ABSTRACT:
Antispasmodic medication is used to relieve urinary and bladder difficulties by relieving muscle spasms of the bladder. Several compounds of this family are known to possess antimicrobial potency in addition to their predesignated pharmacological actions. Based on this rationale present study is intended towards evaluating sedative, antibacterial and antifungal potency of an established antispasmodic drug to establish it as effective sedative and antimicrobial agent. This is based on the theory that the compound is expected to exhibit antimicrobial potency may be due to two benzene rings and secondary or tertiary nitrogen in its core molecule structure. For pursuing this objective, novel and structurally diverse analogs of the lead compound a-cyclohexyl-a-hydroxy-benzeneacetic acid-4-(diethylamino)-2-butynyl ester hydrochloride, a potential antispasmodic drug having two benzene rings and secondary or tertiary nitrogen in its structural framework were synthesized. All the synthesized compounds were confirmed by using physical data and different structure elucidation tools. The novel compounds were screened for their sedative, antibacterial and antifungal potential. The sedative potency of the compounds was evaluated using Thiopental sodium (Thiosol ®) as standard drug following one-way ANOVA followed by Scheffe’s post hoc analysis to find out the significance. The compounds were evaluated in vitro, for their antibacterial activity using acetone as a solvent and MIC was done by broth dilution method. The fungal susceptibility testing on different fungi was done by cup-diffusion method using Clotrimazole (100mcg/mL) as standard using acetone as a solvent. The compounds have shown promising results and definite structure-activity relationship could be established.