Savan S Bhalodiya, Mehul P Parmar, Chirag D Patel, Subham G Patel, Disha P Vala, Nandhakumar Suresh, Bhuvaneshwari Jayachandran, Madankumar Arumugam, Mahesh Narayan, Hitendra M Patel
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引用次数: 0
摘要
以冰乙酸为溶剂,通过 5-氨基[1,2,3]噻二唑、各种芳香醛和不同的乙酰乙酰苯胺的一锅反应,合成了一系列不同的 4,7-二氢-[1,2,3]噻二唑并[5,4-b]吡啶-6-甲酰胺 4(a-o),无需任何催化剂。所得化合物的产率从中等到良好。对所有新合成的化合物进行了抗菌活性评估。其中,与环丙沙星相比,化合物 4e 对革兰氏-(-Ve)-细菌中的溶血性沙林弧菌具有更强的抗菌效果。对 4d 和 4e 的理化特性进行了评估。根据对接分析,DHTDAPy 4e 在受体结合腔中的结合亲和力为 -7.2 kcal moL-1。这些研究结果说明了新合成的 DHTDAPy 对真菌和细菌感染的安全性、耐受性和有效性。
Acetic acid-driven one-pot synthesis of 4,7-dihydro-[1,2,3]thiadiazolo[5,4-b]pyridine-6-carboxamides and Pharmacological Evaluations.
A diverse set of 4,7-dihydro-[1,2,3]thiadiazolo[5,4-b]pyridine-6-carboxamides 4(a-o) were synthesized via a one-pot reaction of 5-amino[1,2,3]thiadiazole, various aromatic aldehydes, and different acetoacetanilides, using glacial acetic acid as the solvent and without the need for any catalysts. The resulting compounds were obtained in moderate to good yields. All the newly synthesized compounds were evaluated for their antimicrobial activity. Among them, compound 4e demonstrated superior efficacy against Salinivibrio proteolyticus strain of Gram-(-Ve)-bacteria compared to ciprofloxacin. Compound 4d exhibited the highest potency against the fungal strain Candida albicans surpassing Amphotericin B. 4d and 4e's physicochemical characteristics were assessed. According to docking analysis, DHTDAPy 4e shows the higher binding affinity of -7.2 kcal moL-1 in the binding cavity of the receptor. These findings illustrate the safety and tolerability as well as the potency of newly syntehsized DHTDAPy against the fungal and bacterial infections.
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