Design and Synthesis of 5-Oxoimidazolidine Derivatives in Search of Potent Antitubercular and Antifungal agents

被引:0
|
作者
Singirisetty, Triveni [1 ]
Chilamakuru, Naresh Babu [2 ]
Peraman, Ramalingam [2 ]
Mallela, Vijaya Jyothi [1 ]
Sana, Maheswari [1 ]
Begum, P. Inthiyaz [3 ]
机构
[1] Raghavendra Inst Pharmaceut Educ & Res, Dept Pharmaceut Chem, Ananthapuramu, Andhra Pradesh, India
[2] Raghavendra Inst Pharmaceut Educ & Res, RERDS CPR, Mol Modeling & Drug Discovery Div, Ananthapuramu, Andhra Pradesh, India
[3] Raghavendra Inst Pharmaceut Educ & Res RIPER, Dept Pharmaceut Qual Assurance, Ananthapuramu, Andhra Pradesh, India
关键词
Molecular docking; ADMET studies; 5-Oxoimidazolidines; Antitubercular activity; Antifungal activity;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
5-Oxoimidazolidines are significant outfits because of their impending biological activity and also because of their resourcefulness as synthons in organic revolutions. The designed library was docked against the crystal structure of Mycobacterium tuberculosis enoyl reductase (2B35) and crystal structure of flavohemoglobin (3OZU) to know the best fit molecule. The ADMET parameters revealed that the compounds have synthetic acceptability and leadlikeness. Accordingly, the selected 5-oxoimidazolidines (S1-8 and A(1-8)) were synthesized from carbohydrazides (1a-h) and characterized by spectral data. Further, these compounds were screened against M tuberculosis H37RV by microplate Alamar Blue assay method. The compound S-3 showed minimum inhibitory concentration at 6.25 mu g/mL, while the antifungal screening demonstrated S-1 as a promising lead with the corresponding zone of inhibitions of 22 mm and 18 mm against Aspergillus niger and Candida albicans.
引用
收藏
页码:441 / 451
页数:11
相关论文
共 50 条
  • [21] SYNTHESIS OF NEW PYRAZOLYL PYRROLE DERIVATIVES AS ANTITUBERCULAR AGENTS
    Hallikeri, Channabasappa S.
    Joshi, Shrinivas D.
    Yenni, Bhimsen
    Dixit, Sheshagiri
    Kulkarni, Venkatarao H.
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2017, 27 (01) : 17 - 23
  • [22] Design, synthesis, evaluation and optimization of novel azole analogues as potent antifungal agents
    Zhang, Juan
    Wang, Zhen
    Gai, Conghao
    Yun, Xiaoqing
    Jiang, Boye
    Zou, Yan
    Meng, Qingguo
    Zhao, Qingjie
    Chai, Xiaoyun
    BIOORGANIC & MEDICINAL CHEMISTRY, 2024, 97
  • [23] Design, synthesis, and in silico studies of pyrazine-based derivatives as potential antitubercular agents
    Ramesh, Madala
    Reddy, Pedavenkatagari Narayana
    Padmaja, Pannala
    Patil, Kalpesh R.
    Pawara, Rahul H.
    Rani, V. Saritha
    Ugale, Vinod G.
    JOURNAL OF MOLECULAR STRUCTURE, 2025, 1321
  • [24] Potent arylamide derivatives as dual-target antifungal agents: Design, synthesis, biological evaluation, and molecular docking studies
    Dong, Yue
    Liu, Xinyong
    An, Yunfei
    Liu, Min
    Han, Jun
    Sun, Bin
    BIOORGANIC CHEMISTRY, 2020, 99
  • [25] Design, synthesis, and mechanism study of novel tetrahydroisoquinoline derivatives as antifungal agents
    Chen, Yang
    Jin, Yanxi
    Wang, Luyao
    Wang, Wanxiang
    Zhou, Haiping
    Chen, Wei
    MOLECULAR DIVERSITY, 2024, : 2585 - 2599
  • [26] Design, Facile Synthesis and Characterization of Dichloro Substituted Chalcones and Dihydropyrazole Derivatives for Their Antifungal, Antitubercular and Antiproliferative Activities
    Shaik, Afzal B.
    Bhandare, Richie R.
    Nissankararao, Srinath
    Edis, Zehra
    Tangirala, N. Ravikiran
    Shahanaaz, Shaik
    Rahman, M. Mukhlesur
    MOLECULES, 2020, 25 (14):
  • [27] Design, synthesis and antifungal evaluation of borrelidin derivatives
    Hu, Caijuan
    Su, Hao
    Luo, Jinghan
    Han, Li
    Liu, Qingyin
    Wu, Wenxi
    Mu, Yu
    Guan, Peipei
    Sun, Tiemin
    Huang, Xueshi
    BIOORGANIC & MEDICINAL CHEMISTRY, 2018, 26 (23-24) : 6035 - 6049
  • [28] Synthesis, Characterization of (E)-N'-(substituted-benzylidene)isonicotino-hydrazide Derivatives as Potent Antitubercular Agents
    Malhotra, Manav
    Sharma, Rajiv
    Monga, Vikramdeep
    Deep, Aakash
    Sahu, Kapendra
    Samad, Abdul
    LETTERS IN DRUG DESIGN & DISCOVERY, 2011, 8 (06) : 575 - 579
  • [29] Design and synthesis of camphor-thiazole derivatives as potent antifungal agents: structure-activity relationship and preliminary mechanistic study
    Dai, Peng
    Ma, Zihua
    Dang, Yuncong
    Huang, Jiaxuan
    Xue, Huizhen
    Sun, Yafang
    Gu, Yu-Cheng
    Xia, Qing
    Zhang, Weihua
    PEST MANAGEMENT SCIENCE, 2025, 81 (03) : 1592 - 1602
  • [30] Synthesis of 2-Amino-5-aryl-1,3,4-thiadiazolopeptides as Potent Antitubercular Agents
    Asif, Karigar
    Himaja, M.
    Ramana, M. V.
    Sikarwar, Mukesh S.
    ASIAN JOURNAL OF CHEMISTRY, 2012, 24 (06) : 2739 - 2743