دورية أكاديمية

Exploring synthetic and therapeutic prospects of new thiazoline derivatives as aldose reductase (ALR2) inhibitors.

التفاصيل البيبلوغرافية
العنوان: Exploring synthetic and therapeutic prospects of new thiazoline derivatives as aldose reductase (ALR2) inhibitors.
المؤلفون: Shehzad MT; Institute of Chemical Sciences, Bahauddin Zakariya University Multan 60800 Pakistan zahidshafiq@bzu.edu.pk., Imran A; Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus Abbottabad 22060 Pakistan drjamshed@ciit.net.pk jamshediqb@googlemail.com., Hameed A; Department of Chemistry, Forman Christian College (A Chartered University) Ferozepur Road Lahore 54600 Pakistan.; Department of Chemistry, University of Sahiwal Sahiwal 57000 Pakistan., Rashida MA; Department of Chemistry, Forman Christian College (A Chartered University) Ferozepur Road Lahore 54600 Pakistan., Bibi M; Department of Biosciences, 90 and 100 Clifton, Shaheed Zulfikar Ali Bhutto Institute of Science and Technology Block 5, Clifton Karachi 75600 Pakistan., Uroos M; Institute of Chemistry, University of the Punjab Lahore 54590 Pakistan., Asari A; Faculty of Science and Marine Environment, Universiti Malaysia Terengganu 21030 Kuala Nerus Terengganu Malaysia., Iftikhar S; Department of Chemistry, University of Sahiwal Sahiwal 57000 Pakistan., Mohamad H; Institute of Marine Biotechnology, Universiti Malaysia Terengganu 21030 Kuala Nerus Terengganu Malaysia., Tahir MN; Department of Physics, University of Sargodha Sargodha Pakistan., Shafiq Z; Institute of Chemical Sciences, Bahauddin Zakariya University Multan 60800 Pakistan zahidshafiq@bzu.edu.pk., Iqbal J; Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus Abbottabad 22060 Pakistan drjamshed@ciit.net.pk jamshediqb@googlemail.com.
المصدر: RSC advances [RSC Adv] 2021 May 11; Vol. 11 (28), pp. 17259-17282. Date of Electronic Publication: 2021 May 11 (Print Publication: 2021).
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101581657 Publication Model: eCollection Cited Medium: Internet ISSN: 2046-2069 (Electronic) Linking ISSN: 20462069 NLM ISO Abbreviation: RSC Adv Subsets: PubMed not MEDLINE
أسماء مطبوعة: Original Publication: Cambridge [England] : Royal Society of Chemistry, [2011]-
مستخلص: Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable approach for the development of new antidiabetic agents. With our ongoing interest towards aldose reductase (ALR2) inhibition, we have synthesized and screened a series of thiazoline derivatives (5a-k, 6a-f, 7a-1 & 8a-j) to find a lead as a potential new antidiabetic agent. The bioactivity results showed the thiazoline-based compound 7b having a benzyl substituent and nitrophenyl substituent-bearing compound 8e were identified as the most potent molecules with IC 50 values of 1.39 ± 2.21 μM and 1.52 ± 0.78 μM respectively compared with the reference sorbinil with an IC 50 value of 3.14 ± 0.02 μM. Compound 7b with only 23.4% inhibition for ALR1 showed excellent selectivity for the targeted ALR2 to act as a potential lead for the development of new therapeutic agents for diabetic complications.
Competing Interests: The authors declare no conflict of interest.
(This journal is © The Royal Society of Chemistry.)
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تواريخ الأحداث: Date Created: 20220428 Latest Revision: 20220430
رمز التحديث: 20221213
مُعرف محوري في PubMed: PMC9033183
DOI: 10.1039/d1ra01716k
PMID: 35479726
قاعدة البيانات: MEDLINE
الوصف
تدمد:2046-2069
DOI:10.1039/d1ra01716k