) instead of 3d .…”

“…The reaction of 1d with 5 in EtOH under reflux has been claimed to form 3d that was used for subsequent reaction without any further characterization (e.g., IR, NMR, MS). 27 However, on the other hand, the treatment of 1d with 5 in EtOH under reflux afforded 6d (IR, NMR, MS) in 89% yield (Table 4, entry 32) instead of 3d. Performing the reaction under the reported condition (reflux in EtOH for 4 h) 28 or extending the reaction time to 12 h led to the exclusive formation of 6d.…”

A Review on Benzimidazole Heterocyclic Compounds: Synthesis and Their Medicinal Activity Applications

“…Anti-Alzheimer's agents [192]- [194], Angiotensin II -AT1 Receptor Antagonist [195]- [200], Antiulcer activity [201]- [204], Anti-Tubercular activity [205]- [211],…”

“…In addition to the above medical applications, benzimidazole derivatives have been widely used as an essential part of biological applications including: antihypertensive activity, 154 155 156 157 158 antiprotozoal activity, 159–163 antiviral activity, 164–167 anthelmintic activity, 168 169 170 171 172 antidiabetic agents, 173 174 175 176 177 analgesic activity, 78 , 178 179 180 181 antispasmodic activity, 182 183 antidepressant activity, 184 185 186 187 188 189 sphingosine kinase 1 inhibitor, 190 191 anti-Alzheimer’s agents, 192 193 194 angiotensin II-AT1 receptor antagonists, 195 196 197 198 199 200 antiulcer activity, 201 202 203 204 anti-tubercular activity, 205 206 207 208 209 210 211 anti-HIV agents, 212 213 214 215 216 217 218 and anti-secretory activity. 219 220 221…”

Synthesis, Characterization, Anti-tubercular Evaluation, and Teratogenicity Studies of Novel 5-(4-fluorobenzoyl) tetrahydro benzamidazoquinazoline Derivatives

“…The creation and development of drugs with broad applicability in the pharmaceutical industry nowadays heavily relies on heterocyclic molecules. The therapeutic effects of benzimidazole derivatives as antibacterial, 5,6 antitubercular, [7][8][9] antitumor, 10 anthelmintic, 11 antihistaminic, 12 proton pump inhibitors, 12 anti-inflammatory, 13 anticancer, 14 antioxidant, 15 and antihypertensive 16 drugs have generated a great deal of attention in the medical community. Quinazolines serve as the building blocks for creating a variety of biologically active compounds and have played significant roles in medicinal chemistry.…”